C-MYC mRNA translation modulators and their use in treatment of cancer

Abstract

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

Description

Technical Field

[0001] This invention relates to novel c-MYC mRNA translation regulators, their compositions and preparation methods, and their use in cancer treatment. Background Technology

[0002] In the United States, cancer is the second leading cause of death, after heart disease. It accounts for one in four deaths in the U.S. The five-year relative survival rate for all cancers 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 incidence of new cancer cases decreased by an average of 0.6% per year in men, while it remained unchanged in women. From 2000 to 2009, the combined mortality rate from all cancers decreased by an average of 1.8% per year in men and 1.4% per year in women. This improved survival reflects advancements in early diagnosis and treatment. The discovery of highly effective, low-toxicity anticancer agents is a primary goal of cancer research.

[0003] The Myc family comprises three main members: the proto-oncogene c-Myc (myeloma cell line), L-myc, and N-myc. These three Myc homologs are involved in the early oncogenesis and metastatic spread of most human cancers. In most types of tumors, the Myc gene is not mutated or replicated, but its mRNA and / or protein levels are increased, indicating that Myc overexpression is induced at the transcriptional, mRNA homeostasis, and translational levels in cancer. Indeed, Myc gene expression is generally dependent on growth factor signaling, and both Myc mRNA and Myc protein have very short half-lives (30 min and 20 min, respectively) [Dang, CV (2012). MYC on the path to cancer. Cell 149, 22-35]. However, in tumor cells, the cellular level of Myc becomes independent of such signaling and regulation, and the resulting amplified Myc function drives intracellular and extracellular transcriptional programs, thereby allowing tumor growth and proliferation. However, Myc does not necessarily need to be overexpressed to make cancer highly dependent on its activity. A study by Soucek et al. (Nature (2008) 455(7213):679-83) showed that tumors expressing c-Myc at endogenous levels exhibited tumor regression after Myc was inhibited by a genetically engineered system. Therefore, treatment with Myc inhibitors is not necessarily limited to cancers that overexpress Myc. The compounds according to the invention can also be used to regulate the translation of Myc mRNA, wherein the direct target of the compounds is a protein or RNA that regulates the translation of Myc mRNA, and therefore any Myc-dependent tumor will benefit from the therapeutic efficacy of these compounds.

[0004] Due to its broad pathogenic significance, MYC is an important anti-cancer target. Dysregulated Myc genes have been found in a wide range of human hematologic malignancies and solid tumors, particularly in breast cancer, ovarian cancer, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin's and 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-origin lymphoma, esophageal squamous cell carcinoma, osteosarcoma, bladder cancer, pancreatic cancer, and lung adenocarcinoma. Recent studies have also shown that c-MYC dysregulation is associated with the development of BRAF V600E thyroid cancer, choroid plexus carcinoma, and colitis-related cancers. Furthermore, MYC gene amplification has been found in numerous cases of epithelial ovarian cancer. In the TCGA dataset, Myc amplification occurs in several cancer types, including breast cancer, colorectal cancer, pancreatic cancer, stomach cancer, and uterine cancer.

[0005] Although the Myc gene is a very important oncogene and is considered a driver of oncogenesis, and the MYC protein is a key transcription factor that broadly targets a variety of genes, the rational design of direct Myc inhibitors remains challenging. This is mainly because the MYC protein lacks structural regions that are easily therapeutically inhibited by small molecules and is considered a druggable target [BioDrugs (2019) 33:539–553].

[0006] Designing and developing MYC regulators is challenging, primarily because the MYC protein has a disordered structure lacking pockets or grooves that can serve as binding sites for regulators. Interference with MYC transcription, blocking protein-protein interactions (PPIs) between MYC and its cofactors, and influencing MYC-related signaling pathways have been considered potential regulatory targets in the past but have failed to be developed as drug candidates. Myc PPI inhibitors have failed to demonstrate sufficient efficacy in cell-based assays and animal models because high target occupancy is required to drive efficacy. Regulators of upstream myc signaling pathways (e.g., mTOR regulators) fail due to a lack of target specificity.

[0007] Nevertheless, therapeutic approaches targeting c-Myc remain elusive. The lack of a well-defined ligand-binding domain presents a formidable barrier to direct inhibition, a challenging feature shared by many compelling transcriptional targets in cancer. Therefore, as outlined in this article, alternative approaches to targeting Myc are needed, namely compounds that regulate Myc mRNA translation. Summary of the Invention

[0008] This invention provides a compound or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof, having the structures defined below by formulas I(j), I(n), and / or I(o) and the structural representations listed in Table 1. In various embodiments, the compound is a c-MYC mRNA translation regulator. In various embodiments, the compound is a c-MYC mRNA transcription regulator. In various embodiments, the compound is a c-MYC inhibitor. In various embodiments, the compound is any combination of a c-MYC mRNA translation regulator, a c-MYC mRNA transcription regulator, and a c-MYC inhibitor.

[0009] The present invention further provides a pharmaceutical composition comprising: a compound or a pharmaceutically acceptable salt thereof, a stereoisomer, a tautomer, a hydrate, an N-oxide, a prodrug, an isotope variant (e.g., a deuterated analog), a PROTAC, a pharmaceutical product thereof, or any combination thereof, having the structure of formula I(j), I(n) and / or I(o) as defined below and the structural representations listed in Table 1; and a pharmaceutically acceptable carrier.

[0010] The present invention further provides a method for treating, inhibiting, reducing the severity of cancer in a subject, reducing the risk of developing cancer in a subject, or suppressing cancer in a subject, the method comprising administering to a subject suffering from cancer, under conditions that effectively treat, inhibit, reduce the severity of cancer in a subject, reduce the risk of developing cancer in a subject, or suppress cancer in a subject, a compound represented by a structure of formula I(j), I(n), and / or I(o) as defined below and a compound represented by a structure listed in Table 1.

[0011] The present invention further provides a method for inhibiting, reducing, or suppressing tumor growth in a subject, the method comprising administering to the subject, under conditions that effectively inhibit, reduce, or suppress tumor growth, a compound represented by a structure of formula I(j), I(n), and / or I(o) as defined below and a compound represented by a structure listed in Table 1. In some embodiments, the tumor is cancerous. In some embodiments, the subject has cancer.

[0012] The present invention further provides a method for regulating c-MYC mRNA translation in cells, the method comprising contacting a compound represented by a structure of formula I(j), I(n) and / or I(o) as defined below and a structure listed in Table 1 with a cell, thereby regulating c-MYC mRNA translation in the cell.

[0013] The present invention further provides a method for regulating c-MYC mRNA transcription in cells, the method comprising contacting a compound represented by a structure of formula I(j), I(n) and / or I(o) as defined below and a structure listed in Table 1 with a cell, thereby regulating c-MYC mRNA transcription in the cell. Attached Figure Description

[0014] The patent or application document contains at least one color drawing. Upon request and payment of the necessary fees, the Patent Office will provide a copy of the patent or patent application publication with the color drawing.

[0015] Figure 1This study demonstrates how protein synthesis monitoring (PSM) specifically monitors c-Myc synthesis. The assay system comprises the human non-small cell lung cancer cell line A549, which expresses high levels of c-Myc. Two tRNAs (di-tRNAs) decoding a specific glutamine codon and a specific serine codon were transfected using either control RNAi or c-Myc-specific RNAi. FRET signaling specifically monitors c-Myc translation because FRET signaling is suppressed in cells treated with c-Myc siRNA. Blue represents cell nuclei stained with DAPI; yellow represents FRET signals from the tRNA pair decoding the glutamine-serine double codon.

[0016] Figure 2 The selective regulation of c-Myc translation was depicted. Insets show metabolic markers in A549 cells treated with a mediator, the universal translation inhibitor cyclohexylimide, or an anti-c-Myc compound. Treatment with cyclohexylimide resulted in complete inhibition of global protein synthesis, while treatment with the test compound showed no significant effect. Gray areas represent cell nuclei stained with DAPI; yellow areas represent L-azidoalanine (AHA) metabolic markers.

[0017] Figure 3 The effects of the compounds on mRNA treatment / stability levels are illustrated. A549 cells were exposed to a mediator, the universal transcription inhibitor actinomycin D, or an anti-c-Myc compound. In the top inset, treatment with actinomycin D or the test compound resulted in a significant reduction in c-Myc protein levels. The bottom inset shows that treatment with actinomycin D completely reduced c-Myc mRNA levels and transcription sites. Although treatment with the test compound reduced c-Myc mRNA levels by 30%, it did not affect transcription sites. Gray represents cell nuclei stained with DAPI; red represents c-Myc protein; purple represents c-Myc mRNA; and yellow represents c-Myc transcription sites.

[0018] Figure 4 The efficacy of the compound according to the invention in A549 cells was demonstrated.

[0019] Figure 5 shows the in vivo data for compound 332. Compound 332 inhibits c-Myc-dependent tumor growth in vivo. The relative tumor volume of A549 xenografts in NMRI-treated female nude mice after treatment with the compound at 3 mg / kg twice weekly for 49 days is also shown. Error bars represent median ± SEM values, n = 10 mice at each time point, and analysis was performed using a one-tailed T-test in Prism. *p < 0.05 Detailed Implementation

[0020] In various embodiments, the present invention relates to a compound having the structure represented by formula (I):

[0021]

[0022] in

[0023] X2, X3, and X4 are each independently nitrogen or CH;

[0024] X5, X6, X7, X8, and X9 are each independently nitrogen or carbon atoms;

[0025] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0026] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0027] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH(CH3)2) ), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), optionally wherein the alkoxy At least one methylene (CH2) is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted; saturated or unsaturated; single; fused; bridged; or spiro 3-10 Monocyclic heterocycles (e.g., piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0028] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanes, piperazines, 2-(piperazin-1-yl)acetamide);

[0029] Or R6 can be represented by the structure of formula B or Bi:

[0030]

[0031] in

[0032] m is 0 or 1; and

[0033] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0034] R 12 and R 13 Both are H;

[0035] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0036] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0037] R 12 and R 13 Connect to form ring B; or

[0038] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0039] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0040] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0041] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0042] in

[0043] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine;

[0044] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0045] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0046] R7 is H, F, Cl, Br, I, OH, OR 20 SH, R8-OH, R8-SH, SR 10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 (COO-CH3), R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR (e.g., C(O)NH(CH3)), C(O)N(R) 10 (R) 11 (For example, C(O)NH(CH3), C(O)NH(CH2CH3), C(O)NH(CH2CH2OCH3), C(O)NH(CH2CH2OH)), SO2R, SO2N(R) 10 (R) 11), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., methylimidazolium, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy, ethoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkyl, C1-C5 straight-chain or branched thioalkoxy, C1-C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclopropanol, cyclohexyl, bicyclo[1.1.1]pentane), substituted or Unsubstituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3-cyanopyrrolidine, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-) Alcohols, piperidine-2-ones, piperidine-4-carboxynitriles, 4-fluoropiperidine, oxadiazoles, triazoles, pyrazoles, 2-oxopyrrolidines, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, piperazine-2-ones), R8- (substituted or unsubstituted mono, fused or spiro3-8-membered heterocycles), substituted or unsubstituted aryl groups, substituted or unsubstituted benzyl groups;

[0047] Or R7 can be represented by the structure of equation A:

[0048]

[0049] in

[0050] X1 is N or O;

[0051] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0052] R1 and R2 may be connected to form an =O or C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0053] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethylene, aminoethylene), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0054] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0055] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0056] If X1 is 0, then R4 does not exist;

[0057] R7' is H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0058] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0059] R 20 It can be represented by the following structure:

[0060]

[0061] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0062] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0063] Each R8 is independently [CH2] p

[0064] Where p is between 1 and 10;

[0065] R9 is [CH] q [C] q

[0066] Where q is between 2 and 10;

[0067] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0068] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0069] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0070] In various embodiments, the present invention relates to a compound having the structure represented by formula I(a):

[0071]

[0072] in

[0073] X2, X3, and X4 are each independently nitrogen or CH;

[0074] X5, X6, X7, X8, and X9 are each independently either nitrogen or carbon atoms;

[0075] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0076] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0077] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10(e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH) (CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), Optionally, at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted 3-8 membered heterocycles (e.g., Piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0078] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanes, piperazines, 2-(piperazin-1-yl)acetamide);

[0079] Or R6 can be represented by the structure of formula B or Bi:

[0080]

[0081] in

[0082] m is 0 or 1; and

[0083] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0084] R 12 and R 13 Both are H;

[0085] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0086] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0087] R 12 and R 13 Connect to form ring B; or

[0088] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0089] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0090] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0091] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0092] in

[0093] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0094] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0095] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0096] R7 is OR 20 , SH, R8-OH, R8-SH, SR 10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), CD3, OCD3, NO2, -CH2CN, -R8CN, R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHCO-N(R 10 (R) 11 ), R8-C(O)-R 10 SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched thioalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, pyrrolidine-3-carboxynitrile, 3-cyanopyrrole). Alkane, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-ol, piperidine-2-one, piperidine-4-carboxynitrile, 4-fluoropiperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, piperazine-2-one), R8- (substituted or unsubstituted mono, fused or spiro3-8-membered heterocycles), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0097] Or R7 can be represented by the structure of equation A:

[0098]

[0099] in

[0100] X1 is N or O;

[0101] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0102] Or R1 and R2 can be connected to form a C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0103] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethyl, aminoethyl), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0104] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0105] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0106] If X1 is 0, then R4 does not exist;

[0107] R7' is H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0108] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0109] R 20 It can be represented by the following structure:

[0110]

[0111] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0112] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0113] Each R8 is independently [CH2] p

[0114] Where p is between 1 and 10;

[0115] R9 is [CH] q [C] q

[0116] Where q is between 2 and 10;

[0117] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0118] Or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0119] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0120] In various embodiments, the present invention relates to a compound having the structure represented by formula I(b):

[0121]

[0122] in

[0123] X2, X3, and X4 are each independently nitrogen or CH;

[0124] X5, X6, X7, X8, and X9 are each independently nitrogen or carbon atoms;

[0125] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0126] R6 is F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl groups) (e.g., CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), (CH2)3-pyran, CH2-tetrahydrofuran, CH2-dioxane, CH2-methyl-THF, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-methyl-azacyclobutane, CH2-azaspiroheptane, CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R)11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3) 2. CH(CH2OH)(CH2CH(CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy The alkoxy group may contain: alkyl group, O-(CH2)2-O-CH3), optionally wherein at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy group; C1-C5 straight-chain or branched haloalkoxy group; C1-C5 straight-chain or branched alkoxyalkyl group; substituted or unsubstituted C3-C8 cycloalkyl group (e.g., methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); substituted or unsubstituted 3-8 member alkyl groups. Heterocyclic compounds (e.g., piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azispiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted benzyl groups;

[0127] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanes, piperazines, 2-(piperazin-1-yl)acetamide);

[0128] Or R6 can be represented by the structure of formula B or Bi:

[0129]

[0130] in

[0131] m is 0 or 1; and

[0132] R 12 It is R 20Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0133] R 12 and R 13 Both are H; or

[0134] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0135] R 12 and R 13 Linked to form substituted or unsubstituted pyrrolidine rings, 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

[0136] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0137] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0138] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0139] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0140] in

[0141] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0142] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0143] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0144] R7 is H, F, Cl, Br, I, OH, OR 20 SH, R8-OH, R8-SH, SR 10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 (COO-CH3), R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR (e.g., C(O)NH(CH3)), C(O)N(R) 10 (R) 11 (For example, C(O)NH(CH3), C(O)NH(CH2CH2OCH3), C(O)NH(CH2CH2OH)), SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methylimidazolium, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl groups (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy groups (e.g., methoxy, ethoxy), optionally wherein at least one methylene (CH2) of said alkoxy group is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkyl groups, C1-C5 straight-chain or branched thioalkoxy groups, C1-C5 straight-chain or branched haloalkoxy groups, C1-C5 straight-chain or branched alkoxyalkyl groups, substituted or unsubstituted C3-C8 cyclic alkyl groups (e.g., cyclopropyl, cyclopropanol, cyclohexyl, bicyclo[1.1.1]pentane), substituted or unsubstituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, pyrrolidine-3-carboxynitrile, 3-cyanopyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, etc.) Piperidine-4-ol, piperidine-2-one, piperidine-4-carboxynitrile, 4-fluoropiperidine, oxadiazole, triazole, 2-oxopyrrolidine, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, piperazine-2-one), R8- (substituted or unsubstituted mono, fused or spiro3-8-membered heterocycles), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0145] Or R7 can be represented by the structure of equation A:

[0146]

[0147] in

[0148] X1 is N or O;

[0149] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0150] R1 and R2 may be connected to form an =O or C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0151] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethylene, aminoethylene), -R8-OR 10(e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0152] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0153] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0154] If X1 is 0, then R4 does not exist;

[0155] R7' is H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R)10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0156] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0157] R 20 It can be represented by the following structure:

[0158]

[0159] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0160] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0161] Each R8 is independently [CH2] p

[0162] Where p is between 1 and 10;

[0163] R9 is [CH] q [C] q

[0164] Where q is between 2 and 10;

[0165] R 10 and R 11Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0166] Or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0167] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0168] In various embodiments, the present invention relates to a compound having the structure represented by formula I(c):

[0169]

[0170] in

[0171] X2, X3, and X4 are each independently nitrogen or CH;

[0172] X5, X6, X7, X8, and X9 are each independently nitrogen or carbon atoms;

[0173] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0174] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0175] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R)11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH) (CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), Optionally, at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted 3-8 membered heterocycles (e.g., Piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0176] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanes, piperazines, 2-(piperazin-1-yl)acetamide);

[0177] Or R6 can be represented by the structure of formula B or Bi:

[0178]

[0179]

[0180] in

[0181] m is 0 or 1; and

[0182] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0183] R 12 and R 13 Both are H;

[0184] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0185] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0186] R 12 and R 13 Connect to form ring B; or

[0187] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0188] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0189] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0190] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0191] in

[0192] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0193] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0194] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0195] R7 represents Br, I, OH, and OR. 20 , SH, R8-OH, R8-SH, SR 10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 (COO-CH3), R8-C(O)-R 10 C(O)H, C(O)-R 10C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR (e.g., C(O)NH(CH3)), C(O)N(R) 10 (R) 11 (For example, C(O)NH(CH3), C(O)NH(CH2CH2OCH3), C(O)NH(CH2CH2OH)), SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 ), C1-C5 straight or branched, substituted or unsubstituted alkyl (e.g., methylimidazolium, methyl, ethyl), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight or branched thioalkyl, C1-C5 straight or branched thioalkoxy, C1-C5 straight or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclopropanol, cyclohexylbicyclo[1.1.1]pentane), substituted or unsubstituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3). - Alcohols, pyrrolidines, pyrrolidine-2-ols, pyrrolidine-3-ols, 3-methoxypyrrolidines, 1-methylpyrrolidines, pyrrolidine-2-ones, pyrrolidine-3-ones, 3-cyanopyrrolidines, pyrrolidones, imidazoles, pyrazoles, isoxazolidines, piperazines, piperidines, piperidine-3-ols, piperidine-4-ols, piperidine-2-ones, piperidine-4-carboxynitrile, 4-fluoropiperidines, oxadiazoles, triazoles, pyrazoles, 2-oxopyrrolidines, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, piperazine-2-ones), R8- (substituted or unsubstituted mono, fused or spiro3-8-membered heterocycles), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0196] Or R7 can be represented by the structure of equation A:

[0197]

[0198] in

[0199] X1 is N or O;

[0200] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0201] R1 and R2 may be connected to form an =O or C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0202] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethylene, aminoethylene), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0203] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0204] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0205] If X1 is 0, then R4 does not exist;

[0206] R7' is F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0207] R7' is different from R7;

[0208] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0209] R 20 It can be represented by the following structure:

[0210]

[0211] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0212] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0213] Each R8 is independently [CH2] p

[0214] Where p is between 1 and 10;

[0215] R9 is [CH] q [C] q

[0216] Where q is between 2 and 10;

[0217] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0218] Or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 1 and 4 (e.g., 1, 2);

[0219] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0220] In various embodiments, the present invention relates to a compound having the structure represented by formula I(d):

[0221]

[0222] in

[0223] X2, X3, and X4 are each independently nitrogen or CH;

[0224] X5, X6, X7, X8, and X9 are each independently nitrogen or carbon atoms;

[0225] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0226] Among them, X2, X3, X4, X5, X6, X7, X8, X9 or X 10 At least one of them is N;

[0227] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0228] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example,

[0229] (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11(e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH) (CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), Optionally, at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted 3-8 membered heterocycles (e.g., Piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0230] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanes, piperazines, 2-(piperazin-1-yl)acetamide);

[0231] Or R6 can be represented by the structure of formula B or Bi:

[0232]

[0233] in

[0234] m is 0 or 1; and

[0235] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0236] R 12 and R 13 Both are H;

[0237] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0238] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0239] R 12 and R 13 Connect to form ring B; or

[0240] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0241] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0242] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0243] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0244] in

[0245] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0246] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0247] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0248] R7 is H, F, Cl, Br, I, OH, OR 20 SH, R8-OH, R8-SH, SR 10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 (COO-CH3), R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR (e.g., C(O)NH(CH3)), C(O)N(R) 10 (R) 11 (For example, C(O)NH(CH3), C(O)NH(CH2CH2OCH3), C(O)NH(CH2CH2OH)), SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methylimidazolium, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl groups (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy groups (e.g., methoxy, ethoxy), optionally wherein at least one methylene (CH2) of the alkoxy group is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkyl groups, C1-C5 straight-chain or branched thioalkoxy groups, C1-C5 straight-chain or branched haloalkoxy groups, C1-C5 straight-chain or branched alkoxyalkyl groups, substituted or unsubstituted C3-C8 cyclic alkyl groups (e.g., cyclopropyl, cyclopropanol, cyclohexylbicyclo[1.1.1]pentane), substituted or unsubstituted Substituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3-cyanopyrrolidine, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-) Alcohols, piperidine-2-ones, piperidine-4-carboxynitriles, 4-fluoropiperidine, oxadiazoles, triazoles, pyrazoles, 2-oxopyrrolidines, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, piperazine-2-ones), R8- (substituted or unsubstituted mono, fused or spiro3-8-membered heterocycles), substituted or unsubstituted aryl groups, substituted or unsubstituted benzyl groups;

[0249] Or R7 can be represented by the structure of equation A:

[0250]

[0251] in

[0252] X1 is N or O;

[0253] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0254] R1 and R2 may be connected to form an =O or C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0255] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethylene, aminoethylene), -R8-OR 10(e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0256] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0257] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0258] If X1 is 0, then R4 does not exist;

[0259] R7' is H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R)10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0260] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0261] R 20 It can be represented by the following structure:

[0262]

[0263] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0264] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0265] Each R8 is independently [CH2] p

[0266] Where p is between 1 and 10;

[0267] R9 is [CH] q [C] q

[0268] Where q is between 2 and 10;

[0269] R 10 and R 11Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0270] Or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0271] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0272] In various embodiments, the present invention relates to a compound represented by the structure of formula I(e):

[0273]

[0274] in

[0275] X2, X3, and X4 are each independently nitrogen or CH;

[0276] X5, X6, X7, X8, and X9 are each independently nitrogen or carbon atoms;

[0277] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0278] R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanes, piperazines, 2-(piperazin-1-yl)acetamide);

[0279] R7 is H, F, Cl, Br, I, OH, OR 20 SH, R8-OH, R8-SH, SR 10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 (COO-CH3), R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR (e.g., C(O)NH(CH3)), C(O)N(R) 10 (R) 11 (For example, C(O)NH(CH3), C(O)NH(CH2CH2OCH3), C(O)NH(CH2CH2OH)), SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methylimidazolium, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl groups (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy groups (e.g., methoxy, ethoxy), optionally wherein at least one methylene (CH2) of the alkoxy group is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkyl groups, C1-C5 straight-chain or branched thioalkoxy groups, C1-C5 straight-chain or branched haloalkoxy groups, C1-C5 straight-chain or branched alkoxyalkyl groups, substituted or unsubstituted C3-C8 cyclic alkyl groups (e.g., cyclopropyl, cyclopropanol, cyclohexylbicyclo[1.1.1]pentane), substituted or unsubstituted Substituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3-cyanopyrrolidine, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-) Alcohols, piperidine-2-ones, piperidine-4-carboxynitriles, 4-fluoropiperidine, oxadiazoles, triazoles, pyrazoles, 2-oxopyrrolidines, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, piperazine-2-ones), R8- (substituted or unsubstituted mono, fused or spiro3-8-membered heterocycles), substituted or unsubstituted aryl groups, substituted or unsubstituted benzyl groups;

[0280] Or R7 can be represented by the structure of equation A:

[0281]

[0282] in

[0283] X1 is N or O;

[0284] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0285] R1 and R2 may be connected to form an =O or C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0286] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethylene, aminoethylene), -R8-OR 10(e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0287] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0288] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0289] If X1 is 0, then R4 does not exist;

[0290] R7' is H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R)10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0291] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0292] R 20 It can be represented by the following structure:

[0293]

[0294] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0295] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0296] Each R8 is independently [CH2] p

[0297] Where p is between 1 and 10;

[0298] R9 is [CH] q [C] q

[0299] Where q is between 2 and 10;

[0300] R 10 and R 11Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0301] Or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0302] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0303] In various embodiments, the present invention relates to a compound having the structure represented by formula I(f):

[0304]

[0305] in

[0306] A' is a 3- to 8-membered single or fused, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring (e.g., pyrrolidine, piperidine, piperazine, isochorium, 1,2,3,4-tetrahydroisoquinoline, indoline, isoyindoline, 1,3-dihydroisobenzofuran, 2,3-dihydro-1H-indene, 1,2,3,4-tetrahydronaphthalene);

[0307] X2, X3, and X4 are each independently nitrogen or CH;

[0308] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0309] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0310] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10(For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH) (CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), Optionally, at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted 3-8 membered heterocycles (e.g., Piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0311] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanane, piperazine, 2-(piperazin-1-yl)acetamide);

[0312] Or R6 can be represented by the structure of formula B or Bi:

[0313]

[0314]

[0315] in

[0316] m is 0 or 1; and

[0317] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0318] R 12 and R 13 Both are H;

[0319] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0320] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0321] R 12 and R 13 Connect to form ring B; or

[0322] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0323] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0324] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0325] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0326] in

[0327] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0328] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0329] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0330] R7 is H, F, Cl, Br, I, OH, OR 20 , SH, R8-OH, R8-SH, SR 10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 (COO-CH3), R8-C(O)-R 10 C(O)H, C(O)-R10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR (e.g., C(O)NH(CH3)), C(O)N(R) 10 (R) 11 (For example, C(O)NH(CH3), C(O)NH(CH2CH2OCH3), C(O)NH(CH2CH2OH)), SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methylimidazolium, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl groups (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy groups (e.g., methoxy, ethoxy), optionally wherein at least one methylene (CH2) of the alkoxy group is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkyl groups, C1-C5 straight-chain or branched thioalkoxy groups, C1-C5 straight-chain or branched haloalkoxy groups, C1-C5 straight-chain or branched alkoxyalkyl groups, substituted or unsubstituted C3-C8 cyclic alkyl groups (e.g., cyclopropyl, cyclopropanol, cyclohexylbicyclo[1.1.1]pentane), substituted or unsubstituted Substituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3-cyanopyrrolidine, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-) Alcohols, piperidine-2-ones, piperidine-4-carboxynitriles, 4-fluoropiperidine, oxadiazoles, triazoles, pyrazoles, 2-oxopyrrolidines, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, piperazine-2-ones), R8- (substituted or unsubstituted mono, fused or spiro3-8-membered heterocycles), substituted or unsubstituted aryl groups, substituted or unsubstituted benzyl groups;

[0331] Or R7 can be represented by the structure of equation A:

[0332]

[0333] in

[0334] X1 is N or O;

[0335] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0336] Or R1 and R2 can be connected to form an =O or C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0337] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethylene, aminoethylene), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0338] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0339] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0340] If X1 is 0, then R4 does not exist;

[0341] R7' is H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0342] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0343] R 20 It can be represented by the following structure:

[0344]

[0345] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R)11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0346] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0347] Each R8 is independently [CH2] p

[0348] Where p is between 1 and 10;

[0349] R9 is [CH] q [C] q

[0350] Where q is between 2 and 10;

[0351] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0352] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0353] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0354] In various embodiments, the present invention relates to a compound having the structure represented by formula I(g):

[0355]

[0356] in

[0357] X2, X3, and X4 are each independently nitrogen or CH;

[0358] X5, X6, X7, X8, and X9 are each independently either nitrogen or carbon atoms;

[0359] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0360] R 100 It is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group (e.g., methyl, ethyl), R8-OH (e.g., (CH2)2-OH), -R8-OR 10(e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (For example, (CH2)2-NH(CH3), (CH2)2-NH2), R 20 Or substituted or unsubstituted 3-8 membered heterocycles (e.g., pyrrolidine, piperidine);

[0361] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0362] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11(For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH) (CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), Optionally, at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted 3-8 membered heterocycles (e.g., Piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0363] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanane, piperazine, 2-(piperazin-1-yl)acetamide);

[0364] Or R6 can be represented by the structure of equation C:

[0365]

[0366] in

[0367] k is between 1 and 4;

[0368] R 12 and R 13 Each is independently H, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., ethyl, isopropyl), R 20 or

[0369] R 12 and R 13 Linked to form substituted or unsubstituted 4-7 membered heterocycles (e.g., piperidine, piperazine, pyrrolidine, oxa-6-azaspiro[3.3]heptane);

[0370] Or R6 can be represented by the structure of Bi:

[0371]

[0372] in

[0373] m is 0 or 1; and

[0374] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0375] R 12 and R 13 Both are H;

[0376] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0377] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0378] R 12 and R 13 Connect to form ring B; or

[0379] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0380] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0381] R 13Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0382] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0383] in

[0384] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0385] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0386] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0387] R7' is H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R)10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0388] R 20 It can be represented by the following structure:

[0389]

[0390] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0391] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0392] Each R8 is independently [CH2] p

[0393] Where p is between 1 and 10;

[0394] R9 is [CH] q [C] q

[0395] Where q is between 2 and 10;

[0396] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0397] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0398] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0399] In some embodiments, if R 100 If it is a methyl group and R5 is H, then R 12 and R 13 None of them are alkyl groups. In some embodiments, if R 100 If it is a methyl group and R5 is H, then R 12 and R 13 It cannot be linked to form piperidine.

[0400] In various embodiments, the present invention relates to a compound having the structure represented by formula I(h):

[0401]

[0402] in

[0403] X2, X3, and X4 are each independently nitrogen or CH;

[0404] X5, X6, X7, X8, and X9 are each independently either nitrogen or carbon atoms;

[0405] X 10It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0406] Ring F is absent or substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0407] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0408] R1 and R2 may be connected to form a 3-8 membered carbon ring or heterocycle (e.g., cyclopropyl);

[0409] Alternatively, R2 and R4 may be linked to form a ring F as defined above (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole), wherein if ring F is aromatic, then R1 and / or R3 are absent;

[0410] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethyl, aminoethyl), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;or

[0411] R3 and R4 are linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0412] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0413] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxocyclic heterocycles) Butane, (CH2)3-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11(e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH) (CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), Optionally, at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted 3-8 membered heterocycles (e.g., Piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0414] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanane, piperazine, 2-(piperazin-1-yl)acetamide);

[0415] Or R6 can be represented by the structure of formula B or Bi:

[0416]

[0417] in

[0418] m is 0 or 1; and

[0419] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0420] R 12 and R 13 Both are H;

[0421] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0422] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0423] R 12 and R 13 Connect to form ring B; or

[0424] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0425] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0426] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0427] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0428] in

[0429] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0430] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0431] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0432] R7' and R7" are independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0433] Or R7' and R7” are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0434] R 20 It can be represented by the following structure:

[0435]

[0436] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0437] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0438] Each R8 is independently [CH2] p

[0439] Where p is between 1 and 10;

[0440] R9 is [CH] q [C] q

[0441] Where q is between 2 and 10;

[0442] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0443] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0444] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0445] In various embodiments, the present invention relates to a compound having the structure represented by formula I(i):

[0446]

[0447] in

[0448] X2, X3, and X4 are each independently nitrogen or CH;

[0449] X5, X6, X7, X8, and X9 are each independently either nitrogen or carbon atoms;

[0450] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0451] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0452] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxocyclic heterocycles) Butane, (CH2)3-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R)11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH) (CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), Optionally, at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted 3-8 membered heterocycles (e.g., Piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0453] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanane, piperazine, 2-(piperazin-1-yl)acetamide);

[0454] Or R6 can be represented by the structure of formula B or Bi:

[0455]

[0456] in

[0457] m is 0 or 1; and

[0458] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0459] R 12 and R 13 Both are H;

[0460] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0461] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0462] R 12 and R 13 Connect to form ring B; or

[0463] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0464] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0465] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0466] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0467] in

[0468] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0469] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0470] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0471] R7, R7', R7”, R7”', and R7”” are each independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R)10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0472] The condition is that at least two of R7, R7', R7”, R7”', and R7”” are not H;

[0473] Or R7' and R7” are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0474] Or R7” and R7 are connected to form 3-8 substituted or unsubstituted carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0475] Or R7 and R7”’ are connected to form 3-8 substituted or unsubstituted carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0476] Or R7”' and R7”” are connected to form 3-8 substituted or unsubstituted carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0477] R 20 It can be represented by the following structure:

[0478]

[0479] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0480] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10(e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0481] Each R8 is independently [CH2] p

[0482] Where p is between 1 and 10;

[0483] R9 is [CH] q [C] q

[0484] Where q is between 2 and 10;

[0485] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0486] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0487] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0488] In various embodiments, the present invention relates to a compound having the structure represented by formula I(j):

[0489]

[0490] in

[0491] X2, X3, and X4 are each independently nitrogen or CH;

[0492] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0493] The ring W is a 3- to 10-membered single, fused, bridged, or spirocyclic, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-cyanopyrrolidine, 1-methylpyrrolidine, 3-(difluoromethyl)pyrrolidine, 3,3-difluoropyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-ol, etc.). 2-Pyridine-2-one, piperidine-4-carboxynitrile, 4-fluoropiperidine, oxadiazole, triazole, 2-oxopyrrolidine, cyclopropyl, 2,2-dimethylpyrrolidine, 4-azaspiro[2.4]heptane, pyrrolidine-3-one O-methyl oxime, 2-oxa-5-azaspiro[3.4]octane, 1,4-dioxa-6-azaspiro[4.4]nonane, 3,3-dimethylmorpholine, 1-methylpiperazine, 4,7-diazaspiro[2.5]octane, bicyclo[1.1.1]pentane, 2,5-diazabicyclo[2.2.1]heptane, piperazine, piperazine-2-one);

[0494] W1 is CH2, C=O, or CH(R) 10 (For example, CHCH3);

[0495] R7' and R7" are independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0496] Or R7' and R7” are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0497] R 20 It can be represented by the following structure:

[0498]

[0499] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0500] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0501] R 200 It is H, R 20 F, Cl, Br, I, OH, SH, alkoxy group, NH2, N(R)2, NH(R) 10 ), N(R 10 (R) 11), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups (e.g., methoxy), C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0502] or R 200 And the carbon atom it is attached to is C=O or CF2;

[0503] Each R8 is independently [CH2] p

[0504] Where p is between 1 and 10;

[0505] R9 is [CH] q [C] q

[0506] Where q is between 2 and 10;

[0507] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0508] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0509] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0510] In each embodiment, the compound is not (R)-2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide. In each embodiment, the compound is not (S)-2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide. In each embodiment, the compound is not 2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide.

[0511] In various embodiments, the present invention relates to a compound having the structure represented by formula I(k):

[0512]

[0513] in

[0514] X2, X3, and X4 are each independently nitrogen or CH;

[0515] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0516] Q1 is O, NH, or CH2;

[0517] Q2 is C=O, NH or CH2;

[0518] R7 and R7' are independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10(R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0519] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0520] R 20 It can be represented by the following structure:

[0521]

[0522] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0523] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0524] R 200 It is H, R 20,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups (e.g., methoxy), C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0525] or R 200 And the carbon atom it is attached to is C=O or CF2;

[0526] Each R8 is independently [CH2] p

[0527] Where p is between 1 and 10;

[0528] R9 is [CH] q [C] q

[0529] Where q is between 2 and 10;

[0530] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0531] or R 10 and R 11Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0532] t is an integer between 0 and 4 (e.g., 1, 2);

[0533] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0534] In each embodiment, the compound is not (R)-2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide. In each embodiment, the compound is not (S)-2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide. In each embodiment, the compound is not 2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide.

[0535] In various embodiments, the present invention relates to a compound having the structure represented by formula I(l):

[0536]

[0537] in

[0538] X2, X3, and X4 are each independently nitrogen or CH;

[0539] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0540] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0541] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10(For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH(CH3)2) ), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), optionally wherein the alkoxy At least one methylene (CH2) is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted; saturated or unsaturated; single; fused; bridged; or spiro 3-10 Monocyclic heterocycles (e.g., piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0542] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanane, piperazine, 2-(piperazin-1-yl)acetamide);

[0543] R7' and R7" are independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR NH(R 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0544] Or R7' and R7” are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0545] R 20 It can be represented by the following structure:

[0546]

[0547] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0548] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0549] R 200 It is H, R 20 F, Cl, Br, I, OH, SH, alkoxy group, NH2, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups (e.g., methoxy), C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10(e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0550] or R 200 And the carbon atom it is attached to is C=O or CF2;

[0551] Each R8 is independently [CH2] p

[0552] Where p is between 1 and 10;

[0553] R9 is [CH] q [C] q

[0554] Where q is between 2 and 10;

[0555] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0556] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0557] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0558] In various embodiments, R6 of the compound of formula I(l) is H, a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group (e.g., methyl), a substituted or unsubstituted 3-8 membered heterocycle (e.g., piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, each representing a separate embodiment according to the invention). In various embodiments, R6 is H. In various embodiments, R6 is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group. In various embodiments, R6 is methyl. In various embodiments, R6 is a substituted or unsubstituted 3-8 membered heterocycle. In various embodiments, R6 is piperidine. In various embodiments, R6 is 1-methylpiperidine. In various embodiments, R6 is 3-fluoro-1-methylpiperidine. In various embodiments, R6 is aziridine. In various embodiments, R6 is 1-methyl-aziridine. In various embodiments, R6 is morpholine. In various embodiments, R6 is tetrahydropyran. In various embodiments, R6 is tetrahydrofuran. In various embodiments, R6 is 8-methyl-8-azirbicyclo[3.2.1]octane. In various embodiments, R6 is dioxane. In various embodiments, R6 is 1,3-dioxane.

[0559] In various embodiments, the present invention relates to a compound whose structure is represented by formula I(m):

[0560]

[0561] in

[0562] X2, X3, and X4 are each independently nitrogen or CH;

[0563] X5, X6, X7, X8, and X9 are each independently either nitrogen or carbon atoms;

[0564] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0565] W1 is CH2, C=O, or CH(R) 10 (For example, CHCH3);

[0566] Ring F is absent or substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0567] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0568] R1 and R2 may be connected to form a 3-8 membered carbon ring or heterocycle (e.g., cyclopropyl);

[0569] Alternatively, R2 and R4 may be linked to form a ring F as defined above (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole), wherein if ring F is aromatic, then R1 and / or R3 are absent;

[0570] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethyl, aminoethyl), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;or

[0571] R3 and R4 are linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0572] R7' and R7" are independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0573] Or R7' and R7” are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0574] R20 It can be represented by the following structure:

[0575]

[0576] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0577] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10(e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0578] Each R8 is independently [CH2] p

[0579] Where p is between 1 and 10;

[0580] R9 is [CH] q [C] q

[0581] Where q is between 2 and 10;

[0582] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0583] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0584] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0585] In various embodiments, the present invention relates to a compound whose structure is represented by formula I(n):

[0586]

[0587] in

[0588] X2, X3, and X4 are each independently nitrogen or CH;

[0589] X 10It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0590] The ring W is a 3- to 10-membered single, fused, bridged, or spirocyclic, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-cyanopyrrolidine, 1-methylpyrrolidine, 3-(difluoromethyl)pyrrolidine, 3,3-difluoropyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-ol, etc.). 2-Pyridine-2-one, piperidine-4-carboxynitrile, 4-fluoropiperidine, oxadiazole, triazole, 2-oxopyrrolidine, cyclopropyl, 2,2-dimethylpyrrolidine, 4-azaspiro[2.4]heptane, pyrrolidine-3-one O-methyl oxime, 2-oxa-5-azaspiro[3.4]octane, 1,4-dioxa-6-azaspiro[4.4]nonane, 3,3-dimethylmorpholine, 1-methylpiperazine, 4,7-diazaspiro[2.5]octane, bicyclo[1.1.1]pentane, 2,5-diazabicyclo[2.2.1]heptane, piperazine, piperazine-2-one);

[0591] W1 is CH2, C=O, or CH(R) 10 (For example, CHCH3);

[0592] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0593] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R)11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH(CH3)2) ), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), optionally wherein the alkoxy At least one methylene (CH2) is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted; saturated or unsaturated; single; fused; bridged; or spiro 3-10 Monocyclic heterocycles (e.g., piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0594] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanane, piperazine, 2-(piperazin-1-yl)acetamide);

[0595] R7' and R7" are independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0596] Or R7' and R7” are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0597] R 20 It can be represented by the following structure:

[0598]

[0599] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0600] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0601] R 200 It is H, R 20 F, Cl, Br, I, OH, SH, alkoxy group, NH2, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups (e.g., methoxy), C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0602] or R 200 And the carbon atom it is attached to is C=O or CF2;

[0603] Each R8 is independently [CH2] p

[0604] Where p is between 1 and 10;

[0605] R9 is [CH] q [C] q

[0606] Where q is between 2 and 10;

[0607] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0608] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0609] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0610] In each embodiment, the compound is not (R)-2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide. In each embodiment, the compound is not (S)-2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide. In each embodiment, the compound is not 2-(2-fluoro-4-(pyrrolidone-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazolyl-7-carboxamide.

[0611] In various embodiments, the present invention relates to a compound having the structure represented by formula I(o):

[0612]

[0613] in

[0614] X2, X3, and X4 are each independently nitrogen or CH;

[0615] X5, X6, X7, X8, and X9 are each independently either nitrogen or carbon atoms;

[0616] X 10 It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0617] R1 is H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0618] R2 is a substituted or unsubstituted C1-C5 alkyl group (e.g., CH2OH, CH2OCH3), a 3-8 membered carbon ring, or a heterocyclic ring (e.g., oxetane);

[0619] R1 and R2 may be connected to form 3-8 membered carbon rings or heterocycles (e.g., cyclopropyl, oxetane);

[0620] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethyl, aminoethyl), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0621] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0622] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0623] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 (For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH(CH3)2) ), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), optionally wherein the alkoxy At least one methylene (CH2) is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted; saturated or unsaturated; single; fused; bridged; or spiro 3-10 Monocyclic heterocycles (e.g., piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0624] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanane, piperazine, 2-(piperazin-1-yl)acetamide);

[0625] R7' and R7" are independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0626] Or R7' and R7” are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0627] R 20 It can be represented by the following structure:

[0628]

[0629] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0630] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R) 11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0631] Each R8 is independently [CH2] p

[0632] Where p is between 1 and 10;

[0633] R9 is [CH] q [C] q

[0634] Where q is between 2 and 10;

[0635] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0636] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0637] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0638] In various embodiments, R7' is F. In various embodiments, R7" is H. In various embodiments, R1 is H. In various embodiments, R2 is a substituted C1-C5 alkyl group. In various embodiments, R2 is CH2OH. In various embodiments, R2 is CH2OCH3. In various embodiments, R2 is a 3-8 membered heterocycle. In various embodiments, R2 is oxetane. In various embodiments, R2 is 3-oxetane or 2-oxetane; each represents a separate embodiment. In various embodiments, R6 is H. In various embodiments, R6 is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group. Alkyl group. In various embodiments, R6 is methyl. In various embodiments, R6 is a substituted or unsubstituted, saturated or unsaturated, monolithic, fused, bridged, or spirocyclic 3-10-membered heterocycle. In various embodiments, R6 is a substituted or unsubstituted, saturated monolithic 3-8-membered heterocycle. In various embodiments, the heterocycle is tetrahydropyran. In various embodiments, R7' is F, R1 is H, and R6 is an unsubstituted C1-C5 straight-chain or branched alkyl group or a substituted or unsubstituted, saturated monolithic 3-8-membered heterocycle. In various embodiments, R7' is F, R1 is H, and R6 is methyl.

[0639] In various embodiments, the present invention relates to a compound having the structure represented by formula (II):

[0640]

[0641] in

[0642] X2, X3, and X4 are each independently nitrogen or CH;

[0643] X5, X6, X7, X8, and X9 are each independently either nitrogen or carbon atoms;

[0644] X 10It is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH));

[0645] R5 is an H or a C1-C5 straight-chain or branched alkyl group (e.g., methyl);

[0646] R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR 10 (e.g., CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2), R8-SR 10 (For example, (CH2)3-S-(CH2)2CH3), R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl) (e.g., CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol), R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles) (e.g., (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxazone) Cyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11(For example, (CH2)3-4-fluoropiperidine, (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3)), R8-C(O)N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), R9-R8-N(R 10 (R) 11 (e.g., (CH2)2-C(O)-piperidine), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH) (CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2), C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy (e.g., methoxy, O-(CH2)2-O-CH3), Optionally, at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy; C1-C5 straight-chain or branched haloalkoxy; C1-C5 straight-chain or branched alkoxyalkyl; substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole); R8- (substituted or unsubstituted C3-C8 cycloalkyl); substituted or unsubstituted 3-8 membered heterocycles (e.g., Piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane), substituted or unsubstituted aryl groups, substituted or unsubstituted R8-aryl groups (e.g., benzyl), substituted or unsubstituted benzyl groups;

[0647] Or R6 and R5 are linked to form substituted or unsubstituted 5-8 membered heterocycles (e.g., azirroheptanane, piperazine, 2-(piperazin-1-yl)acetamide);

[0648] Or R6 can be represented by the structure of formula B or Bi:

[0649]

[0650]

[0651] in

[0652] m is 0 or 1; and

[0653] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0654] R 12 and R 13 Both are H;

[0655] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl);

[0656] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0657] R 12 and R 13 Connect to form ring B; or

[0658] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0659] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0660] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0661] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0662] in

[0663] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (e.g., A: pyrrolidine, methylpyrrolidine, ethylpyrrolidine); C: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, 2-azaspiro[3.3]heptane; E: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, methylpiperidine);

[0664] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle (B: piperidine, piperidin-2-one, 4-fluoropiperidin-2-one, piperidin-4-carboxynitrile, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, methyl-piperidine, fluoropiperidine, difluoropiperidine, pyrrolidine, piperazine, methylpyrrolidine, thiomorpholine 1,1-dioxide, 2-oxa-6-azaspiro[3.3]heptane, methyl-piperazine, dimethyl-pyrazole, imidazole, 2-methyl-2,5-diazabicyclo[2.2.1]heptane, hydroxymethyl-pyrrolidine, dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane; and

[0665] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group (e.g., cyclobutane, cyclohexane);

[0666] R7 is H, F, Cl, Br, I, OH, OR 20 , SH, R8-OH, R8-SH, SR 10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 (COO-CH3), R8-C(O)-R 10 C(O)H, C(O)-R 10C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR (e.g., C(O)NH(CH3)), C(O)N(R) 10 (R) 11 (For example, C(O)NH(CH3), C(O)NH(CH2CH3), C(O)NH(CH2CH2OCH3), C(O)NH(CH2CH2OH)), SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., methylimidazolium, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy, ethoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkyl, C1-C5 straight-chain or branched thioalkoxy, C1-C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclopropanol, cyclohexyl, bicyclo[1.1.1]pentane), substituted or Unsubstituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3-cyanopyrrolidine, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-) Alcohols, piperidine-2-ones, piperidine-4-carboxynitriles, 4-fluoropiperidine, oxadiazoles, triazoles, pyrazoles, 2-oxopyrrolidines, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, piperazine-2-ones), R8- (substituted or unsubstituted mono, fused or spiro3-8-membered heterocycles), substituted or unsubstituted aryl groups, substituted or unsubstituted benzyl groups;

[0667] Or R7 can be represented by the structure of equation A:

[0668]

[0669] in

[0670] X1 is N or O;

[0671] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy.

[0672] Or R1 and R2 can be connected to form an =O or C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0673] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethylene, aminoethylene), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0674] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0675] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0676] If X1 is 0, then R4 does not exist;

[0677] R7' is H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy, C1 -C5 straight-chain or branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycles (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl;

[0678] Or R7 and R7' are connected to form 3-8 substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic rings (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine);

[0679] R 20 It can be represented by the following structure:

[0680]

[0681] R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 ), N(R 10 (R)11 ), CF3, CN, NO2, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight-chain or branched alkoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0682] R is H, F, Cl, Br, I, OH, SH, alkoxy group, NH (R 10 ), NH-CH2-cyclopropyl, N(R 10 (R) 11 ), CF3, CN, NO2, COOH, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl groups, cyclopropyl, C1-C5 straight-chain or branched alkoxy groups, isopropoxy groups, C1-C5 straight-chain or branched haloalkyl groups (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl groups (e.g., phenyl), substituted or unsubstituted heteroaryl groups (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine));

[0683] Each R8 is independently [CH2] p

[0684] Where p is between 1 and 10;

[0685] R9 is [CH] q [C] q

[0686] Where q is between 2 and 10;

[0687] R 10 and R 11 Each of the following is independently H, a C1-C5 substituted or unsubstituted straight-chain or branched alkyl group (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), a C1-C5 substituted or unsubstituted straight-chain or branched haloalkyl group (e.g., CH2CF3), a C1-C5 straight-chain or branched alkoxy group (e.g., O-CH3), or R 20 , C(O)R or S(O)2R;

[0688] or R 10 and R 11 Linked to form substituted or unsubstituted 3-8 membered heterocycles (e.g., piperazine, piperidine), where n is an integer between 0 and 4 (e.g., 1, 2);

[0689] Or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotope variant (e.g., deuterated analog), PROTAC, pharmaceutical product, or any combination thereof.

[0690] In some embodiments, X2 in formulas I, II, and / or I(a)-I(o) is a nitrogen atom. In other embodiments, X2 is CH.

[0691] In some embodiments, X3 in formulas I, II, and / or I(a)-I(o) is a nitrogen atom. In other embodiments, X3 is CH.

[0692] In some embodiments, X4 in formulas I, II, and / or I(a)-I(o) is a nitrogen atom. In other embodiments, X4 is CH.

[0693] In some embodiments, X5 of formulas I, II, I(a)-I(i), I(m) and / or I(o) is a nitrogen atom. In other embodiments, X5 is a carbon atom.

[0694] In some embodiments, X6 of formulas I, II, I(a)-I(i), I(m) and / or I(o) is a nitrogen atom. In other embodiments, X6 is a carbon atom.

[0695] In some embodiments, X7 in formulas I, II, and / or I(a)-I(e) is a nitrogen atom. In other embodiments, X7 is a carbon atom.

[0696] In some embodiments, X8 of formulas I, II, I(a)-I(i), I(m) and / or I(o) is a nitrogen atom. In other embodiments, X8 is a carbon atom.

[0697] In some embodiments, X9 of formulas I, II, I(a)-I(i), I(m) and / or I(o) is a nitrogen atom. In other embodiments, X9 is a carbon atom.

[0698] In some embodiments, X of formulas I, II and / or I(a)-I(o) 10 It is a nitrogen atom. In other embodiments, X... 10 It is N. In other embodiments, X 10 It is CH. In other embodiments, X 10 It is C(R), where R is defined below. In other embodiments, X 10 It is C(R), where R is an alkyl group. In other embodiments, X 10 It is C(R), where R is a methyl group. In other embodiments, X 10 It is C(R), where R is a cycloalkyl group. In other embodiments, X 10 It is C(R), where R is cyclopropyl. In other embodiments, X... 10 It is C(R), where R is COOH. In other embodiments, X... 10 It is C(R), where R is N(H)R 10 And R 10 It is a substituted alkyl group. In other embodiments, X 10 It is C(N(H)(CH2-cyclopropyl)). In other embodiments, X 10 It is C(R), where R is a substituted alkyl group. In other embodiments, X 10 It is C(R), where R is CH2-OH. In other embodiments, X 10 It is C(R), where R is CH2-CH2-OH. In other embodiments, X 10 It is C(R), where R is not an alkoxy group. In other embodiments, X 10 It is C(R), where R is isopropoxy.

[0699] In some embodiments, at least one of X2, X3, X4, X5, X6, X7, X8, and X9 in formulas I, II, I(a)-I(e) is a nitrogen atom. In some embodiments, at least one of X2, X3, X4, X5, X6, X8, and X9 in formulas I, II, I(a)-I(e), I(g)-I(i), I(m), and / or I(o) is a nitrogen atom. In some embodiments, at least one of X2, X3, X4, X5, X6, X7, X8, and X9 in formula I(d) is a nitrogen atom. In some embodiments, at least one of X2, X3, X4, X5, X6, X7, X8, and X9 in formula I(d) is a nitrogen atom. 10 At least one of them is a nitrogen atom.

[0700] In some embodiments, X2, X3, X4, and X of formulas I, II, and / or I(a)-I(o) 10 At least one of them is a nitrogen atom. In some embodiments, X2, X3, X4, and X of formula I(d) are nitrogen atoms. 10 At least one of them is a nitrogen atom. In some embodiments, at least one of X5, X6, X8 and X9 of formulas I, II and / or I(a)-I(o) is a nitrogen atom.

[0701] In some embodiments, R5 of formulas I, II, I(a)-I(d), I(f)-I(i), I(l), I(n) and / or I(o) is H. In other embodiments, R5 is a C1-C5 straight-chain or branched alkyl group. In other embodiments, R5 is methyl. In other embodiments, R5 is methyl, ethyl, propyl, isopropyl, butyl, tert-butyl, isobutyl, pentyl, or neopentyl; each representing a separate embodiment according to the invention.

[0702] In some embodiments, R5 and R6 of formulas I, II, and / or I(a)-I(i) are linked to form a substituted or unsubstituted 5-8 membered heterocycle. In some embodiments, R5 and R6 are linked to form a substituted 5-8 membered heterocycle. In some embodiments, R5 and R6 are linked to form an unsubstituted 5-8 membered heterocycle. In some embodiments, the heterocycle is an azaheptanane, piperazine, or 2-(piperazin-1-yl)acetamide; each representing a separate embodiment according to the invention. In some embodiments, the heterocycle is substituted by at least one of the following: F, Cl, Br, I, CF3, R 20 C1-C5 straight-chain or branched alkyl groups, C1-C5 straight-chain or branched haloalkyl groups, OH, alkoxy groups, R8-OH (e.g., CH2-OH), OMe, amides, C(O)N(R)2, C(O)N(R) 10 (R) 11 ), R8-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(CH3)2, NH2, CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl, cyclobutanol, substituted or unsubstituted 3-8 membered heterocycles (which may be saturated, unsaturated, aromatic, monocyclic, fused or helical), pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole, halophenyl, (benzyloxy)phenyl, CN and NO2; each of which is a separate embodiment according to the invention. In some embodiments, the heterocycle of formula I(e) is not substituted with CO2-R.

[0703] In some embodiments, R6 in formulas I, II, I(a)-I(d), I(f)-I(i), I(l), I(n), and / or I(o) is H. In other embodiments, R6 is H, F, Cl, Br, I, OH, SH, R8-OH, R8-SH, -R8-OR. 10 , CH2-O-CH3, (CH2)2-O-CH3, (CH2)3-O-CH3, (CH2)2-O-CH(CH3)2, R8-SR 10 , (CH2)3-S-(CH2)2CH3, R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl), CH2-cyclopropyl, CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol, R8- (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro 3-10 membered heterocycles), (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazole, CH2-tetrahydro Furan, CH2-dioxane, CH2-oxacyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, CH2-azaspiroheptane, CF3, CD3, OCD 3、 CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R 10 ), N(R 10 (R) 11), R8-N(R 10 (R) 11 ), (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)3-4-fluoro-piperidine, (CH2)3-piperidin-2-one, (CH2)3-4-cyano-piperidine, (CH2)3-4-trifluoromethyl-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, (CH2)3-N(CH2CH3)(CH2CF3), R8-C(O)N(R 10 (R) 11 ), (CH2)2-C(O)-piperidine, R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight or branched alkyl groups, substituted or unsubstituted alkyl groups, CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH(CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3) Benzyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, isopentyl, neopentyl, hexyl, CH2-OCH2-CH2-O-CH3, CH(CH3)C(O)N(CH3)2, C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight-chain or branched or C3-C8 cyclic alkoxymethoxy, optionally wherein at least one methylene (CH2) of said alkoxy group is replaced by an oxygen atom, O-(CH2)2-O-CH3, C1-C5 straight-chain or branched thioalkoxy, C1-C5 straight-chain or branched haloalkoxy, C 1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl, cyclopropyl, cyclobutyl, cyclohexyl, 4,4-difluorocyclohexane, methoxycyclopropyl, methylcyclobutyl, cyclopropyl, aminomethyl-cyclobutyl, methoxycyclobutyl, 2,3-dihydro-1H-indole, R8- (substituted or unsubstituted C3-C8 cycloalkyl), substituted or unsubstituted, saturated or unsaturated, single, fused, bridged or spirocyclic 3-10-membered carbon rings or heterocycles, piperidine (2-piperidine, 3-piperidine or 4-piperidine), 1-methylpiperidine (e.g., 1-methyl-3-piperidine, 1-methyl-4-piperidine), 3-fluoro-1-methylpiperidine, 1-(2,2,2-trifluoroethyl) Piperidine, azacyclobutane, 1-methyl-azacyclobutane (e.g., 1-methyl-3-azacyclobutane), morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran (e.g., 4-tetrahydropyran or 3-tetrahydropyran), tetrahydrofuran, azaspiro[3.3]heptane, 8-methyl-8-azabicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxecyclobutane, hydroxy-tetrahydrofuran, azacycloheptane-2-one, azabicyclohexane, 4,4-difluorocyclohexane, substituted or unsubstituted aryl, substituted or unsubstituted R8-aryl (e.g., benzyl) or substituted or unsubstituted benzyl; each represents a separate embodiment according to the invention.In some embodiments, R6 may be further substituted by at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched 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 The following are listed: N(CH3)2, NH2, CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl, cyclobutanol, substituted or unsubstituted 3-8 membered heterocyclic pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole, C1-C5 straight-chain or branched haloalkyl (e.g., CH2CF3, CHF2), halophenyl, (benzyloxy)phenyl, CN, and NO2; each representing a separate embodiment according to the invention. In some embodiments, R6 is H. In some embodiments, R6 is -R8-OR 10 In some embodiments, R6 is CH2-O-CH3. In some embodiments, R6 is R8-SR. 10 In some embodiments, R6 is (CH2)3-S-(CH2)2CH3. In some embodiments, R6 is R8-NHC(O)-R 10 In some embodiments, R6 is (CH2)3-NHC(O)-R 10 In some embodiments, R6 is (CH2)-NHC(O)-R 10In some embodiments, R6 is R8- (substituted or unsubstituted C3-C8 cycloalkyl). Examples of R8- (substituted or unsubstituted C3-C8 cycloalkyl) include, but are not limited to: CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, and CH2-cyclohexanol; each representing a separate embodiment according to the invention. In some embodiments, R6 is R8- (substituted or unsubstituted, saturated, unsaturated, or aromatic, monocyclic, fused, or spiro-3-8 membered heterocycle). In some embodiments, R6 is R8- (substituted or unsubstituted saturated monocyclic 3-8 membered heterocycle). In some embodiments, R6 is R8- (substituted or unsubstituted unsaturated monocyclic 3-8 membered heterocycle). In some embodiments, R6 is (CH2)3-4-fluoropiperidine. In some embodiments, R6 is R8- (substituted or unsubstituted aromatic monocyclic 3-8 membered heterocycle). In some embodiments, R6 is R8- (a substituted or unsubstituted saturated fused 3-8 membered heterocycle). In some embodiments, R6 is R8- (a substituted or unsubstituted unsaturated fused 3-8 membered heterocycle). In some embodiments, R6 is R8- (a substituted or unsubstituted aromatic fused 3-8 membered heterocycle). In some embodiments, R6 is R8- (a substituted or unsubstituted spiro 3-8 membered heterocycle). Examples of R8 (substituted or unsubstituted, saturated, unsaturated or aromatic, single, fused or spiro3-8 membered heterocycles) include, but are not limited to: (CH2)3-4-fluoropiperidine, (CH2)3-pyran, (CH2)2-pyrazole, (CH2)2-imidazolium, CH2-tetrahydrofuran, CH2-dioxane, CH2-oxacyclobutane, CH2-piperidine, CH2-triazole, CH2-1-oxa-8-azaspiro[4.5]decane, (CH2)3-diazabicyclo[2.2.1]heptane, CH2-methyl-THF, CH2-ethyl-piperidine, CH2-oxa-azaspirodecane, (CH2)3-dimethylpyrazole, CH2-2-oxo-methylpyrrolidine, CH2-methyl-azacyclobutane, and CH2-azaspiroheptane. In some embodiments, R6 is NH2. In some embodiments, R6 is NHR. In some embodiments, R6 is N(R)2. In some embodiments, R6 is NH(R)2. 10 In some embodiments, R6 is N(R 10 (R) 11 In some embodiments, R6 is R8-N(R 10 (R) 11 In some embodiments, R8-N(R) 10 (R) 11Including but not limited to: (CH2)3-N(CH2CH3)2, (CH2)3-N(CH(CH3)2)2, (CH2)3-piperidine, (CH2)4-NH(CH3), (CH2)3-NH-CH3, (CH2)3-NH-CH2CH3, (CH2)3-N(CH2CH3)2, (CH2)3-NH2, and (CH2)3-N(CH2CH3)(CH2CF3). In some embodiments, R6 is R8-C(O)N(R 10 (R) 11 ), such as (CH2)2-C(O)-piperidine. In some embodiments, R6 is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group. Examples of C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups include, but are not limited to: CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH(CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), CH(CH3)C(O)N(CH3)2, benzyl, methyl, ethyl, and CH2-OCH2-CH2-O-CH3. In some embodiments, R6 is a substituted or unsubstituted C3-C8 cycloalkyl group. In some embodiments, the substituted or unsubstituted C3-C8 cycloalkyl group includes: cyclopropyl, cyclobutyl, cyclohexyl, methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, methoxycyclobutyl, and 2,3-dihydro-1H-indendrone. In some embodiments, R6 is R8- (substituted or unsubstituted C3-C8 cycloalkyl). In some embodiments, R6 is a substituted or unsubstituted, saturated or unsaturated, monocyclic, fused, bridged, or spirocyclic 3-10 membered carbon ring or heterocyclic ring. In some embodiments, the ring may be further substituted by at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched alkyl, OH, alkoxy, OMe, amide, C(O)N(R)2, C(O)-alkyl, C(O)-pyrrolidine, C(O)-piperidine, N(R)2, NH ... 10 ), N(R 10 (R) 11The following are listed: N(CH3)2, NH2, CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl, cyclobutanol, substituted or unsubstituted 3-8 membered heterocyclic pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole, C1-C5 straight-chain or branched haloalkyl (e.g., CH2CF3, CHF2), halophenyl, (benzyloxy)phenyl, CN, and NO2; each representing a separate embodiment according to the invention. In some embodiments, R6 is a substituted or unsubstituted, saturated or unsaturated, monolithic, fused, bridged, or spiro3-10 membered heterocycle. In some embodiments, R6 is a substituted or unsubstituted, saturated, unsaturated, or aromatic, monolithic, fused, or spiro3-10 membered heterocycle. In some embodiments, R6 is a substituted or unsubstituted, saturated, unsaturated, or aromatic, monolithic 3-10 membered heterocycle. In some embodiments, R6 is a substituted or unsubstituted, saturated, single 3- to 10-membered heterocycle. In some embodiments, the ring is piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, 1-(2,2,2-trifluoroethyl)piperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azispiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane, each representing a separate embodiment according to the invention. In some embodiments, R6 is a substituted or unsubstituted, saturated or unsaturated, single, fused, bridged, or spiro3- to 10-membered carbon ring. In some embodiments, R6 is 4,4-difluorocyclohexane. In some embodiments, R6 is a substituted or unsubstituted R8-aryl group, such as benzyl. In some embodiments, R6 may be further substituted by at least one of the following: F, Cl, Br, I, CF3, R 20 C1-C5 straight-chain or branched alkyl groups, C1-C5 straight-chain or branched haloalkyl groups, OH, alkoxy groups, R8-OH (e.g., CH2-OH), OMe, amides, C(O)N(R)2, C(O)N(R) 10 (R) 11 ), R8-C(O)N(R 10 (R) 11 ), C(O)-pyrrolidine, C(O)-piperidine, N(R)2, NH(R) 10 ), N(R 10 (R) 11N(CH3)2, NH2, CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl, cyclobutanol, substituted or unsubstituted 3-8 membered heterocycles (which may be saturated, unsaturated, aromatic, single, fused or helical), pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole, C1-C5 straight or branched haloalkyl (e.g., CH2CF3, CHF2), halophenyl, (benzyloxy)phenyl, CN and NO2; each of which is a separate embodiment according to the invention.

[0704] In some embodiments, R6 of formula I(n) and / or I(o) is H. In some embodiments, R6 is CD3. In some embodiments, R6 is a C1-C5 straight-chain or branched alkyl group. In some embodiments, R6 is methyl. In some embodiments, R6 is ethyl. In some embodiments, R6 is isopropyl. In some embodiments, R6 is a substituted or unsubstituted, saturated or unsaturated, monocyclic, fused, bridged, or spirocyclic 3-10-membered heterocycle. In some embodiments, R6 is an unsubstituted monocyclic 3-8-membered heterocycle. In some embodiments, R6 is piperidine. In some embodiments, R6 is 4-piperidine. In some embodiments, R6 is azahexacyclic butane. In some embodiments, R6 is morpholine. In some embodiments, R6 is tetrahydropyran. In some embodiments, R6 is tetrahydrofuran. In some embodiments, R6 is dioxane. In some embodiments, R6 is 1,3-dioxane. In some embodiments, R6 is pyrrolidine. In some embodiments, R6 is a substituted monocyclic 3-8-membered heterocycle. In some embodiments, R6 is 1-methylpiperidine. In some embodiments, R6 is 3-fluoro-1-methylpiperidine. In some embodiments, R6 is 1-methyl-azacyclobutane. In some embodiments, R6 is trifluoromethyl-oxacyclobutane. In some embodiments, R6 is hydroxy-tetrahydrofuran. In some embodiments, R6 is 1-(2,2,2-trifluoroethyl)piperidine. In some embodiments, R6 is a substituted or unsubstituted, unsaturated single 3- to 8-membered heterocycle. In some embodiments, R6 is pyrrolidone. In some embodiments, R6 is imidazole. In some embodiments, R6 is azacycloheptane-2-one. In some embodiments, R6 is a substituted or unsubstituted, saturated bridging 3- to 10-membered heterocycle. In some embodiments, R6 is a quinine ring. In some embodiments, R6 is 8-methyl-8-azabicyclo[3.2.1]octane. In some embodiments, R6 is azabicyclohexane. In some embodiments, R6 is a substituted or unsubstituted, saturated spiro3- to 10-membered heterocycle. In some embodiments, R6 is azaspiro[3.3]heptane. In some embodiments, R6 is a substituted or unsubstituted C3-C8 cycloalkyl group. In some embodiments, R6 is a cyclopropyl group. In some embodiments, R6 is 4,4-difluorocyclohexane.

[0705] In some embodiments, R6 and R5 of formulas I, II, I(a)-I(i), I(l), I(n) and / or I(o) are linked 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 azaheptanane, piperazine, or 2-(piperazin-1-yl)acetamide; each representing a separate embodiment according to the invention. In some embodiments, the ring may be further substituted by at least one of the following: F, Cl, Br, I, C1-C5 straight or branched alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R)2), C(O)-pyrrolidine, C(O)-piperidine, N(R)2NH(R) 10 ), N(R 10 (R) 11 (e.g., N(CH3)2, NH2), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3-8 membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), C1-C5 straight-chain or branched haloalkyl (e.g., CH2CF3, CHF2), halophenyl, (benzyloxy)phenyl, CN, and NO2; each of which represents a separate embodiment according to the invention.

[0706] In some embodiments, R6 of equations I, II and / or I(a)-I(i) is represented by the structure of equation B:

[0707]

[0708] in

[0709] m is 0 or 1; and

[0710] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0711] R 12 and R 13 Both are H; or

[0712] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl); or

[0713] R 12 Connect with C3 to form a ring A, and R 13It is R 30 ;or

[0714] R 12 and R 13 Connect to form ring B; or

[0715] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0716] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0717] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0718] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0719] in

[0720] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle;

[0721] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle; and

[0722] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group;

[0723] In some embodiments, formula B is represented by formula Bi.

[0724] In some embodiments, R6 of formulas I, II and / or I(a)-I(i) is represented by the structure of formula Bi:

[0725]

[0726] in

[0727] m is 0 or 1; and

[0728] R 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 ;or

[0729] R 12 and R 13 Both are H; or

[0730] R 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl); or

[0731] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0732] R 12 and R 13 Connect to form ring B; or

[0733] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0734] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0735] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0736] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D;

[0737] in

[0738] Rings A, C, and E are each independently a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle;

[0739] Ring B is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle; and

[0740] Cycle D is a substituted or unsubstituted C3-C8 cycloalkyl group;

[0741] In some embodiments, R of formula B and / or Bi 12 It is H. In some embodiments, R 12 It is R 20 In other embodiments, R 12 It is R 30 In some embodiments, R 12 It is a C1-C5 C(O)-alkyl group. In some embodiments, R 12 It is a substituted or unsubstituted C1-C5 alkyl group. In some embodiments, R 12It is an unsubstituted C1-C5 alkyl group. In some embodiments, the alkyl group is an ethyl group. In some embodiments, R 12 It is a substituted C1-C5 alkyl group. In some embodiments, the alkyl group is trifluoroethyl.

[0742] In some embodiments, R of formula B and / or Bi 13 It is H. In other embodiments, R 13 It is R 30 In some embodiments, R 13 It is a substituted or unsubstituted C1-C5 alkyl group. In some embodiments, R 13 It is an unsubstituted C1-C5 alkyl group. In some embodiments, the alkyl group is an ethyl group. In some embodiments, R 13 It is a substituted C1-C5 alkyl group. In some embodiments, the alkyl group is trifluoroethyl.

[0743] In some embodiments, R6 of formulas I, II, and / or I(a)-I(i) is represented by formula B. In some embodiments, R6 of formula B 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 In some embodiments, R of formula B 12 and R 13 Both are H. In some embodiments, R of formula B 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl). In some embodiments, R of formula B 12 and R 13 Each is independently H or trifluoroethyl. In some embodiments, R of formula B 12 Connect with C3 to form a ring A, and R 13 It is R 30 In some embodiments, R of formula B 12 and R 13 Connect to form ring B. In some embodiments, R of formula B 12 Connect C1 to form a loop C, and R 13 It is R 30 In some embodiments, C1 and C3 of formula B are connected to form ring D, and R of formula B... 12 and R 13 Each is R independently 30 In some embodiments, R of formula B 13 Connect C2 to form ring E, m is 1, and R of equation B 12 It is R 30 In some embodiments, R of formula B 12and R 13 Connect to form ring B, and connect C1 and C3 of form B to form ring D.

[0744] In some embodiments, R6 of formulas I, II, and / or I(a)-I(h) is represented by formula Bi. In some embodiments, R of formula Bi 12 It is R 20 Or C1-C5 C(O)-alkyl, and R 13 It is R 30 In some embodiments, R of formula Bi 12 and R 13 Both are H. In some embodiments, R of formula Bi 12 and R 13 Each is independently H or a substituted or unsubstituted C1-C5 alkyl group (e.g., ethyl, trifluoroethyl). In some embodiments, R of formula Bi 12 and R 13 Each is independently H or trifluoroethyl. In some embodiments, R of formula Bi 12 Connect with C3 to form a ring A, and R 13 It is R 30 In some embodiments, R of formula Bi 12 and R 13 Connect to form ring B. In some embodiments, R of formula Bi 12 Connect C1 to form a loop C, and R 13 It is R 30 In some embodiments, C1 and C3 of formula Bi are connected to form ring D, and R of formula Bi... 12 and R 13 Each is R independently 30 In some embodiments, R of formula Bi 13 Connecting with C2 to form a ring E, m is 1, and the R of equation Bi 12 It is R 30 In some embodiments, R of formula Bi 12 and R 13 Connect to form ring B, and connect C1 and C3 of formula Bi to form ring D.

[0745] In some embodiments, R6 of formula I(g) is represented by the structure of formula C:

[0746]

[0747] in

[0748] K is an integer between 1 and 4;

[0749] R 12 and R 13Each is independently H, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl (e.g., ethyl, isopropyl), R 20 or

[0750] R 12 and R 13 Linked to form substituted or unsubstituted 4-7 membered heterocycles (e.g., piperidine, piperazine, pyrrolidine, oxa-6-azaspiro[3.3]heptane).

[0751] In some embodiments, k in equation C is 1. In some embodiments, k is 2. In some embodiments, k is 3. In some embodiments, k is 4.

[0752] In some embodiments, R of formula C 12 and R 13 Each is independently an H, C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group (e.g., ethyl, isopropyl) or R. 20 Each of these represents a separate embodiment of the invention. In some embodiments, R of formula C 12 and R 13 All are ethyl. In some embodiments, R of formula C 12 and R 13 Both are isopropyl. In some embodiments, R of formula C 12 and R 13 They are all alkyl groups.

[0753] In some embodiments, R of formula C 12 and R 13 Linkages are used to form substituted or unsubstituted 4-7 membered heterocycles. In some embodiments, R of formula C 12 and R 13 Linked to form piperidine, piperazine, pyrrolidine, oxa-6-azaspiro[3.3]heptane; each representing a separate embodiment according to the invention. In some embodiments, the heterocycle may be further substituted with at least one heterocycle as defined herein.

[0754] In some embodiments, R6 of formula I(b) is represented by formula Bi and / or B, and

[0755] R of formula Bi and / or B 12 It is R 20 Or C1-C5 C(O)-alkyl, and R of formula Bi and / or B 13 It is R 30 ;or

[0756] R 12 and R 13 All are H, or

[0757] R12 and R 13 Each independently is H or trifluoroethyl; or

[0758] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0759] R 12 and R 13 Linked to form substituted or unsubstituted pyrrolidine rings, 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

[0760] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0761] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0762] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0763] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D.

[0764] In some embodiments, R6 of formula I(b) is represented by formula Bi and / or B, and

[0765] R of formula Bi and / or B 12 It is R 20 Or C1-C5 C(O)-alkyl, and R of formula Bi and / or B 13 It is R 30 ;or

[0766] R 12 Connect with C3 to form a ring A, and R 13 It is R 30 ;or

[0767] R 12 and R 13Linked to form substituted or unsubstituted pyrrolidine rings, 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

[0768] R 12 Connect C1 to form a loop C, and R 13 It is R 30 ;or

[0769] C1 and C3 are connected to form a ring D, and R 12 and R 13 Each is R independently 30 ;or

[0770] R 13 Connect C2 to form a ring E, m is 1, and R 12 It is R 30 ;or

[0771] R 12 and R 13 Connect to form loop B, and connect C1 and C3 to form loop D.

[0772] In some embodiments, ring A of formula Bi is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle. In some embodiments, ring A is an unsubstituted single 3-8 membered heterocycle. In some embodiments, ring A is an unsubstituted spiro 3-8 membered heterocycle. In some embodiments, ring A is an unsubstituted fused 3-8 membered heterocycle. In some embodiments, ring A is a substituted single 3-8 membered heterocycle. In some embodiments, ring A is a substituted spiro 3-8 membered heterocycle. In some embodiments, ring A is a substituted fused 3-8 membered heterocycle. In some embodiments, ring A is: pyrrolidine, methylpyrrolidine, ethylpyrrolidine, 2-oxopyrrolidine, piperidine, methylpiperidine, methyl-2-oxopyrrolidine, pyran-azacyclobutane, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, or 2-azaspiro[3.3]heptane; each representing a separate embodiment according to the invention. In some embodiments, ring A is: pyrrolidine, methylpyrrolidine, or ethylpyrrolidine; each of which represents a separate embodiment according to the invention.

[0773] In some embodiments, ring B of formula Bi is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle. In some embodiments, ring B is an unsubstituted single 3-8 membered heterocycle. In some embodiments, ring B is an unsubstituted spiro 3-8 membered heterocycle. In some embodiments, ring B is an unsubstituted fused 3-8 membered heterocycle. In some embodiments, ring B is a substituted single 3-8 membered heterocycle. In some embodiments, ring B is a substituted spiro 3-8 membered heterocycle. In some embodiments, ring B is a substituted fused 3-8 membered heterocycle. In some embodiments, ring B is: pyrrolidine, methylpyrrolidine, ethylpyrrolidine, 2-oxopyrrolidine, hydroxymethylpyrrolidine, piperidine, piperin-2-one, 4-fluoropiperidine-2-one, piperin-4-carboxynitrile, methylpiperidine, fluoropiperidine, 4-fluoropiperidine, 4-fluoro-2-methylpiperidine, difluoropiperidine, piperazine, methylpiperazine, dimethylpyrazole, methyl-2-oxopyrrolidine, pyran, azacyclobutane. Alkane, methyl-azacyclobutane, 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-dioxa-2-oxa-6-azaspiro[3.3]heptane; each representing a separate embodiment according to the invention. In some embodiments, ring B 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-dioxide-2-oxa-6-azaspiro[3.3]heptane, hydroxymethyl-pyrrolidine, or dizabicyclo[2.2.1]heptane, 6-fluoro-3-azabicyclo[3.1.1]heptane, each representing a separate embodiment according to the invention.

[0774] In some embodiments, the ring C of formula Bi is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle. In some embodiments, the ring C is an unsubstituted single 3-8 membered heterocycle. In some embodiments, the ring C is an unsubstituted spiro 3-8 membered heterocycle. In some embodiments, the ring C is an unsubstituted fused 3-8 membered heterocycle. In some embodiments, the ring C is a substituted single 3-8 membered heterocycle. In some embodiments, the ring C is a substituted spiro 3-8 membered heterocycle. In some embodiments, the ring C is a substituted fused 3-8 membered heterocycle. In some embodiments, the ring C is: pyrrolidine, methylpyrrolidine, ethylpyrrolidine, 2-oxopyrrolidine, piperidine, methylpiperidine, methyl-2-oxopyrrolidine, pyran-azacyclobutane, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, or 2-azaspiro[3.3]heptane; each representing a separate embodiment according to the invention. In some embodiments, ring C is: piperidine, pyrrolidine, methyl-2-oxopyrrolidine, pyran-pyrrolidine, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane or 2-azaspiro[3.3]heptane; each representing a separate embodiment according to the invention.

[0775] In some embodiments, ring D of formula Bi is a substituted or unsubstituted C3-C8 cycloalkyl group. In some embodiments, ring D is a substituted C3-C8 cycloalkyl group. In some embodiments, ring D is an unsubstituted C3-C8 cycloalkyl group. In some embodiments, ring D is cyclopropane, cyclobutane, cyclopentane, cyclohexane, or cycloheptane; each of which represents a separate embodiment according to the invention.

[0776] In some embodiments, ring E of formula Bi is a substituted or unsubstituted single, spiro, or fused 3-8 membered heterocycle. In some embodiments, ring E is an unsubstituted single 3-8 membered heterocycle. In some embodiments, ring E is an unsubstituted spiro 3-8 membered heterocycle. In some embodiments, ring E is an unsubstituted fused 3-8 membered heterocycle. In some embodiments, ring E is a substituted single 3-8 membered heterocycle. In some embodiments, ring E is a substituted spiro 3-8 membered heterocycle. In some embodiments, ring E is a substituted fused 3-8 membered heterocycle. In some embodiments, ring E is: pyrrolidine, methylpyrrolidine, ethylpyrrolidine, 2-oxopyrrolidine, piperidine, methylpiperidine, methyl-2-oxopyrrolidine, pyran-azacyclobutane, methyl-azacyclobutane, azabicyclooctane, 2-azabicyclo[2.1.1]hexane, or 2-azaspiro[3.3]heptane; each representing a separate embodiment according to the invention. In some embodiments, ring E is: pyrrolidine, azacyclobutane, ethylpyrrolidine, oxopyrrolidine, or methylpiperidine; each of which represents a separate embodiment according to the invention.

[0777] In some embodiments, R6 in formula I(b) is F, Cl, Br, I, OH, SH, R8-OH, R8-SH, or -R8-OR. 10 CH2-O-CH3, R8-SR 10 , (CH2)3-S-(CH2)2CH3, R8-NHC(O)-R 10 -O-R8-R 10 R8- (substituted or unsubstituted C3-C8 cycloalkyl), CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol, (CH2)3-pyran, CH2-tetrahydrofuran, CH2-dioxane, CH2-methyl-THF, CH2-oxa-azaspirodecane, CH2-azaspiroheptane, (CH2)3-dimethylpyrazole, CH2-methyl-azacyclobutane, CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups, CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH(CH3)2), CH2CH(CH3) (OCH3), CH2CH(N(CH3)2)(CH2CH3), benzyl, methyl, ethyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, isopentyl, neopentyl, hexyl, CH2-OCH2-CH2-O-CH3, C1-C5 straight or branched, substituted or unsubstituted alkenyl, C1-C5 straight or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight or branched or C3-C8 cyclic alkoxy, methoxy, O-(CH2)2-O-CH3), substituted or unsubstituted C1-C5 straight or branched or C3-C8 Cyclic alkoxy groups, wherein at least one methylene (CH2) group of the alkoxy group is replaced by an oxygen atom; C1-C5 straight-chain or branched thioalkoxy groups; C1-C5 straight-chain or branched haloalkoxy groups; C1-C5 straight-chain or branched alkoxyalkyl groups; substituted or unsubstituted C3-C8 cycloalkyl groups; methoxycyclopropyl groups; methylcyclobutyl groups; cyclopropyl groups; cyclobutyl groups; cyclohexyl groups; 4,4-difluorocyclohexane; aminomethyl-cyclobutyl groups; methoxycyclobutyl groups; 2,3-dihydro-1H-indole; substituted or unsubstituted; saturated or unsaturated; single; fused; bridged or spirocyclic; 3-10 membered carbon rings or heterocycles; piperidine; 1-methyl Piperidine, 3-fluoro-1-methylpiperidine, 1-(2,2,2-trifluoroethyl)piperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azirspiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane, 4,4-difluorocyclohexane, substituted or unsubstituted aryl or substituted or unsubstituted benzyl; each represents a separate embodiment according to the invention. In some embodiments, R6 may be further substituted with at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched 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 (e.g., N(CH3)2, NH2), NH(R)2, NH3, NH4 ... 10), N(R 10 (R) 11 ), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3-8 membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), C1-C5 straight-chain or branched haloalkyl (e.g., CH2CF3, CHF2), halophenyl, (benzyloxy)phenyl, CN and NO2; each of which represents a separate embodiment according to the invention.

[0778] In some embodiments, R6 of equation I(b) and / or I(l) is -R8-OR 10 In some embodiments, -R8-OR 10 It is CH2-O-CH3. In some embodiments, R6 is R8-SR. 10 In some embodiments, R8-SR 10 It is (CH2)3-S-(CH2)2CH3. In some embodiments, R6 is R8-NHC(O)-R 10In some embodiments, R6 is R8- (substituted or unsubstituted C3-C8 cycloalkyl). In some embodiments, R8- (substituted or unsubstituted C3-C8 cycloalkyl) is CH2-cyclobutanol, CH2-difluorocyclopropyl, CH2-methylcyclopropyl, CH2-dimethylamino-cyclohexyl, (CH2)2-cyclopentanol, CH2-cyclohexanol, (CH2)3-pyran, CH2-tetrahydrofuran, CH2-dioxane, CH2-methyl-THF, CH2-oxazaspirodecane, (CH2)3-dimethylpyrazole, CH2-methylazacyclobutane, or CH2-azaspiroheptane; each representing a separate embodiment according to the invention. In some embodiments, R6 is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl. In some embodiments, R6 is a C1-C5 straight-chain or branched substituted alkyl. In some embodiments, the substituted alkyl group is CH(CH3)CH2OCH3, CH(CH3)CH2NH2, CH(CH3)C(O)N(CH3)2, CH2-CH(OH)Ph, (CH2)3N(H)CH2CH3, CH(CH3)(CH2)2OH, CH(CH2OH)(CH2CH3), (CH2)3-OCH3, (CH2)2-OCH3, (CH2)2-OCH(CH3)2, CH(CH2OH)(CH2CH(CH3)2), CH2CH(CH3)(OCH3), CH2CH(N(CH3)2)(CH2CH3), CH2-OCH2-CH2-O-CH3, or benzyl; each representing a separate embodiment according to the invention. In some embodiments, R6 is a C1-C5 straight-chain or branched unsubstituted alkyl group. In some embodiments, the unsubstituted alkyl group is methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, or neopentyl; each representing a separate embodiment according to the invention. In some embodiments, R6 is a substituted or unsubstituted C3-C8 cycloalkyl group. In some embodiments, R6 is a substituted C3-C8 cycloalkyl group. In some embodiments, the substituted cycloalkyl group is methoxycyclopropyl, methylcyclobutyl, aminomethyl-cyclobutyl, or methoxycyclobutyl, 2,3-dihydro-1H-indanol; each representing a separate embodiment according to the invention. In some embodiments, R6 is an unsubstituted C3-C8 cycloalkyl group. In some embodiments, the unsubstituted cycloalkyl group is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; each representing a separate embodiment according to the invention. In some embodiments, R6 is a substituted or unsubstituted, saturated or unsaturated, single, fused, bridged, or spiro 3-10 membered carbon ring or heterocyclic ring.In some embodiments, the R6 carbocyclic or heterocyclic ring as defined in R6 is further substituted by at least one of the following: F, Cl, Br, I, C1-C5 straight or branched alkyl, OH, alkoxy (e.g., 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 The following are possible combinations of compounds: N(CH3)2, NH2, CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3-8 membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, triazole, imidazole), C1-C5 straight-chain or branched haloalkyl (e.g., CH2CF3, CHF2), halophenyl, (benzyloxy)phenyl, CN, and NO2. In some embodiments, R6 is a substituted or unsubstituted 3-10 membered heterocycle. In some embodiments, the substituted heterocycle is piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, 1-(2,2,2-trifluoroethyl)piperidine, aziridine, 1-methyl-aziridine, morpholine, pyrrolidine, pyrrolidone, quinine ring, tetrahydropyran, tetrahydrofuran, azispiro[3.3]heptane, 8-methyl-8-azibicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, aziridine-2-one, azibicyclohexane, each representing a separate embodiment according to the invention. In some embodiments, R6 is piperidine. In some embodiments, R6 is 1-methylpiperidine. In some embodiments, R6 is 3-fluoro-1-methylpiperidine. In some embodiments, R6 is 1-(2,2,2-trifluoroethyl)piperidine. In some embodiments, R6 is aziridine. In some embodiments, R6 is 1-methyl-azacyclobutane. In some embodiments, R6 is morpholine. In some embodiments, R6 is pyrrolidine. In some embodiments, R6 is pyrrolidone. In some embodiments, R6 is tetrahydropyran. In some embodiments, R6 is tetrahydrofuran. In some embodiments, R6 is 8-methyl-8-azabicyclo[3.2.1]octane. In some embodiments, R6 is dioxane. In some embodiments, R6 is 1,3-dioxane. In some embodiments, R6 is a substituted or unsubstituted, saturated or unsaturated, single, fused, bridged, or spirocyclic 3-10 membered carbon ring. In some embodiments, R6 is 4,4-difluorocyclohexane.

[0779] In some embodiments, R7 of formulas I, II, I(a)-I(f) and / or I(i) is H, F, Cl, Br, I, OH, OR 20 , SH, R8-OH, R8-SH, SR10 -R8-OR 10 -R8-SR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 COO-CH3, R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10), C1-C5 straight-chain or branched, substituted or unsubstituted alkyl, methylimidazolium, methyl, ethyl, C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl, C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy, optionally wherein at least one methylene (CH2) in said alkoxy is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkyl, C1-C5 straight-chain or branched thioalkoxy, C1-C5 straight-chain or Branched haloalkoxy, C1-C5 straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl, cyclopropyl-1-ol, cyclopropylamine, oxetane-3-ol, bicyclo[1.1.1]pentane, substituted or unsubstituted 4-7 membered heterocycles, morpholine, 3,3-dimethylmorpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, pyrrolidine-3-carboxynitrile, 3-cyanopyrrole Alkane, 1-methylpyrrolidine, 2,2-dimethylpyrrolidine, 3,3-difluoropyrrolidine, difluoromethylpyrrolidine, pyrrolidine-3-one-O-methyloxime, pyrrolidine-2-one, pyrrolidine-3-one, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperazine-2-one, 1-methylpiperazine, piperidine, piperidine-3-ol, piperidine-4-ol, piperidine-2-one, piperidine-4-carboxynitrile, 4-fluoropiperidine, oxadiazole, triazole, 2-oxopyrrolidine, isoxazolidine, piperazine-2-one, substituted or unsubstituted The 3-10 bridging, fused or spiroheterocyclic, 4-azaspiro[2.4]heptane, 2-oxa-5-azaspiro[3.4]octane, 1,4-dioxa-6-azaspiro[4.4]nonane, 4,7-diazaspiro[2.5]octane, 2,5-diazabicyclo[2.2.1]heptane, R8- (substituted or unsubstituted mono, fused or spiro3-8 fused heterocyclic), substituted or unsubstituted aryl or substituted or unsubstituted benzyl; each represents a separate embodiment according to the invention. In some embodiments, R7 is further substituted with at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched 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)2NH(R) 10 ), N(R 10 (R) 11(e.g., N(CH3)2, NH2), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (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 NO2; each of which represents a separate embodiment according to the invention.

[0780] In some embodiments, R7 in formulas I, II, I(b), I(d)-I(f) and / or I(i) is H. In some embodiments, R7 is F. In some embodiments, R7 is Cl. In some embodiments, R7 is Br. In some embodiments, R7 is I. In some embodiments, R7 is OH. In some embodiments, R7 is OR 20 In some embodiments, R7 is CF3. In some embodiments, R7 is CN. In some embodiments, R7 is NH2. In some embodiments, R7 is NHR. In some embodiments, R7 is N(R)2. In some embodiments, R7 is NH(R)2. 10 In some embodiments, R7 is N(R). 10 (R) 11 In some embodiments, R7 is NHC(O)-R. 10 In some embodiments, R7 is COOH. In some embodiments, R7 is -C(O)Ph. In some embodiments, R7 is C(O)OR. 10 In some embodiments, R7 is COO-CH3. In some embodiments, R7 is C(O)H. In some embodiments, R7 is C(O)-R 10 In some embodiments, R7 is a C1-C5 straight-chain or branched C(O)-haloalkyl group. In some embodiments, R7 is -C(O)NH2. In some embodiments, R7 is C(O)NHR. In some embodiments, C(O)NHR is C(O)NH(CH3). In some embodiments, R7 is C(O)N(R 10 (R) 11 In some embodiments, C(O)N(R) 10 (R) 11R7 is C(O)NH(CH3), C(O)NH(CH2CH2OCH3), or C(O)NH(CH2CH2OH); each representing a separate embodiment according to the invention. In some embodiments, R7 is SO2R. In some embodiments, R7 is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group. In some embodiments, the alkyl group is methylimidazolium, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, neopentyl, or hexyl; each representing a separate embodiment according to the invention. In some embodiments, R7 is a C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl group. In some embodiments, R7 is a C1-C5 straight-chain haloalkyl group. In some embodiments, the haloalkyl group is CHF2. In some embodiments, R7 is a C1-C5 branched haloalkyl group. In some embodiments, R7 is a C3-C8 cyclic haloalkyl group. In some embodiments, R7 is a C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy group, optionally wherein at least one methylene (CH2) group in the alkoxy group is replaced by an oxygen atom. In some embodiments, R7 is a C1-C5 straight-chain alkoxy group. In some embodiments, the alkoxy group is a methoxy group. In some embodiments, the alkoxy group is an ethoxy group. In some embodiments, R7 is a C1-C5 branched alkoxy group. In some embodiments, R7 is a C3-C8 cyclic alkoxy group. In some embodiments, R7 is a C1-C5 straight-chain or branched thioalkyl group. In some embodiments, R7 is a C1-C5 straight-chain or branched haloalkoxy group. In some embodiments, R7 is a C1-C5 straight-chain haloalkoxy group. In some embodiments, R7 is a C1-C5 branched haloalkoxy group. In some embodiments, R7 is a C1-C5 straight-chain or branched alkoxyalkyl group. In some embodiments, R7 is a substituted or unsubstituted C3-C8 cyclic alkyl group. In some embodiments, the cycloalkyl group is cyclopropyl, cyclopropanol, cyclobutyl, cyclopentyl, bicyclo[1.1.1]pentane, cyclohexyl, cycloheptyl, or cyclooctyl; each representing a separate embodiment according to the invention. In some embodiments, R7 is a substituted or unsubstituted 3- to 10-membered monocyclic, fused, bridged, or spirocyclic, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring. In some embodiments, R7 is a substituted or unsubstituted 3- to 10-membered monocyclic, fused, bridged, or spirocyclic, saturated, unsaturated, or aromatic heterocyclic ring. In some embodiments, R7 is a substituted or unsubstituted 47-membered heterocyclic ring. In some embodiments, R7 is an unsubstituted 4- to 7-membered heterocyclic ring. In some embodiments, the heterocycle is morpholine, tetrahydrofuran, tetrahydropyran, oxadiazine, pyrrolidine, pyrrolidine-3-one, pyrrolidine-2-one, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperazine-2-one, piperidine, piperidine-2-one, oxadiazole, triazole, isoxazolidine, or 2-oxopyrrolidine; each of which represents a separate embodiment according to the invention.In some embodiments, R7 is a substituted 47-membered heterocycle. In some embodiments, the heterocycle is 3,3-dimethylmorpholine, oxetane-3-ol, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, pyrrolidine-3-carboxynitrile, 3-cyanopyrrolidine, 1-methylpyrrolidine, 2,2-dimethylpyrrolidine, 3,3-difluoropyrrolidine, difluoromethylpyrrolidine, pyrrolidine-3-one-O-methyloxime, pyrrolidine-3-one-methyloxime, 1-methylpiperazine, 1-methylpiperazine, piperidin-3-ol, piperidin-4-ol, piperidin-4-carboxynitrile, 4-fluoropiperidine; each representing a separate embodiment according to the invention. In some embodiments, R7 is a substituted or unsubstituted 3- to 10-membered bridging, fused, or spiroheterocycle. In some embodiments, the ring is 4-azaspiro[2.4]heptane, 2-oxa-5-azaspiro[3.4]octane, 1,4-dioxa-6-azaspiro[4.4]nonane, 4,7-diazaspiro[2.5]octane, or 2,5-diazabicyclo[2.2.1]heptane; each representing a separate embodiment according to the invention. In some embodiments, R7 is R8- (a substituted or unsubstituted single, fused, or spiro3-8 membered heterocycle). In some embodiments, R7 is R8- (an unsubstituted single 3-8 membered heterocycle). In some embodiments, R7 is R8- (an unsubstituted fused 3-8 membered heterocycle). In some embodiments, R7 is R8- (an unsubstituted spiro3-8 membered heterocycle). In some embodiments, R7 is R8- (a substituted single 3-8 membered heterocycle). In some embodiments, R7 is R8- (a substituted fused 3-8 membered heterocycle). In some embodiments, R7 is R8- (a substituted spiro 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, R7 is a substituted or unsubstituted aryl group. In some embodiments, R7 is a phenyl group. In some embodiments, R7 may be further substituted by at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R)2), C(O)-pyrrolidine, C(O)-piperidine, N(R)2NH(R). 10 ), N(R 10 (R) 11(e.g., N(CH3)2, NH2), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclobutanol), C1-C5 straight-chain or branched haloalkyl (e.g., CH2CF3, CHF2), substituted or unsubstituted 3-8 membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), halophenyl, (benzyloxy)phenyl, CN and NO2; each of which represents a separate embodiment according to the invention.

[0781] In some embodiments, R7 in equation I(a) is OR 20In some embodiments, R7 is a substituted or unsubstituted 4-7 membered heterocycle. In some embodiments, R7 is a substituted or unsubstituted 3-10 membered monocyclic, fused, bridged, or spirocyclic, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring. In some embodiments, R7 is a substituted or unsubstituted 3-10 membered monocyclic, fused, bridged, or spirocyclic, saturated, unsaturated, or aromatic heterocycle. In some embodiments, R7 is a substituted or unsubstituted 47-membered heterocycle. In some embodiments, R7 is an unsubstituted 4-7 membered heterocycle. In some embodiments, the heterocycle is morpholine, tetrahydrofuran, tetrahydropyran, oxadiazole, pyrrolidine-3-one, pyrrolidine-2-one, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-2-one, oxadiazole, triazole, isoxazolidine, or 2-oxopyrrolidine; each representing a separate embodiment according to the invention. In some embodiments, R7 is a substituted 47-membered heterocycle. In some embodiments, the heterocycle is 3,3-dimethylmorpholine, oxetane-3-ol, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, pyrrolidine-3-carboxynitrile, 3-cyanopyrrolidine, 1-methylpyrrolidine, 2,2-dimethylpyrrolidine, 3,3-difluoropyrrolidine, difluoromethylpyrrolidine, pyrrolidine-3-one-O-methyloxime, pyrrolidine-3-one-methyloxime, 1-methylpiperazine, 1-methylpiperazine, piperidin-3-ol, piperidin-4-ol, piperidin-4-carboxynitrile, 4-fluoropiperidine; each representing a separate embodiment according to the invention. In some embodiments, R7 is a substituted or unsubstituted 3- to 10-membered bridging, fused, or spiroheterocycle. In some embodiments, the ring is 4-azaspiro[2,4]heptane, 2-oxa-5-azaspiro[3,4]octane, or 1,4-dioxa-6-azaspiro[4,4]nonane; each representing a separate embodiment according to the invention. In some embodiments, R7 is morpholine. In some embodiments, R7 is tetrahydrofuran. In some embodiments, R7 is tetrahydropyran. In some embodiments, R7 is oxecyclobutane. In some embodiments, R7 is oxecyclobutane-3-ol. In some embodiments, R7 is pyrrolidine. In some embodiments, R7 is pyrrolidine-2-ol. In some embodiments, R7 is pyrrolidine-3-ol. In some embodiments, R7 is 3-methoxypyrrolidine. In some embodiments, R7 is pyrrolidine-3-carboxynitrile. In some embodiments, R7 is 1-methylpyrrolidine. In some embodiments, R7 is pyrrolidine-2-one. In some embodiments, R7 is pyrrolidine-3-one. In some embodiments, R7 is pyrrolidone. In some embodiments, R7 is imidazole. In some embodiments, R7 is pyrazole. In some embodiments, R7 is isoxazolidine. In some embodiments, R7 is piperazine. In some embodiments, R7 is piperidine. In some embodiments, R7 is piperidine-3-ol.In some embodiments, R7 is piperidin-4-ol. In some embodiments, R7 is piperidin-2-one. In some embodiments, R7 is piperazine-2-one. In some embodiments, R7 is piperidin-4-carboxynitrile. In some embodiments, R7 is 4-fluoropiperidine. In some embodiments, R7 is 2,2-dimethylpyrrolidine. In some embodiments, R7 is pyrrolidine-3-one O-methyl oxime. In some embodiments, R7 is a substituted or unsubstituted 3- to 10-membered bridged, fused, or spiroheterocyclic ring. In some embodiments, R7 is 4-azaspiro[2.4]heptane. In some embodiments, R7 is 2-oxa-5-azaspiro[3.4]octane. In some embodiments, R7 is 1,4-dioxa-6-azaspiro[4.4]nonane. In some embodiments, R7 is 4,7-diazaspiro[2.5]octane. In some embodiments, R7 is 2,5-diazabicyclo[2.2.1]heptane. In some embodiments, R7 is 3,3-dimethylmorpholine. In some embodiments, R7 is 1-methylpiperazine. In some embodiments, R7 is oxadiazole. In some embodiments, R7 is triazole. In some embodiments, R7 is a substituted or unsubstituted aryl group. In some embodiments, R7 is phenyl. In some embodiments, R7 may be further substituted by at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R)2), C(O)-pyrrolidine, C(O)-piperidine, N(R)2NH(R). 10 ), N(R 10 (R) 11 (e.g., N(CH3)2, NH2), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3-8 membered heterocycles (e.g., pyran, oxetane, piperidine, pyrazole, methyl-pyrazole, triazole, imidazole), C1-C5 straight-chain or branched haloalkyl (e.g., CH2CF3, CHF2), halophenyl, (benzyloxy)phenyl, CN, and NO2; each of which represents a separate embodiment according to the invention.

[0782] In some embodiments, R7 of formula I(c) is not H, F, Cl, C1-C5 straight or branched or C3-C8 cyclic alkoxy, C1-C5 straight or branched haloalkoxy or C1-C5 straight or branched, substituted or unsubstituted alkyl.

[0783] In some embodiments, R7 of equations I, II, I(a)-I(f) and / or I(i) is represented by the structure of equation A:

[0784]

[0785] in

[0786] X1 is N or O;

[0787] R1 and R2 are each independently H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g. CH2OH, CH2OCH3), C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy, 3-8 membered carbon ring or heterocycle (e.g. oxetane);

[0788] Or R1 and R2 can be connected to form a C3-C8 carbon ring or heterocycle (e.g., cyclopropyl);

[0789] R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl groups (e.g., methoxyethylene, methylaminoethyl, aminoethyl), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 (R) 11 (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl groups (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycles (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;

[0790] Or R3 and R4 can be linked to form 3-8 membered heterocycles (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole);

[0791] Or R2 and R4 are linked to form substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycles (e.g., pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidine-2-one, imidazole, pyrimidine, triazole, oxadiazole, pyrazole);

[0792] If X1 is 0, then R4 does not exist;

[0793] In some embodiments, X1 in formula A is N. In other embodiments, X1 is 0.

[0794] In some embodiments, R1 of formula A, I(h), I(m), and / or I(o) is H. In other embodiments, R1 is F. In other embodiments, R1 is CF3. In other embodiments, R1 is Cl. In other embodiments, R1 is Br. In other embodiments, R1 is I. In other embodiments, R1 is OH. In other embodiments, R1 is SH. In other embodiments, R1 is a substituted or unsubstituted C1-C5 alkyl group. In other embodiments, R1 is CH2OH. In other embodiments, R1 is CH2OCH3. In other embodiments, R1 is a C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl group. In other embodiments, R1 is a substituted or unsubstituted C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy group. In other embodiments, R1 is a 3-8 membered carbon ring or heterocycle. In other embodiments, R1 is a 3-8 membered heterocycle. In other embodiments, R1 is an oxobutane. In other embodiments, R1 is a 3-8 member carbon ring.

[0795] In some embodiments, R2 in formula A, I(h), I(m), and / or I(o) is H. In other embodiments, R2 is F. In other embodiments, R2 is CF3. In other embodiments, R2 is Cl. In other embodiments, R2 is Br. In other embodiments, R2 is I. In other embodiments, R2 is OH. In other embodiments, R2 is SH. In other embodiments, R2 is a substituted or unsubstituted C1-C5 alkyl group. In other embodiments, R2 is CH2OH. In other embodiments, R2 is CH2OCH3. In other embodiments, R2 is a C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl group. In other embodiments, R2 is a substituted or unsubstituted C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy group. In other embodiments, R2 is a 3-8 membered carbon ring or heterocycle. In other embodiments, R2 is a 3-8 membered heterocycle. In other embodiments, R2 is an oxobutane. In other embodiments, R2 is a 3-8 member carbon ring.

[0796] In some embodiments, R1 and R2 of formulas A, I(h), I(m), and / or I(o) are connected to form C=O. In other embodiments, R1 and R2 are connected to form a 3-8 membered carbon ring or heterocycle. In other embodiments, R1 and R2 are connected to form a 3-8 membered carbon ring. In some embodiments, the carbon ring is cyclopropyl. In other embodiments, R1 and R2 are connected to form a 3-8 membered heterocycle.

[0797] In some embodiments, R1 and R2 of formula A or formula I(a) and / or I(h) are not connected to form =O.

[0798] In some embodiments, R3 in formula A, I(h), I(m), and / or I(o) is H. In some embodiments, R3 is methyl. In some embodiments, R3 is a substituted or unsubstituted C1-C5 alkyl group. In some embodiments, the alkyl group is methoxyethylidene, methylaminoethylidene, or aminoethylidene; each of which represents a separate embodiment according to the invention. In some embodiments, R3 is -R8-OR 10 In some embodiments, R3 is (CH2)2-O-CH3. In some embodiments, R3 is R8-N(R 10 (R) 11 In some embodiments, R3 is (CH2)2-NH(CH3). In some embodiments, R3 is a substituted or unsubstituted C3-C8 cycloalkyl group. In some embodiments, the cycloalkyl group is cyclopropyl. In some embodiments, R3 is a substituted or unsubstituted 5-7 membered heterocycle. In some embodiments, the heterocycle is pyrrolidine, methylpyrrolidine, or piperidine; each representing a separate embodiment according to the invention. In some embodiments, R3 is pyrrolidine. In some embodiments, R3 is methylpyrrolidine. In some embodiments, R3 is piperidine. In some embodiments, R3 is R as defined below. 20 .

[0799] In some embodiments, R4 of formula A, I(h), I(m), and / or I(o) is H. In some embodiments, R4 is methyl. In some embodiments, R4 is a substituted or unsubstituted C1-C5 alkyl group. In some embodiments, the alkyl group is methoxyethylidene, methylaminoethylidene, or aminoethylidene; each of which represents a separate embodiment according to the invention. In some embodiments, R4 is -R8-OR 10 In some embodiments, R4 is (CH2)2-O-CH3. In some embodiments, R4 is R8-N(R 10 (R) 11 In some embodiments, R4 is (CH2)2-NH(CH3). In some embodiments, R4 is a substituted or unsubstituted C3-C8 cycloalkyl group. In some embodiments, the cycloalkyl group is cyclopropyl. In some embodiments, R4 is a substituted or unsubstituted 5-7 membered heterocycle. In some embodiments, the heterocycle is pyrrolidine, methylpyrrolidine, or piperidine; each representing a separate embodiment according to the invention. In some embodiments, R4 is pyrrolidine. In some embodiments, R4 is methylpyrrolidine. In some embodiments, R4 is piperidine. In some embodiments, R4 is R as defined below. 20 .

[0800] In some embodiments, R3 and R4 of formulas A, I(h), I(m), and / or I(o) are linked to form a 3-8 membered heterocycle. In some embodiments, the heterocycle is an imidazole, pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, or piperazine; each representing a separate embodiment according to the invention.

[0801] In some embodiments, R2 and R4 of formula A, I(h), and / or I(m) are linked to form ring F. In some embodiments, ring F is absent. In some embodiments, ring F is a substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycle. In some embodiments, R2 and R4 are linked to form pyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyridine, piperidine, imidazole, pyrimidine, triazole, oxadiazole, pyrazole; each representing a separate embodiment according to the invention. In some embodiments, ring F is an unsubstituted, saturated 4-8 membered heterocycle. In some embodiments, ring F is pyrrolidine, morpholine, or piperidine; each representing a separate embodiment according to the invention. In some embodiments, ring F is a substituted, saturated 4-8 membered heterocycle. In some embodiments, ring F is 1-methylpyrrolidine, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, or pyrrolidine-3-carboxynitrile; each representing a separate embodiment according to the invention. In some embodiments, ring F is a substituted or unsubstituted or unsaturated 4-8 membered heterocycle. In some embodiments, ring F is pyrrolidone-2-one, pyrrolidone-3-one, pyridine, piperidin-2-one, imidazole, pyrimidine, triazole, oxadiazole, or pyrazole; each representing a separate embodiment according to the invention. In some embodiments, if ring F is aromatic, then R1 is absent. In some embodiments, if ring F is aromatic, then R3 is absent. In some embodiments, if ring F is aromatic, then R1 and / or R3 are absent.

[0802] In some embodiments, R2 and R4 of formula A, I(h) and / or I(m) are linked to form a substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycle. In some embodiments, the heterocycle is pyrrolidine, morpholine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, pyrrolidine-3-carboxynitrile, pyridine, piperidine, piperidin-2-one, imidazole, pyrimidine, triazole, oxadiazole, or pyrazole; each representing a separate embodiment according to the invention.

[0803] In some embodiments, if X1 in equation A is 0, then R4 does not exist.

[0804] In some embodiments, R2 and R4 of formula I(h) and / or I(m) are connected to form ring F. In some embodiments, ring F is absent. In some embodiments, ring F is a substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycle. In some embodiments, ring F is an unsubstituted, saturated 4-8 membered heterocycle. In some embodiments, ring F is pyrrolidine, morpholine, or piperidine; each represents a separate embodiment according to the invention. In some embodiments, ring F is a substituted, saturated 4-8 membered heterocycle. In some embodiments, ring F is 1-methylpyrrolidine, 3,3-difluoropyrrolidine, pyrrolidine-3-ol, 3-methoxypyrrolidine, 3-(difluoromethyl)pyrrolidine, or pyrrolidine-3-carboxynitrile; each represents a separate embodiment according to the invention. In some embodiments, ring F is a substituted or unsubstituted or unsaturated 4-8 membered heterocycle. In some embodiments, ring F is pyrrolidone-2-one, pyrrolidone-3-one, pyridine, piperidin-2-one, imidazole, pyrimidine, triazole, oxadiazole, or pyrazole; each of which represents a separate embodiment according to the invention.

[0805] In some embodiments, ring F of formula I(h) and / or I(m) is absent. In some embodiments, ring F is a substituted or unsubstituted, saturated or unsaturated 4-8 membered heterocycle. In some embodiments, ring F is a substituted, saturated 4-8 membered heterocycle. In some embodiments, ring F is a substituted, unsaturated 4-8 membered heterocycle. In some embodiments, ring F is an unsubstituted, saturated 4-8 membered heterocycle. In some embodiments, ring F is an unsubstituted, unsaturated 4-8 membered heterocycle. In some embodiments, ring F is pyrrolidine. In some embodiments, ring F is pyrrolidine-2-one. In some embodiments, ring F is piperidine. In some embodiments, ring F is piperazine. In some embodiments, ring F is morpholine. In some embodiments, ring F is pyridinyl. In other embodiments, ring F is 2-pyridinyl. In other embodiments, ring F is pyrimidine. In other embodiments, ring F is imidazole. In other embodiments, ring F is pyridazine. In other embodiments, ring F is pyrazine. In other embodiments, ring F is pyrazole. In other embodiments, ring F is thiazole. In other embodiments, ring F is isothiazolyl. In other embodiments, ring F is thiadiazolyl. In other embodiments, ring F is triazolyl. In other embodiments, ring F is thiazolyl. In other embodiments, ring F is oxazolyl. In other embodiments, ring F is isoxazolyl. In other embodiments, ring F is pyrroleyl. In other embodiments, ring F is oxadiazolyl. In other embodiments, ring F is 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, or 1,3,4-oxadiazolyl; each being a separate embodiment of the invention. In other embodiments, ring F is oxazoloneyl. In other embodiments, ring F is oxazolidinoneyl. In other embodiments, ring F is thiazolyl. In other embodiments, ring F is isothiazolinoneyl. In other embodiments, ring F is isoxazolidinoneyl. In other embodiments, ring F is imidazolinoneyl. In other embodiments, ring F is pyrazoloneyl. In other embodiments, ring F is 2H-pyrrole-2-one. In other embodiments, ring F is triazolopyrimidine. In other embodiments, ring F 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 of which is a separate embodiment of the invention. In other embodiments, ring F is 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine.

[0806] In some embodiments, R7 in equation I(a) is OR20 Substituted or unsubstituted 4-7 membered heterocycles (e.g., morpholine, tetrahydrofuran, tetrahydropyran, oxetane, oxetane-3-ol, pyrrolidine, pyrrolidine-2-ol, pyrrolidine-3-ol, 3-methoxypyrrolidine, 1-methylpyrrolidine, pyrrolidine-2-one, pyrrolidine-3-one, pyrrolidine-3-carboxynitrile, 3-cyanopyrrolidine, pyrrolidone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidine-3-ol, piperidine-4-ol, piperidine-2-one, piperidine-4-carboxynitrile, 4-fluoropiperidine, oxadiazole, triazole, pyrazole, 2-oxopyrrolidine; each representing a separate embodiment according to the invention) or substituted or unsubstituted aryl groups. In some embodiments, R7 in equation I(a) is represented by equation A, where X1, R1, R2, R3 and R4 are as defined above, except that R1 and R2 cannot be connected to form =0.

[0807] In some embodiments, R7' in formula I(c) is not H.

[0808] In some embodiments, R7' of formulas I, II, I(a)-I(b) and / or I(d)-I(o) is H. In some embodiments, R7' of formulas I, II and / or I(a)-I(o) is F, Cl, Br, I, OH, OR. 20 ,SH,R8-OH,R8-SH,-R8-OR 10 R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11), CH(CF3)(NH-R 10 C1-C5 straight-chain or branched, substituted or unsubstituted alkyl, C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl, C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy, optionally wherein at least one methylene (CH2) of said alkoxy is replaced by an oxygen atom, methoxy, C1-C5 straight-chain or branched thioalkoxy, C1-C5 straight-chain or branched haloalkoxy, C1-C5 Straight-chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl, cyclopropyl, cyclohexyl, substituted or unsubstituted 3-8 membered heterocycles, morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine, substituted or unsubstituted aryl or substituted or unsubstituted benzyl; each represents a separate embodiment according to the invention. In some embodiments, the heterocycle is morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine; each represents a separate embodiment according to the invention. In some embodiments, R7' is morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine; each representing a separate embodiment according to the invention. In some embodiments, R7' is further substituted with at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R)2), C(O)-pyrrolidine, C(O)-piperidine, N(R)2NH(R) 10 ), N(R 10 (R) 11 (e.g., N(CH3)2, NH2), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (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 NO2; each of which represents a separate embodiment according to the invention.

[0809] In some embodiments, R7' of formulas I, II, and / or I(a)-I(o) is H. In some embodiments, R7' is F. In some embodiments, R7' is Cl. In some embodiments, R7' is Br. In some embodiments, R7' is I. In some embodiments, R7' is CF3. In some embodiments, R7' is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group. In some embodiments, R7' is a C1-C5 straight-chain or branched unsubstituted alkyl group. In some embodiments, the alkyl group is isopropyl, methyl, or ethyl; each representing a separate embodiment according to the invention. In some embodiments, R7' is a C1-C5 straight-chain or branched substituted alkyl group. In some embodiments, R7' is isopropyl. In some embodiments, R7' is methyl. In some embodiments, R7' is ethyl. In some embodiments, R7' is a C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl group. In some embodiments, R7' is a C1-C5 straight-chain or branched haloalkyl group. In some embodiments, the haloalkyl group is CHF2. In some embodiments, R7' is a C3-C8 cyclic haloalkyl. In some embodiments, R7' is a substituted or unsubstituted C3-C8 cycloalkyl. In some embodiments, the cycloalkyl group is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; each representing a separate embodiment according to the invention. In some embodiments, the cycloalkyl group is cyclopropyl. In some embodiments, the cycloalkyl group is cyclohexyl. In some embodiments, R7' is morpholine. In some embodiments, R7' is pyran. In some embodiments, R7' is oxacyclobutane. In some embodiments, R7' is pyrrolidine. In some embodiments, R7' is 3,3-difluoropyrrolidine. In some embodiments, R7' is imidazole. In some embodiments, R7' is pyrazole. In some embodiments, R7' is triazole. In some embodiments, R7' is piperazine. In some embodiments, R7' is piperidine. In some embodiments, R7' is piperidin-2-one. In some embodiments, R7' is piperidin-4-ol. In some embodiments, R7' is dioxazole. In some embodiments, R7' is 2-oxopyrrolidine.

[0810] In some embodiments, R7 and R7' of formulas I, II, and / or I(a)-I(f) are connected to form a 3-8 member substituted or unsubstituted, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring, including but not limited to cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, and pyrrolidine; each representing a separate embodiment according to the invention. In some embodiments, R7 and R7' are connected to form a 5 or 6 member substituted or unsubstituted, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring. In some embodiments, R7 and R7' are connected to form a 5 member unsubstituted saturated or unsaturated carbocyclic ring. In some embodiments, R7 and R7' are connected to form a 6 member unsubstituted saturated or unsaturated carbocyclic ring. In some embodiments, R7 and R7' are connected to form a cyclohexyl group. In some embodiments, R7 and R7' are connected to form a 5 member substituted saturated or unsaturated carbocyclic ring. In some embodiments, R7 and R7' are connected to form a cyclopentyl group. In some embodiments, R7 and R7' are connected to form a 6-membered substituted saturated or unsaturated carbocyclic ring. In some embodiments, R7 and R7' are connected to form a 6-membered substituted or unsubstituted aromatic carbocyclic ring. In some embodiments, R7 and R7' are connected to form a 5- or 6-membered substituted or unsubstituted aromatic heterocyclic ring. In some embodiments, R7 and R7' are connected to form a 5- or 6-membered substituted or unsubstituted heterocyclic ring. In some embodiments, R7 and R7' are connected to form a 6-membered substituted or unsubstituted heterocyclic ring. In some embodiments, R7 and R7' are connected to form piperidine. In some embodiments, R7 and R7' are connected to form tetrahydropyran. In some embodiments, R7 and R7' are connected to form a 5-membered substituted or unsubstituted heterocyclic ring. In some embodiments, R7 and R7' are connected to form pyrrolidine. In some embodiments, R7 and R7' are connected to form tetrahydrofuran.

[0811] In some embodiments, R7 and R7' of Formula I(c) are different. In some embodiments, R7 and R7' of Formula I(c) are not H, F, Cl, C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy, C1-C5 straight-chain or branched haloalkoxy or C1-C5 straight-chain or branched, substituted or unsubstituted alkyl; each represents a separate embodiment according to the invention.

[0812] In some embodiments, R7” in formulas I(i)-I(o) is H. In some embodiments, R7” in formulas I(i)-I(m) is F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 The following are examples of alkyl groups: C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups, C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy groups, optionally wherein at least one methylene (CH2) of the alkoxy group is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy groups, C1-C5 straight-chain or branched haloalkoxy groups, C1-C5 straight-chain or branched alkoxyalkyl groups, substituted or unsubstituted C3-C8 cycloalkyl groups, substituted or unsubstituted 3-8 membered heterocycles, substituted or unsubstituted aryl groups, or substituted or unsubstituted benzyl groups; each of which represents a separate embodiment according to the invention. In some embodiments, R7” is further substituted with at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R)2), C(O)-pyrrolidine, C(O)-piperidine, N(R)2NH(R) 10 ), N(R 10 (R) 11(e.g., N(CH3)2, NH2), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (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 NO2; each of which represents a separate embodiment according to the invention.

[0813] In some embodiments, R7” of formulas I(i)-I(o) is H. In some embodiments, R7” is F. In some embodiments, R7” is Cl. In some embodiments, R7” is Br. In some embodiments, R7” is I. In some embodiments, R7” is CF3. In some embodiments, R7” is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group. In some embodiments, R7” is a C1-C5 straight-chain or branched unsubstituted alkyl group. In some embodiments, the alkyl group is isopropyl, methyl, or ethyl; each representing a separate embodiment according to the invention. In some embodiments, R7” is a C1-C5 straight-chain or branched substituted alkyl group. In some embodiments, R7” is isopropyl. In some embodiments, R7” is methyl. In some embodiments, R7” is ethyl. In some embodiments, R7” is a C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy group, optionally wherein at least one methylene (CH2) in the alkoxy group is substituted with an oxygen atom. In some embodiments, R7” is a C1-C5 straight-chain or branched alkoxy group. In some embodiments, R7” is methoxy. In some embodiments, R7” is a C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl. In some embodiments, R7” is a C1-C5 straight-chain or branched haloalkyl. In some embodiments, the haloalkyl is CHF2. In some embodiments, R7” is a C3-C8 cyclic haloalkyl. In some embodiments, R7” is a substituted or unsubstituted C3-C8 cycloalkyl. In some embodiments, the cycloalkyl is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; each representing a separate embodiment according to the invention. In some embodiments, the cycloalkyl is cyclopropyl. In some embodiments, the cycloalkyl is cyclohexyl. In some embodiments, R7” is a substituted or unsubstituted 3-8 membered heterocycle. In some embodiments, R7” is morpholine. In some embodiments, R7” is pyran. In some embodiments, R7” is oxetane. In some embodiments, R7” is pyrrolidine. In some embodiments, R7”” is 3,3-difluoropyrrolidine. In some embodiments, R7” is imidazole. In some embodiments, R7”” is pyrazole. In some embodiments, R7”” is triazole. In some embodiments, R7”” is piperazine. In some embodiments, R7”” is piperidine. In some embodiments, R7”” is piperidin-2-one. In some embodiments, R7”” is piperidin-4-ol. In some embodiments, R7”” is dioxazole. In some embodiments, R7”” is 2-oxopyrrolidine.

[0814] In some embodiments, R7' and R7" of formulas I(j)-I(o) are connected to form a 3-8 member substituted or unsubstituted, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring, including but not limited to cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, and pyrrolidine; each representing a separate embodiment according to the invention. In some embodiments, R7' and R7" are connected to form a 5 or 6 member substituted or unsubstituted, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring. In some embodiments, R7' and R7" are connected to form a 5 member unsubstituted saturated or unsaturated carbocyclic ring. In some embodiments, R7' and R7" are connected to form a 6 member unsubstituted saturated or unsaturated carbocyclic ring. In some embodiments, R7' and R7" are connected to form a cyclohexyl group. In some embodiments, R7' and R7" are connected to form a 5 member substituted saturated or unsaturated carbocyclic ring. In some embodiments, R7' and R7" are connected to form a cyclopentyl group. In some embodiments, R7' and R7" are connected to form a 6-membered substituted saturated or unsaturated carbocyclic ring. In some embodiments, R7' and R7" are connected to form a 6-membered substituted or unsubstituted aromatic carbocyclic ring. In some embodiments, R7' and R7" are connected to form a 5- or 6-membered substituted or unsubstituted aromatic heterocyclic ring. In some embodiments, R7' and R7" are connected to form a 5- or 6-membered substituted or unsubstituted heterocyclic ring. In some embodiments, R7' and R7" are connected to form a 6-membered substituted or unsubstituted heterocyclic ring. In some embodiments, R7' and R7" are connected to form piperidine. In some embodiments, R7' and R7" are connected to form tetrahydropyran. In some embodiments, R7' and R7" are connected to form a 5-membered substituted or unsubstituted heterocyclic ring. In some embodiments, R7' and R7" are connected to form pyrrolidine. In some embodiments, R7' and R7" are connected to form tetrahydrofuran.

[0815] In some embodiments, R7' and R7' of formula I(c) and / or I(i)-I(o) are different. In some embodiments, R7 and R7' of formula I(c) and / or I(i)-I(n) are not H, F, Cl, C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy, C1-C5 straight-chain or branched haloalkoxy or C1-C5 straight-chain or branched, substituted or unsubstituted alkyl; each of which represents a separate embodiment according to the invention.

[0816] In some embodiments, R7”' of formula I(i) is H. In some embodiments, R7”' of formula I(i) is F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 The following are examples of alkyl groups: C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups, C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy groups, optionally wherein at least one methylene (CH2) of the alkoxy group is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy groups, C1-C5 straight-chain or branched haloalkoxy groups, C1-C5 straight-chain or branched alkoxyalkyl groups, substituted or unsubstituted C3-C8 cycloalkyl groups, substituted or unsubstituted 3-8 membered heterocycles, substituted or unsubstituted aryl groups, or substituted or unsubstituted benzyl groups; each of which represents a separate embodiment according to the invention. In some embodiments, R7”' is further substituted with at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R)2), C(O)-pyrrolidine, C(O)-piperidine, N(R)2NH(R) 10 ), N(R 10 (R) 11(e.g., N(CH3)2, NH2), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (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 NO2; each of which represents a separate embodiment according to the invention.

[0817] In some embodiments, R7”' of formula I(i) is H. In some embodiments, R7”' is F. In some embodiments, R7”' is Cl. In some embodiments, R7”' is Br. In some embodiments, R7”' is I. In some embodiments, R7”' is CF3. In some embodiments, R7”' is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group. In some embodiments, R7”' is a C1-C5 straight-chain or branched unsubstituted alkyl group. In some embodiments, the alkyl group is isopropyl, methyl, or ethyl; each representing a separate embodiment according to the invention. In some embodiments, R7”' is a C1-C5 straight-chain or branched substituted alkyl group. In some embodiments, R7”' is isopropyl. In some embodiments, R7”' is methyl. In some embodiments, R7”' is ethyl. In some embodiments, R7”' is a C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy group, optionally wherein at least one methylene (CH2) group in the alkoxy group is replaced by an oxygen atom. In some embodiments, R7”' is a C1-C5 straight-chain or branched alkoxy group. In some embodiments, R7”' is a methoxy group. In some embodiments, R7”' is a C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl group. In some embodiments, R7”' is a C1-C5 straight-chain or branched haloalkyl group. In some embodiments, the haloalkyl group is CHF2. In some embodiments, R7”' is a C3-C8 cyclic haloalkyl group. In some embodiments, R7”' is a substituted or unsubstituted C3-C8 cyclic alkyl group. In some embodiments, the cyclic alkyl group is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; each of which represents a separate embodiment according to the invention. In some embodiments, R7”' is a substituted or unsubstituted 3-8 membered heterocycle. In some embodiments, R7”' is morpholine. In some embodiments, R7”' is pyran. In some embodiments, R7”' is oxetane. In some embodiments, R7”' is pyrrolidine. In some embodiments, R7”' is 3,3-difluoropyrrolidine. In some embodiments, R7”' is imidazole. In some embodiments, R7”' is pyrazole. In some embodiments, R7”' is triazole. In some embodiments, R7”' is piperazine. In some embodiments, R7”' is piperidine. In some embodiments, R7”' is piperidin-2-one. In some embodiments, R7”' is piperidin-4-ol. In some embodiments, R7”' is dioxazole. In some embodiments, R7”' is 2-oxopyrrolidine.

[0818] In some embodiments, R7”” in formula I(i) is H. In some embodiments, R7”” in formula I(i) is F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocyclic), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R) 10 ), N(R 10 (R) 11 ), R8-N(R 10 (R) 11 ), R9-R8-N(R 10 (R) 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 NHCO-N(R) 10 (R) 11 ), COOH, -C(O)Ph, C(O)OR 10 R8-C(O)-R 10 C(O)H, C(O)-R 10 C1-C5 straight-chain or branched C(O)-haloalkyl, -C(O)NH2, C(O)NHR, C(O)N(R) 10 (R) 11 SO2R, SO2N(R) 10 (R) 11 ), CH(CF3)(NH-R 10 The following are examples of alkyl groups: C1-C5 straight-chain or branched, substituted or unsubstituted alkyl groups, C1-C5 straight-chain or branched, substituted or unsubstituted alkenyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl groups, C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy groups, optionally wherein at least one methylene (CH2) of the alkoxy group is replaced by an oxygen atom, C1-C5 straight-chain or branched thioalkoxy groups, C1-C5 straight-chain or branched haloalkoxy groups, C1-C5 straight-chain or branched alkoxyalkyl groups, substituted or unsubstituted C3-C8 cycloalkyl groups, substituted or unsubstituted 3-8 membered heterocycles, substituted or unsubstituted aryl groups, or substituted or unsubstituted benzyl groups; each of which represents a separate embodiment according to the invention. In some embodiments, R7”” is further substituted by at least one of the following: F, Cl, Br, I, C1-C5 straight-chain or branched alkyl, OH, alkoxy (e.g., OMe), amide (e.g., C(O)N(R)2), C(O)-pyrrolidine, C(O)-piperidine, N(R)2NH(R) 10 ), N(R 10 (R) 11(e.g., N(CH3)2, NH2), CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (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 NO2; each of which represents a separate embodiment according to the invention.

[0819] In some embodiments, R7”” of formula I(i) is H. In some embodiments, R7”” is F. In some embodiments, R7”” is Cl. In some embodiments, R7”” is Br. In some embodiments, R7”” is I. In some embodiments, R7”” is CF3. In some embodiments, R7”” is a C1-C5 straight-chain or branched, substituted or unsubstituted alkyl group. In some embodiments, R7”” is a C1-C5 straight-chain or branched unsubstituted alkyl group. In some embodiments, the alkyl group is isopropyl, methyl, or ethyl; each representing a separate embodiment according to the invention. In some embodiments, R7”” is a C1-C5 straight-chain or branched substituted alkyl group. In some embodiments, R7”” is isopropyl. In some embodiments, R7”” is methyl. In some embodiments, R7”” is ethyl. In some embodiments, R7”” is a C1-C5 straight-chain or branched or C3-C8 cyclic alkoxy group, optionally wherein at least one methylene (CH2) in the alkoxy group is replaced by an oxygen atom. In some embodiments, R7”” is a C1-C5 straight-chain or branched alkoxy group. In some embodiments, R7”” is a methoxy group. In some embodiments, R7”” is a C1-C5 straight-chain or branched or C3-C8 cyclic haloalkyl group. In some embodiments, R7”” is a C1-C5 straight-chain or branched haloalkyl group. In some embodiments, the haloalkyl group is CHF2. In some embodiments, R7”” is a C3-C8 cyclic haloalkyl group. In some embodiments, R7”” is a substituted or unsubstituted C3-C8 cyclic alkyl group. In some embodiments, the cyclic alkyl group is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; each of which represents a separate embodiment according to the invention. In some embodiments, R7”” is a substituted or unsubstituted 3-8 membered heterocycle. In some embodiments In this context, R7”” is morpholine. In some embodiments, R7”” is pyran. In some embodiments, R7”” is oxacyclobutane. In some embodiments, R7”” is pyrrolidine. In some embodiments, R7”” is 3,3-difluoropyrrolidine. In some embodiments, R7”” is imidazole. In some embodiments, R7”” is pyrazole. In some embodiments, R7”” is triazole. In some embodiments, R7”” is piperazine. In some embodiments, R7”” is piperidine. In some embodiments, R7”” is piperidin-2-one. In some embodiments, R7”” is piperidin-4-ol. In some embodiments, R7”” is dioxazole. In some embodiments, R7”” is 2-oxopyrrolidine.

[0820] In some embodiments, R7' and R7" of Formula I(i) are connected to form a 3-8 member substituted or unsubstituted, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring. In some embodiments, R7' and R7" are connected to form a 5 member unsubstituted, saturated or unsaturated carbocyclic ring. In some embodiments, R7' and R7" are connected to form cyclopentane. In some embodiments, R7' and R7" are connected to form a 6 member unsubstituted, saturated or unsaturated carbocyclic ring. In some embodiments, R7' and R7" are connected to form cyclohexane. In some embodiments, R7' and R7" are connected to form a 5 member substituted, saturated or unsaturated carbocyclic ring. In some embodiments, R7' and R7" are connected to form a 6 member substituted, saturated or unsaturated carbocyclic ring. In some embodiments, R7' and R7" are connected to form a 6 member substituted or unsubstituted, aromatic carbocyclic ring. In some embodiments, R7' and R7" are connected to form a 5- or 6-membered substituted or unsubstituted aromatic heterocycle. In some embodiments, R7' and R7" are connected to form a 5- or 6-membered substituted or unsubstituted heterocycle. In some embodiments, R7' and R7" are connected to form a 6-membered substituted or unsubstituted heterocycle. In some embodiments, R7' and R7" are connected to form piperidine. In some embodiments, R7' and R7" are connected to form tetrahydropyran. In some embodiments, R7' and R7" are connected to form a 5-membered substituted or unsubstituted heterocycle. In some embodiments, R7' and R7" are connected to form tetrahydrofuran. In some embodiments, R7' and R7" are connected to form pyrrolidine.

[0821] In some embodiments, R7' and R7" of Formula I(i) are different. In some embodiments, R7' and R7" of Formula I(i) are not H, F, Cl, C1-C5 straight or branched or C3-C8 cyclic alkoxy, C1-C5 straight or branched haloalkoxy or C1-C5 straight or branched, substituted or unsubstituted alkyl; each represents a separate embodiment according to the invention.

[0822] In some embodiments, R7” and R7 of Formula I(i) are connected to form a 3-8 member substituted or unsubstituted, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring. In some embodiments, R7” and R7 are connected to form a 5 member unsubstituted saturated or unsaturated carbocyclic ring. In some embodiments, R7” and R7 are connected to form cyclopentane. In some embodiments, R7” and R7 are connected to form a 6 member unsubstituted saturated or unsaturated carbocyclic ring. In some embodiments, R7” and R7 are connected to form cyclohexane. In some embodiments, R7” and R7 are connected to form a 5 member substituted saturated or unsaturated carbocyclic ring. In some embodiments, R7” and R7 are connected to form a 6 member substituted saturated or unsaturated carbocyclic ring. In some embodiments, R7’ and R7” are connected to form a 6 member substituted or unsubstituted aromatic carbocyclic ring. In some embodiments, R7” and R7 are connected to form a 5- or 6-membered substituted or unsubstituted aromatic heterocycle. In some embodiments, R7” and R7 are connected to form a 5- or 6-membered substituted or unsubstituted heterocycle. In some embodiments, R7” and R7 are connected to form a 6-membered substituted or unsubstituted heterocycle. In some embodiments, R7” and R7 are connected to form piperidine. In some embodiments, R7” and R7 are connected to form tetrahydropyran. In some embodiments, R7” and R7 are connected to form a 5-membered substituted or unsubstituted heterocycle. In some embodiments, R7” and R7 are connected to form tetrahydrofuran. In some embodiments, R7” and R7 are connected to form pyrrolidine.

[0823] In some embodiments, R7” and R7 of formula I(i) are different. In some embodiments, R7” and R7 of formula I(i) are not H, F, Cl, C1-C5 straight or branched or C3-C8 cyclic alkoxy, C1-C5 straight or branched haloalkoxy or C1-C5 straight or branched, substituted or unsubstituted alkyl; each represents a separate embodiment according to the invention.

[0824] In some embodiments, R7 and R7"' of Formula I(i) are connected to form a 3-8 substituted or unsubstituted, saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring. In some embodiments, R7 and R7"' are connected to form a 5 substituted or unsubstituted saturated or unsaturated carbocyclic ring. In some embodiments, R7 and R7"' are connected to form a 6 substituted or unsubstituted saturated or unsaturated carbocyclic ring. In some embodiments, R7 and R7"' are connected to form a 6 substituted or unsubstituted aromatic carbocyclic ring. In some embodiments, R7 and R7"' are connected to form a 5 or 6 substituted or unsubstituted aromatic heterocyclic ring. In some embodiments, R7 and R7"' are connected to form a 5 or 6 substituted or unsubstituted heterocyclic ring. In some embodiments, R7 and R7"' are connected to form a 6-membered substituted or unsubstituted heterocycle. In some embodiments, R7 and R7"' are connected to form piperidine. In some embodiments, R7 and R7"' are connected to form tetrahydrofuran. In some embodiments, R7 and R7"' are connected to form tetrahydropyran. In some embodiments, R7 and R7"' are connected to form a 5-membered substituted or unsubstituted heterocycle. In some embodiments, R7 and R7"' are connected to form pyrrolidine. In some embodiments, R7 and R7"' are connected t...

Claims

1. A compound represented by the structure of Formula I(j): in X2, X3 and X4 are each independently nitrogen or CH; X 10 is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH)); Ring W is a 3-10 membered single, fused, bridged or spiro, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring (e.g., morpholine (2-morpholine or 3-morpholine), tetrahydrofuran, tetrahydropyran, oxetane, pyrrolidine, pyrrolidin-2-one, pyrrolidin-3-one, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidin-2-one, oxadiazole, triazole, 2-oxopyrrolidine, cyclopropyl, 2,2-dimethylpyrrole oxime, 2-oxa-5-azaspiro[3.4]octane, 1,4-dioxa-6-azaspiro[4.4]nonane, 3,3-dimethylmorpholine, 1-methylpiperazine, 4,7-diazaspiro[2.5]octane, bicyclo[1.1.1]pentane, 2,5-diazabicyclo[2.2.1]heptane, piperazine, piperazin-2-one); W1 is CH2, C=O or CH(R 10 )(e.g., CHCH3); R7' and R7" are each independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 、R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocycle), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R 10 )、N(R 10 )(R 11 )、R8-N(R 10 )(R 11 )、R9-R8-N(R 10 )(R 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 、NHCO-N(R 10 )(R 11 )、COOH、-C(O)Ph、C(O)OR 10 、R8-C(O)-R 10 、C(O)H、C(O)-R 10 、C1-C5 straight chain or branched C(O)-haloalkyl、-C(O)NH2、C(O)NHR、C(O)N(R 10 )(R 11 )、SO2R、SO2N(R 10 )(R 11 )、CH(CF3)(NH-R 10 ), C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) in the alkoxy is replaced by an oxygen atom, C1-C5 straight chain or branched thioalkoxy ... -C5 straight chain or branched haloalkoxy, C1-C5 straight chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl; or R7′ and R7″ are connected to form a 3-8 membered substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine); R 20 Represented by the following structure: R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R 10 ), NH-CH2-cyclopropyl, N(R 10 )(R 11 ), CF3, CN, NO2, COOH, C1-C5 straight or branched, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl, cyclopropyl, C1-C5 straight or branched alkoxy, isopropoxy, C1-C5 straight or branched haloalkyl (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 (CH2-OH, CH2-CH2-OH), -R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl (e.g., phenyl), substituted or unsubstituted heteroaryl (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine)); R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 )、N(R 10 )(R 11 ), CF3, CN, NO2, C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight chain or branched alkoxy, C1-C5 straight chain or branched haloalkyl (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 、-R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl (e.g., phenyl), substituted or unsubstituted heteroaryl (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine)); R 200 It is H, R 20 、F、Cl、Br、I、OH、SH、alkoxy、NH2、N(R)2、NH(R 10 )、N(R 10 )(R 11 ), CF3, CN, NO2, C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight chain or branched alkoxy (e.g., methoxy), C1-C5 straight chain or branched haloalkyl (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 、-R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl (e.g., phenyl), substituted or unsubstituted heteroaryl (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine)); or R 200 and the carbon atom to which it is attached is C=O, C=NO(R) (e.g., C=NO-CH3) or C(R)2 (e.g., C(CH3)2, CF2); Each R8 is independently [CH2] p Where p is between 1 and 10; R9 is [CH] q , [C] q Where q is between 2 and 10; R 10 and R 11 are each independently H, C1-C5 substituted or unsubstituted straight or branched alkyl (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), C1-C5 substituted or unsubstituted straight or branched haloalkyl (e.g., CH2CF3), C1-C5 straight or branched alkoxy (e.g., O-CH3), R 20 , C(O)R or S(O)2R; or R 10 and R 11 connected to form a substituted or unsubstituted 3-8 membered heterocyclic ring (eg, piperazine, piperidine), n is an integer between 0 and 4 (eg, 1, 2); or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., a deuterated analog), PROTAC, drug product, or any combination thereof.

2. The compound according to claim 1, wherein Ring W is a 3-8 membered single saturated heterocyclic ring, preferably morpholine (2-morpholine or 3-morpholine), tetrahydrofuran, tetrahydropyran, oxetane, pyrrolidine, isoxazolidine, piperazine, piperidine; 3-8 membered single unsaturated heterocyclic ring, preferably pyrrolidin-2-one, pyrrolidin-3-one, imidazole, pyrazole, piperidin-2-one, piperazin-2-one, oxadiazole, triazole, 2-oxopyrrolidine; 3-10 membered spiro saturated heterocycle, preferably 4-azaspiro[2.4]heptane, 2-oxa-5-azaspiro[3.4]octane, 1,4-dioxa-6-azaspiro[4.4]nonane, 4,7-diazaspiro[2.5]octane; 3-10 membered bridged saturated heterocyclic ring, preferably bicyclo[1.1.1]pentane, 2,5-diazabicyclo[2.2.1]heptane; or a 3-8 membered single saturated carbocyclic ring (ie, cycloalkyl), preferably, cyclopropyl; R 200 is H, OH, F, NH2, C1-C5 straight chain or branched alkoxy, methoxy, CN, C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., methyl), C1-C5 straight chain or branched haloalkyl, CHF2, or R 200 and the carbon atom to which it is attached is C=O, C=NO(R) (e.g., C=NO-CH3) or C(R)2 (e.g., C(CH3)2, CF2) X2 and X3 are CH; X4 is N or CH; X 10 is N, CH, C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropyloxy) or C(COOH); R7' is H, F, Cl, CF3, C1-C5 linear or branched, substituted or unsubstituted alkyl, preferably methyl, C1-C5 linear or branched or C3-C8 cyclic alkoxy, preferably methoxy, substituted or unsubstituted C3-C8 cycloalkyl, preferably cyclopropyl or cyclohexyl, or substituted or unsubstituted aryl; R7” is H or F; n is 1 or 2; or any combination thereof.

3. The compound according to claim 1 or 2, which is selected from the following:

4. The compound of any one of claims 1 to 3, wherein the compound is not (R)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazole-7-carboxamide, (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazole-7-carboxamide or 2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-N-(3-(4-fluoropiperidin-1-yl)propyl)benzo[d]imidazo[2,1-b]thiazole-7-carboxamide.

5. A compound represented by the structure of Formula I(n): in X2, X3 and X4 are each independently nitrogen or CH; X 10 is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH)); Ring W is a 3-10 membered single, fused, bridged or spiro, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring (e.g., morpholine (2-morpholine or 3-morpholine), tetrahydrofuran, tetrahydropyran, oxetane, pyrrolidine, pyrrolidin-2-one, pyrrolidin-3-one, pyrrolidinone, imidazole, pyrazole, isoxazolidine, piperazine, piperidine, piperidin-2-one, oxadiazole, triazole, 2-oxo pyrrolidine, cyclopropyl, 4-azaspiro[2.4]heptane, pyrrolidin-3-one-O-methyloxime, 2-oxa-5-azaspiro[3.4]octane, 1,4-dioxa-6-azaspiro[4.4]nonane, 4,7-diazaspiro[2.5]octane, bicyclo[1.1.1]pentane, 2,5-diazabicyclo[2.2.1]heptane, piperazine, piperazin-2-one); R 200 It is H, R 20 、F、Cl、Br、I、OH、SH、alkoxy、methoxy、NH2、N(R)2、NH(R 10 )、N(R 10 )(R 11 ), CF3, CN, NO2, C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight chain or branched alkoxy (e.g., methoxy), C1-C5 straight chain or branched halogenated alkyl (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 、-R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl (e.g., phenyl), substituted or unsubstituted heteroaryl (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine)); or R 200 and the carbon atom to which it is attached is C=O, C=NO(R) (e.g., C=NO-CH3) or C(R)2 (e.g., C(CH3)2, CF2); R5 is H or C1-C5 straight or branched chain alkyl (e.g., methyl); R6 is H, C1-C5 straight or branched alkyl (e.g., methyl, ethyl, isopropyl), CD3, or substituted or unsubstituted, saturated or unsaturated, single, fused, bridged or spiro 3-10 membered carbocyclic or heterocyclic ring (e.g., piperidine (2-piperidine, 3-piperidine or 4-piperidine), 1-methylpiperidine (1-methyl-3-piperidine, 1-methyl-4-piperidine), 3-fluoro-1-methylpiperidine, 1-(2,2,2-trifluoroethyl)piperidine, azetidine, 1 -methyl-azetidine (1-methyl-3-azetidine), morpholine, pyrrolidine, pyrrolidone, quinuclidine, tetrahydropyran (4-tetrahydropyran or 3-tetrahydropyran), tetrahydrofuran, azaspiro[3.3]heptane, 8-methyl-8-azabicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane, 4,4-difluorocyclohexane, cyclopropyl); R7' and R7" are each independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 、R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocycle), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R 10 )、N(R 10 )(R 11 )、R8-N(R 10 )(R 11 )、R9-R8-N(R 10 )(R 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 、NHCO-N(R 10 )(R 11 )、COOH、-C(O)Ph、C(O)OR 10 、R8-C(O)-R 10 、C(O)H、C(O)-R 10 、C1-C5 straight chain or branched C(O)-haloalkyl、-C(O)NH2、C(O)NHR、C(O)N(R 10 )(R 11 )、SO2R、SO2N(R 10 )(R 11 )、CH(CF3)(NH-R 10 ), C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) in the alkoxy is replaced by an oxygen atom, C1-C5 straight chain or branched thioalkoxy ... -C5 straight chain or branched haloalkoxy, C1-C5 straight chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl; or R7′ and R7″ are linked to form a 3-8 membered substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine); R 20 Represented by the following structure: R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R 10 ), NH-CH2-cyclopropyl, N(R 10 )(R 11 ), CF3, CN, NO2, COOH, C1-C5 straight or branched, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl, cyclopropyl, C1-C5 straight or branched alkoxy, isopropoxy, C1-C5 straight or branched haloalkyl (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 、-R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl (e.g., phenyl), substituted or unsubstituted heteroaryl (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine)); R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 )、N(R 10 )(R 11 ), CF3, CN, NO2, C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight chain or branched alkoxy, C1-C5 straight chain or branched haloalkyl (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 、-R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl (e.g., phenyl), substituted or unsubstituted heteroaryl (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine)); Each R8 is independently [CH2] p Where p is between 1 and 10; R9 is [CH] q , [C] q Where q is between 2 and 10; R 10 and R 11 are each independently H, C1-C5 substituted or unsubstituted straight or branched alkyl (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), C1-C5 substituted or unsubstituted straight or branched haloalkyl (e.g., CH2CF3), C1-C5 straight or branched alkoxy (e.g., O-CH3), R 20 , C(O)R or S(O)2R; or R 10 and R 11 connected to form a substituted or unsubstituted 3-8 membered heterocyclic ring (e.g., piperazine, piperidine), n is an integer between 0 and 4 (e.g., 1, 2); or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., a deuterated analog), PROTAC, drug product, or any combination thereof.

6. The compound according to claim 5, wherein X2 and X3 are CH; X4 is CH or nitrogen; Ring W is a 3-10 membered single saturated heterocyclic ring, preferably morpholine (eg, 2-morpholine or 3-morpholine), tetrahydrofuran, tetrahydropyran, pyrrolidine, isoxazolidine, piperazine, piperidine; 3-10 membered single unsaturated heterocyclic ring, preferably, piperazin-2-one; 3-10 membered spiroheterocycle, preferably 4-azaspiro[2.4]heptane, 2-oxa-5-azaspiro[3.4]octane, 1,4-dioxa-6-azaspiro[4.4]nonane, 4,7-diazaspiro[2.5]octane; 3-10 membered bridged heterocycle, preferably, bicyclo[1.1.1]pentane, 2,5-diazabicyclo[2.2.1]heptane; or a 3-10 membered single unsaturated heterocyclic ring, preferably pyrrolidin-2-one, pyrrolidin-3-one, piperazin-2-one, piperidine-2-one, pyrrolidin-3-one-O-methyloxime; R 200 is H, OH, CN, NH2, C1-C5 straight chain or branched, substituted or unsubstituted alkyl, C1-C5 straight chain or branched alkoxy (e.g., methoxy), C1-C5 straight chain or branched haloalkyl (e.g., CHF2); or R 200 and the carbon atom to which it is attached is C=O, C=NO(R) (e.g., C=NO-CH3) or C(R)2 (e.g., C(CH3)2, CF2); R5 is H or C1-C5 straight or branched chain alkyl (e.g., methyl); R6 is H, C1-C5 linear or branched, substituted or unsubstituted alkyl, preferably methyl, ethyl or isopropyl, CD3, A substituted or unsubstituted saturated single 3-10 membered heterocycle, preferably piperidine (e.g., 2-piperidine, 3-piperidine or 4-piperidine), 1-methylpiperidine (e.g., 1-methyl-3-piperidine, 1-methyl-4-piperidine), 3-fluoro-1-methylpiperidine, 1-(2,2,2-trifluoroethyl)piperidine, azetidine, 1-methyl-azetidine (e.g., 1-methyl-3-azetidine), morpholine, tetrahydropyran (e.g., 4-tetrahydropyran or 3-tetrahydropyran), tetrahydrofuran, dioxane or 1,3-dioxane Saturated bridged or spiro 3-10 membered heterocycle, preferably 8-methyl-8-azabicyclo[3.2.1]octane, or a substituted or unsubstituted saturated single 3-10 membered carbon ring (ie, cycloalkyl), preferably, 4,4-difluorocyclohexane, cyclopropyl; R7' and R7" are each independently H or F; or any combination thereof.

7. A compound according to claim 5 or 6, wherein the carbocyclic ring or the heterocyclic ring as defined in R6 is further substituted by at least one substitution selected from the group consisting of F, Cl, Br, I, C1-C5 straight or branched alkyl, OH, alkoxy (e.g., OMe), amide, C(O)N(R)2, C(O)-alkyl, C(O)-pyrrolidine, C(O)-piperidine, N(R)2, NH(R)2, 10 )、N(R 10 )(R 11 ), N(CH3)2, NH2, CF3, aryl, phenyl, heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclobutanol), substituted or unsubstituted 3-8 membered heterocycle (e.g., pyran, oxetane, piperidine, pyrazole, triazole, imidazole), C1-C5 straight chain or branched haloalkyl (e.g., CH2CF3, CHF2), halophenyl, (benzyloxy)phenyl, CN and NO2.

8. according to the compound described in any one of claims 5 to 7, wherein R described substituted or unsubstituted ring is piperidine (for example, 2-piperidine, 3-piperidine or 4-piperidine), 1-methylpiperidine (for example, 1-methyl-3-piperidine, 1-methyl-4-piperidine), 3-fluoro-1-methylpiperidine, 1-(2,2,2-trifluoroethyl)piperidine, azetidine, 1-methyl-azetidine (for example, 1-methyl-3-azetidine), morpholine, tetrahydropyran (for example, 4-tetrahydropyran or 3-tetrahydropyran), tetrahydrofuran, dioxane or 1,3-dioxane, 8-methyl-8-azabicyclo[3.2.1]octane, 4,4-difluorocyclohexane or cyclopropyl.

9. A compound according to any one of claims 5 to 8, selected from the following:

10. A compound represented by the structure of Formula I(o): in X2, X3 and X4 are each independently nitrogen or CH; X5, X6, X7, X8 and X9 are each independently a nitrogen or carbon atom; X 10 is N, CH or C(R) (e.g., C(CH2)OH, C(CH2)2OH, C(NH-CH2-cyclopropyl), C(CH3), C(cyclopropyl), C(isopropoxy), C(COOH)); R1 is H, F, Cl, Br, I, OH, SH or CF3, substituted or unsubstituted C1-C5 alkyl (e.g., CH2OH), C1-C5 linear or branched or C3-C8 cyclic haloalkyl, substituted or unsubstituted C1-C5 linear or branched or C3-C8 cyclic alkoxy; R2 is a substituted or unsubstituted C1-C5 alkyl group (e.g., CH2OH, CH2OCH3), a 3-8 membered carbocyclic ring or a heterocyclic ring (e.g., oxetane); or R1 and R2 are linked to form a 3-8 membered carbocyclic or heterocyclic ring (e.g., cyclopropyl, oxetane); R3 and R4 are each independently H, Me, substituted or unsubstituted C1-C5 alkyl (e.g., methoxyethylene, methylaminoethyl, aminoethyl), -R8-OR 10 (e.g., (CH2)2-O-CH3), R8-N(R 10 )(R 11 ) (e.g., (CH2)2-NH(CH3)), substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl), substituted or unsubstituted 5-7 membered heterocycle (e.g., pyrrolidine, methylpyrrolidine, piperidine) or R 20 ;or R3 and R4 are linked to form a 3-8 membered heterocyclic ring (e.g., pyrrolidine, pyrrolidone, 2-oxopyrrolidine, piperidine, morpholine, piperazine, imidazole); R5 is H or C1-C5 straight or branched chain alkyl (e.g., methyl); R6 is H, C1-C5 straight or branched alkyl (e.g., methyl, ethyl), substituted or unsubstituted, saturated or unsaturated, single, fused, bridged or spiro 3-10 membered heterocycle (e.g., piperidine, 1-methylpiperidine, 3-fluoro-1-methylpiperidine, azetidine, 1-methyl-azetidine, morpholine, pyrrolidine, pyrrolidone, quinuclidine, tetrahydropyran, tetrahydrofuran, azaspiro[3.3]heptane, 8-methyl-8-azabicyclo[3.2.1]octane, dioxane, 1,3-dioxane, imidazole, trifluoromethyl-oxetane, hydroxy-tetrahydrofuran, azepan-2-one, azabicyclohexane), or (CH2)3-4-fluoro-piperidine; R7' and R7" are each independently H, F, Cl, Br, I, OH, OR 20 ,SH,R8-OH,R8-SH,-R8-OR 10 、R8-(C3-C8 cycloalkyl), R8-(3-8 membered heterocycle), CF3, CD3, OCD3, CN, NO2, -CH2CN, -R8CN, NH2, NHR, N(R)2, NH(R 10 )、N(R 10 )(R 11 )、R8-N(R 10 )(R 11 )、R9-R8-N(R 10 )(R 11 ), B(OH)2, -OC(O)CF3, -OCH2Ph, NHC(O)-R 10 、NHCO-N(R 10 )(R 11 )、COOH、-C(O)Ph、C(O)OR 10 、R8-C(O)-R 10 、C(O)H、C(O)-R 10 、C1-C5 straight chain or branched C(O)-haloalkyl、-C(O)NH2、C(O)NHR、C(O)N(R 10 )(R 11 )、SO2R、SO2N(R 10 )(R 11 )、CH(CF3)(NH-R 10 ), C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., isopropyl, methyl, ethyl), C1-C5 straight chain or branched, substituted or unsubstituted alkenyl, C1-C5 straight chain or branched or C3-C8 cyclic haloalkyl (e.g., CHF2), C1-C5 straight chain or branched or C3-C8 cyclic alkoxy (e.g., methoxy), optionally wherein at least one methylene (CH2) in the alkoxy is replaced by an oxygen atom, C1-C5 straight chain or branched thioalkoxy ... -C5 straight chain or branched haloalkoxy, C1-C5 straight chain or branched alkoxyalkyl, substituted or unsubstituted C3-C8 cycloalkyl (e.g., cyclopropyl, cyclohexyl), substituted or unsubstituted 3-8 membered heterocycle (e.g., morpholine, pyran, oxetane, pyrrolidine, 3,3-difluoropyrrolidine, imidazole, pyrazole, triazole, piperazine, piperidine, piperidin-2-one, piperidin-4-ol, dioxazole, 2-oxopyrrolidine), substituted or unsubstituted aryl, substituted or unsubstituted benzyl; or R7′ and R7″ are connected to form a 3-8 membered substituted or unsubstituted, saturated, unsaturated or aromatic carbocyclic or heterocyclic ring (e.g., cyclopentyl, cyclohexyl, piperidine, tetrahydrofuran, tetrahydropyran, pyrrolidine); R 20 Represented by the following structure: R is H, F, Cl, Br, I, OH, SH, alkoxy, NH(R 10 ), NH-CH2-cyclopropyl, N(R 10 )(R 11 ), CF3, CN, NO2, COOH, C1-C5 straight or branched, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH2-OH, CH2-CH2-OH, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C3-C8 substituted or unsubstituted cycloalkyl, cyclopropyl, C1-C5 straight or branched alkoxy, isopropoxy, C1-C5 straight or branched haloalkyl (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 、-R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl (e.g., phenyl), substituted or unsubstituted heteroaryl (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine)); R 30 It is H, R 20 ,F,Cl,Br,I,OH,SH,alkoxy,N(R)2,NH(R 10 )、N(R 10 )(R 11 ), CF3, CN, NO2, C1-C5 straight chain or branched, substituted or unsubstituted alkyl (e.g., methyl, ethyl, CH2-CH2-O-CH2-CH2-O-CH3, CH2-O-CH2-CH2-O-CH3), C1-C5 straight chain or branched alkoxy, C1-C5 straight chain or branched haloalkyl (e.g., CHF2, CF3, CF2CH3, CH2CF3, CF2CH2CH3, CH2CH2CF3, CF2CH(CH3)2, CF(CH3)-CH(CH3)2), R8-aryl (e.g., CH2-Ph), -R8-O-R8-OR 10 (e.g., (CH2)2-O-(CH2)2-O-CH3), -R8-OR 10 、-R8-R 10 (e.g., (CH2)2-O-CH3), substituted or unsubstituted aryl (e.g., phenyl), substituted or unsubstituted heteroaryl (e.g., pyridine (2-pyridine, 3-pyridine and 4-pyridine)); Each R8 is independently [CH2] p Where p is between 1 and 10; R9 is [CH] q , [C] q Where q is between 2 and 10; R 10 and R 11 are each independently H, C1-C5 substituted or unsubstituted straight or branched alkyl (e.g., methyl, ethyl, CH2-cyclopropyl, CH2-CH2-O-CH3), C1-C5 substituted or unsubstituted straight or branched haloalkyl (e.g., CH2CF3), C1-C5 straight or branched alkoxy (e.g., O-CH3), R 20 , C(O)R or S(O)2R; or R 10 and R 11 connected to form a substituted or unsubstituted 3-8 membered heterocyclic ring (eg, piperazine, piperidine), n is an integer between 0 and 4 (eg, 1, 2); or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., a deuterated analog), PROTAC, drug product, or any combination thereof.

11. The compound according to claim 10, wherein R1 is H; R2 is a substituted C1-C5 alkyl group (e.g., CH2OH, CH2OCH3), or a 3-8 membered heterocycle (e.g., Oxetane); R3 and R4 are each independently H; R5 is H or C1-C5 straight or branched chain alkyl (e.g., methyl); R6 is C1-C5 straight or branched alkyl (e.g., methyl, ethyl), (CH2)3-4-fluoro-piperidine or tetrahydropyran; R7' is F; R7” is H; n is 1; or any combination thereof.

12. The compound according to claim 10 or 11, wherein the compound is represented by the structure of any one of the following compounds:

13. A compound represented by the structure of any one of the following compounds: or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, N-oxide, reverse amide analog, prodrug, isotopic variant (e.g., a deuterated analog), PROTAC, drug product, or any combination thereof.

14. The compound according to any one of claims 1 to 13, wherein the compound is a c-MYC mRNA translation regulator, a c-MYC mRNA transcription regulator, a c-MYC inhibitor, or any combination thereof.

15. A pharmaceutical composition comprising a compound according to any one of claims 1 to 14 and a pharmaceutically acceptable carrier.

16. A compound according to any one of claims 1 to 14 or a pharmaceutical composition according to claim 15, for use in treating cancer in a subject, suppressing cancer in a subject, reducing the severity of cancer in a subject, reducing the risk of a subject developing cancer, or inhibiting cancer in a subject.

17. The compound according to claim 16, wherein the cancer is selected from the following list: breast cancer, ovarian cancer, acute myeloid leukemia, chronic myeloid leukemia, Hodgkin's and 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, BRAF V600E thyroid cancer, choroid plexus carcinoma, colitis-associated cancer, epithelial ovarian cancer, colorectal cancer, pancreatic cancer, and uterine cancer; wherein the cancer is an early stage cancer, an advanced stage cancer, an invasive cancer, a metastatic cancer, a drug-resistant cancer, or any combination thereof; wherein the subject has been previously treated with chemotherapy, immunotherapy, radiation therapy, biological therapy, surgical intervention, or any combination thereof; wherein the compound is administered in combination with an anti-cancer therapy; or any combination thereof.

18. The compound of claim 17, wherein the anti-cancer therapy is chemotherapy, immunotherapy, radiotherapy, biological therapy, surgical intervention, or any combination thereof.

19. The compound according to any one of claims 1 to 14 or the pharmaceutical composition according to claim 15, for use in suppressing, reducing or inhibiting tumor growth in a subject.

20. A method for regulating c-MYC mRNA translation in a cell or regulating c-MYC mRNA transcription in a cell, the method comprising contacting a compound according to any one of claims 1 to 14 with a cell, thereby regulating c-MYC mRNA translation in the cell or regulating c-MYC mRNA transcription in the cell.

21. The method according to claim 20, wherein the method is carried out as follows: (a) by regulating c-MYC mRNA splicing (inclusion or exclusion of untranslated regions or alternative usage of exons); (b) by regulating c-MYC mRNA modification; (c) by modulating the interaction of RNA binding proteins with c-MYC mRNA, thereby altering mRNA localization; (d) by regulating c-MYC mRNA localization in the cytoplasm; (e) by regulating ribosomes or ribosomal cofactors of c-MYC mRNA; (f) by reducing the amount of c-MYC protein in the cell; or any combination thereof.

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