Compositions and methods for the treatment of CNS disorders

Abstract

To provide methods for treating diseases.SOLUTION: Provided herein is a compound of Formula (I-I) or a pharmaceutically acceptable salt thereof, where in the formula (I-I), R7, R3, R9, R6a, R6b, R11a, R11b, R15a, R15b, R16a, R16b, R17a, R17b, R18a, R18b, R19a, R19b, R5a, R5b, R8, and R13 are as defined in the disclosure. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I), and methods of using the compounds, e.g., in the treatment of CNS related disorders. Provided is a compound designed to act as a GABA regulator in the disclosure. In some embodiments, the compound is expected to be useful as a therapeutic agent for treating CNS related disorders.SELECTED DRAWING: None

Description

[Technical field]

[0001] CITED RELATED APPLICATIONS This application is a joint venture of U.S. Provisional Patent Application No. 62 / 610,067 (filed December 22, 2017), No. 62 / 611,977 (filed on December 29, 2017), No. 62 / 765,16 No. 4 (filed on August 17, 2018), No. 62 / 612,067 (December 2, 2017) 9, 62 / 728,499 (filed September 7, 2018), 62 / 75 No. 4,977 (filed on November 2, 2018), No. 62 / 612,070 (filed on November 2, 2017) No. 62 / 612,164 (filed on December 29, 2017), No. 62 / 612,164 (filed on December 29, 2017), This application claims priority from Application No. 62 / 737,559 (filed September 27, 2018). The entirety of which is incorporated herein by reference. [Background technology]

[0002] 2. Background of the Invention Brain excitability is defined as the level of alertness of an animal on a continuum ranging from coma to seizures, and can vary In general, neurotransmitters cross the neuronal membrane. At rest, the neuronal membrane is at approximately -70 The cell has a potential (or membrane voltage) of 100 mV, with the inside of the cell being negative relative to the outside of the cell. (voltage) is the force of ions (K + , Na + , Cl - , organic anion Neurotransmitters are stored in presynaptic vesicles and mediate neuronal activity. It is released under the influence of a dynamic potential. When released into the synaptic cleft, it is released at potentials between -70mV and -5 This action causes a change in potential to 0 mV. +A to increase membrane permeability to ions Mediated by postsynaptic nicotinic receptors stimulated by cetylcholine. Low The lowered membrane potential stimulates neuronal excitability in the form of postsynaptic action potentials.

[0003] In the case of the GABA receptor complex (GRC), its effect on brain excitability is mediated by the neurotransmitter It is mediated by the substance gamma-aminobutyric acid (GABA), which is secreted by up to 40% of neurons in the brain. However, since it uses GABA as a neurotransmitter, GABA has a significant effect on the excitability of the entire brain. GABA has a significant effect on the conductance of chloride ions across neuronal membranes. GABA regulates the excitability of individual neurons by regulating the By interacting with the recognition site, chloride ions are transported down the electrochemical gradient of the GRC. This increase in the intracellular level of this anion promotes the overshoot of the transmembrane potential. It causes polarization and decreases the sensitivity of neurons to excitatory inputs (i.e., In other words, the higher the chloride ion concentration in the neuron, the , brain excitability and alertness levels decrease.

[0004] The GRC is well-documented to be involved in mediating anxiety, seizure activity, and sedation. GABA and drugs that act like GABA or enhance the effects of GABA substances (e.g., therapeutically useful barbiturates and benzodiazepines (BZ), e.g., Valium® inhibits the GABAergic receptor by interacting with specific regulatory sites on the GRC. Accumulating evidence currently supports the notion that GRC is a benzodiazepine that exerts its therapeutically beneficial effects. In addition to the azepine and barbiturate binding sites, there is a separate site for neuroactive steroids. It has been suggested that the ribosome contains a site. For example, Lan, NC et al., Neurochem. See s. (1991) 16:347-356.

[0005] Neuroactive steroids can occur endogenously. The most potent endogenous neuroactive steroids 3α-hydroxy-5-reduced pregnan-20-one and 3α-21-dihydro 5-reduced oxy-5-pregnan-20-one (progesterone, These steroids are metabolites of gesterone and deoxycorticosterone. The ability of metabolites to alter brain excitability was recognized in 1986 (Majewska, Harris, MD et al., Science 232:1004-1007 (1986); on, NL et al., J Pharmacol. Exp. Ther. 241:346-35 3(1987)). Regulators of brain excitability and agents for the prevention and treatment of CNS-related diseases There is a need for new and improved compounds that act as The disclosed compounds, compositions and methods are directed to this end. [Prior art documents] [Non-patent literature]

[0006] [Non-Patent Document 1] Lan, N.C. et al., Neurochem. Res. (1991) 16:347-356 [Non-Patent Document 2] Majewska, MD et al., Science 232:1004-1007(1986) [Non-Patent Document 3] Harrison, N.L. et al., J Pharmacol. Exp. Ther. 241:346-353 (1987) Summary of the Invention [Means for solving the problem]

[0007] Provided herein are compounds designed to act as GABA modulators. In some embodiments, such compounds are useful as therapeutic agents for treating CNS-related disorders. It is assumed that.

[0008] In one aspect, the present specification provides a compound of formula (II): [ka] or a pharma- ceutically acceptable salt thereof.

[0009] In some embodiments, the compound has the formula (I-Ia): [ka] or a pharma- ceutically acceptable salt thereof.

[0010] In some embodiments, the compound has the formula (I-Iab): [ka] or a pharma- ceutically acceptable salt thereof.

[0011] In some embodiments, the compound has formula (I-Ib) or formula (I-Ibb): [ka] or a pharma- ceutically acceptable salt thereof.

[0012] In some embodiments, the compound has formula (I-Ic) or formula (I-Icb) [ka] or a pharma- ceutically acceptable salt thereof. In some embodiments, the compound has formula (I-Id) or formula (I-Idb): [ka] or a pharma- ceutically acceptable salt thereof. In some embodiments, the compound has formula (I-Ie) or formula (I-Ieb) [ka] or a pharma- ceutically acceptable salt thereof. In some embodiments, the compound has formula (I-If) or formula (I-Ifb): [ka] or a pharma- ceutically acceptable salt thereof. In some embodiments, the compound has formula (I-Ig) or formula (I-Igb): [ka] or a pharma- ceutically acceptable salt thereof. In some embodiments, the compound has formula (I-Ih) or formula (I-Ihb): [ka] or a pharma- ceutically acceptable salt thereof. In some embodiments, the compound has formula (I-Ii) or formula (I-Iib) [ka] or a pharma- ceutically acceptable salt thereof. In some embodiments, the compound has the formula (I-Ik) or the formula (I-Ikb) [ka] or a pharma- ceutically acceptable salt thereof. In one aspect, the present specification provides a compound represented by formula (I-II): [ka] or a pharma- ceutically acceptable salt thereof.

[0013] In some embodiments, the compound has formula (I-IIa) or formula (I-IIab) [ka] or a pharma- ceutically acceptable salt thereof.

[0014] In some embodiments, the compound has formula (I-IIb) or formula (I-IIbb) [ka] or a pharma- ceutically acceptable salt thereof.

[0015] In some embodiments, the compound has formula (I-IId) or formula (I-IIdb) [ka] or a pharma- ceutically acceptable salt thereof.

[0016] In some embodiments, the compound has formula (I-IIe) or formula (I-IIeb) [ka] or a pharma- ceutically acceptable salt thereof.

[0017] In some embodiments, the compound has formula (I-IIf) or formula (I-IIfb): [ka] or a pharma- ceutically acceptable salt thereof.

[0018] In some embodiments, the compound has formula (I-IIg) or formula (I-IIgb) [ka] or a pharma- ceutically acceptable salt thereof.

[0019] In some embodiments, the compound has formula (I-IIh) or formula (I-IIhb) [ka] or a pharma- ceutically acceptable salt thereof.

[0020] In some embodiments, the compound has formula (I-IIi) or formula (I-IIib) [ka] or a pharma- ceutically acceptable salt thereof.

[0021] In some embodiments, the compound has the formula (I-IIj): [ka] or a pharma- ceutically acceptable salt thereof.

[0022] In one aspect, the present specification provides a compound represented by formula (II-I): [ka] or a pharma- ceutically acceptable salt thereof.

[0023] In some embodiments, the compound has the formula (II-II): [ka] or a pharma- ceutically acceptable salt thereof.

[0024] In some embodiments, the compound has formula (II-Ia), (II-Iab) or (II- Iac) [ka] or a pharma- ceutically acceptable salt thereof.

[0025] In some embodiments, the compound has formula (II-Ib), (II-Ibb) or (II- Ibc) [ka] or a pharma- ceutically acceptable salt thereof.

[0026] In some embodiments, the compound has formula (II-Ic), (II-Icb), or (II- Icc) [ka] or a pharma- ceutically acceptable salt thereof.

[0027] In some embodiments, the compound has formula (II-Ie), (II-Ieb), or (II- Iec) [ka] or a pharma- ceutically acceptable salt thereof.

[0028] In some embodiments, the compound has formula (II-Ig), (II-Igb), or (II- Igc) [ka] or a pharma- ceutically acceptable salt thereof.

[0029] In some embodiments, the compound has the formula (II-Ieg), (II-Iegb), or (II I-Iegc) [ka] or a pharma- ceutically acceptable salt thereof.

[0030] In some embodiments, the compound has the formula (II-Ih), (II-Ihb), or (II- IHC) [ka] or a pharma- ceutically acceptable salt thereof.

[0031] In some embodiments, the compound has formula (II-Ii), (II-Iib) or (II- Iic) [ka] or a pharma- ceutically acceptable salt thereof.

[0032] In some embodiments, the compound has formula (II-IIa) or (II-IIab) [ka] or a pharma- ceutically acceptable salt thereof.

[0033] In some embodiments, the compound has formula (II-IIb) or (II-IIbb) [ka] or a pharma- ceutically acceptable salt thereof.

[0034] In some embodiments, the compound has formula (II-IIc) or (II-IIcb) [ka] or a pharma- ceutically acceptable salt thereof.

[0035] In some embodiments, the compound has formula (II-IIe) or (II-IIeb) [ka] or a pharma- ceutically acceptable salt thereof.

[0036] In some embodiments, the compound has formula (II-IIg) or (II-IIgb): [ka] or a pharma- ceutically acceptable salt thereof.

[0037] In some embodiments, the compound has the formula (II-IIh) or (II-IIhb): [ka] or a pharma- ceutically acceptable salt thereof.

[0038] In some embodiments, the compound has formula (II-IIi) or (II-IIib) [ka] or a pharma- ceutically acceptable salt thereof.

[0039] In one aspect, the present specification provides a compound represented by formula (III-I): [ka] or a pharma- ceutically acceptable salt thereof.

[0040] In some embodiments, the compound has formula (III-Ia): [ka] or a pharma- ceutically acceptable salt thereof.

[0041] In some embodiments, the compound has formula (III-Ib): [ka] or a pharma- ceutically acceptable salt thereof.

[0042] In some embodiments, the compound has formula (III-Ic): [ka] or a pharma- ceutically acceptable salt thereof.

[0043] In some embodiments, the compound has formula (III-Id): [ka] or a pharma- ceutically acceptable salt thereof.

[0044] In some embodiments, the compound has formula (III-Ie): [ka] or a pharma- ceutically acceptable salt thereof.

[0045] In some embodiments, the compound has formula (III-If): [ka] or a pharma- ceutically acceptable salt thereof.

[0046] In some embodiments, the compound has formula (III-Ig): [ka] or a pharma- ceutically acceptable salt thereof.

[0047] In some embodiments, the compound has formula (III-Ih): [ka] or a pharma- ceutically acceptable salt thereof.

[0048] In some embodiments, the compound has formula (III-Ii): [ka] or a pharma- ceutically acceptable salt thereof.

[0049] In some embodiments, the compound has formula (III-Ij): [ka] or a pharma- ceutically acceptable salt thereof.

[0050] In some embodiments, the compound has formula (III-Ik): [ka] or a pharma- ceutically acceptable salt thereof.

[0051] In some embodiments, the compound has formula (III-IL): [ka] or a pharma- ceutically acceptable salt thereof.

[0052] In some embodiments, the compound has the formula (III-Im): [ka] or a pharma- ceutically acceptable salt thereof.

[0053] In some embodiments, the compound has formula (III-In) or formula (III-Io) [ka] or a pharma- ceutically acceptable salt thereof.

[0054] In one aspect, the present specification provides a compound represented by formula (III-II): [ka] or a pharma- ceutically acceptable salt thereof.

[0055] In some embodiments, the compound has the formula (III-IIa): [ka] or a pharma- ceutically acceptable salt thereof.

[0056] In some embodiments, the compound has the formula (III-IIb): [ka] or a pharma- ceutically acceptable salt thereof.

[0057] In some embodiments, the compound has the formula (III-IIc): [ka] or a pharma- ceutically acceptable salt thereof.

[0058] In some embodiments, the compound has the formula (III-IId): [ka] or a pharma- ceutically acceptable salt thereof.

[0059] In some embodiments, the compound has the formula (III-IIe): [ka] or a pharma- ceutically acceptable salt thereof.

[0060] In some embodiments, the compound has the formula (III-IIf): [ka] or a pharma- ceutically acceptable salt thereof.

[0061] In some embodiments, the compound has the formula (III-IIg): [ka] or a pharma- ceutically acceptable salt thereof.

[0062] In some embodiments, the compound has the formula (III-IIh): [ka] or a pharma- ceutically acceptable salt thereof.

[0063] In some embodiments, the compound has formula (III-IIi): [ka] or a pharma- ceutically acceptable salt thereof.

[0064] In some embodiments, the compound has the formula (III-IIj): [ka] or a pharma- ceutically acceptable salt thereof.

[0065] In some embodiments, the compound has the formula (III-IIk): [ka] or a pharma- ceutically acceptable salt thereof.

[0066] In some embodiments, the compound has the formula (III-IIL): [ka] or a pharma- ceutically acceptable salt thereof.

[0067] In some embodiments, the compound has the formula (III-IIm): [ka] or a pharma- ceutically acceptable salt thereof.

[0068] In some embodiments, the compound has formula (III-IIn) or formula (III-IIo) [ka] or a pharma- ceutically acceptable salt thereof.

[0069] In one aspect, the present specification provides a compound represented by formula (IV-I): [ka] or a pharma- ceutically acceptable salt thereof.

[0070] In some embodiments, the compound has formula (IV-Ia): [ka] or a pharma- ceutically acceptable salt thereof.

[0071] In some embodiments, the compound has formula (IV-Ib): [ka] or a pharma- ceutically acceptable salt thereof.

[0072] In some embodiments, the compound has formula (IV-Ic): [ka] or a pharma- ceutically acceptable salt thereof

[0073] In some embodiments, the formula (IV-Id) [ka] or a pharma- ceutically acceptable salt thereof.

[0074] In some embodiments, the compound has formula (IV-Ie): [ka] or a pharma- ceutically acceptable salt thereof.

[0075] In some embodiments, the compound of formula (IV-I) has the formula (IV-If): [ka] or a pharma- ceutically acceptable salt thereof.

[0076] In some embodiments, the compound of formula (IV-I) has the formula (IV-Ig): [ka] or a pharma- ceutically acceptable salt thereof.

[0077] In some embodiments, the compound has formula (IV-Ih): [ka] or a pharma- ceutically acceptable salt thereof.

[0078] In some embodiments, the compound has formula (IV-Ii): [ka] or a pharma- ceutically acceptable salt thereof.

[0079] In some embodiments, the compound has formula (IV-Ij): [ka] or a pharma- ceutically acceptable salt thereof.

[0080] In some embodiments, the compound has the formula (IV-Ik): [ka] or a pharma- ceutically acceptable salt thereof.

[0081] In some embodiments, the compound has formula (IV-IL): [ka] or a pharma- ceutically acceptable salt thereof.

[0082] In some embodiments, the compound has the formula (IV-Im): [ka] or a pharma- ceutically acceptable salt thereof.

[0083] In some embodiments, the compound has formula (IV-In) or formula (IV-Io) [ka] or a pharma- ceutically acceptable salt thereof.

[0084] In one aspect, the compound of formula (IV-II): [ka] Provided herein are compounds of the formula:

[0085] In some embodiments, the compound has the formula (IV-IIa): [ka] or a pharma- ceutically acceptable salt thereof.

[0086] In some embodiments, the compound has formula (IV-IIb): [ka] or a pharma- ceutically acceptable salt thereof.

[0087] In some embodiments, the compound has the formula (IV-IIc): [ka] or a pharma- ceutically acceptable salt thereof.

[0088] In some embodiments, the compound has the formula (IV-IId): [ka] or a pharma- ceutically acceptable salt thereof.

[0089] In some embodiments, the compound has the formula (IV-IIe): [ka] or a pharma- ceutically acceptable salt thereof.

[0090] In some embodiments, the compound has formula (IV-IIf): [ka] or a pharma- ceutically acceptable salt thereof.

[0091] In some embodiments, the compound has the formula (IV-IIg): [ka] or a pharma- ceutically acceptable salt thereof.

[0092] In some embodiments, the compound has formula (IV-IIh): [ka] or a pharma- ceutically acceptable salt thereof.

[0093] In some embodiments, the compound has formula (IV-IIi): [ka] or a pharma- ceutically acceptable salt thereof.

[0094] In some embodiments, the compound has the formula (IV-IIj): [ka] or a pharma- ceutically acceptable salt thereof.

[0095] In some embodiments, the compound has the formula (IV-IIk): [ka] or a pharma- ceutically acceptable salt thereof.

[0096] In some embodiments, the compound has the formula (IV-IIL): [ka] or a pharma- ceutically acceptable salt thereof.

[0097] In some embodiments, the compound has the formula (IV-IIm): [ka] or a pharma- ceutically acceptable salt thereof.

[0098] In some embodiments, the compound has formula (IV-IIn) or formula (IV-IIo) [ka] or a pharma- ceutically acceptable salt thereof.

[0099] In one aspect, the compound of formula (IV-III) [ka] or a pharma- ceutically acceptable salt thereof.

[0100] In one aspect, the present specification provides a compound represented by formula (VI): [ka] or a pharma- ceutically acceptable salt thereof.

[0101] In some embodiments, the compound has formula (V-Ia): [ka] or a pharma- ceutically acceptable salt thereof.

[0102] In some embodiments, the compound has formula (V-Ib): [ka] or a pharma- ceutically acceptable salt thereof.

[0103] In some embodiments, the compound has formula (V-Ic): [ka] or a pharma- ceutically acceptable salt thereof.

[0104] In some embodiments, the compound has formula (V-Id): [ka] or a pharma- ceutically acceptable salt thereof.

[0105] In some embodiments, the compound has formula (V-Ie): [ka] or a pharma- ceutically acceptable salt thereof.

[0106] In some embodiments, the compound has the formula (V-If): [ka] or a pharma- ceutically acceptable salt thereof.

[0107] In some embodiments, the compound has the formula (V-Ig): [ka] or a pharma- ceutically acceptable salt thereof.

[0108] In some embodiments, the compound has formula (V-Ih): [ka] or a pharma- ceutically acceptable salt thereof.

[0109] In some embodiments, the compound has formula (V-Ii): [ka] or a pharma- ceutically acceptable salt thereof.

[0110] In some embodiments, the compound has formula (V-Ij): [ka] or a pharma- ceutically acceptable salt thereof.

[0111] In some embodiments, the compound has the formula (V-Ik): [ka] or a pharma- ceutically acceptable salt thereof.

[0112] In some embodiments, the compound has the formula (V-IL): [ka] or a pharma- ceutically acceptable salt thereof.

[0113] In some embodiments, the compound has the formula (V-Im): [ka] or a pharma- ceutically acceptable salt thereof.

[0114] In some embodiments, the compound has the formula (V-In) or the formula (V-Io): [ka] or a pharma- ceutically acceptable salt thereof.

[0115] In one aspect, the present specification provides a compound represented by formula (V-II): [ka] or a pharma- ceutically acceptable salt thereof.

[0116] In some embodiments, the compound has formula (V-IIa): [ka] or a pharma- ceutically acceptable salt thereof.

[0117] In some embodiments, the compound has formula (V-IIb): [ka] or a pharma- ceutically acceptable salt thereof.

[0118] In some embodiments, the compound has formula (V-IIc): [ka] or a pharma- ceutically acceptable salt thereof.

[0119] In some embodiments, the compound has formula (V-IId): [ka] or a pharma- ceutically acceptable salt thereof.

[0120] In some embodiments, the compound has formula (V-IIe): [ka] or a pharma- ceutically acceptable salt thereof.

[0121] In some embodiments, the compound has the formula (V-IIf): [ka] or a pharma- ceutically acceptable salt thereof.

[0122] In some embodiments, the compound has formula (V-IIg): [ka] or a pharma- ceutically acceptable salt thereof.

[0123] In some embodiments, the compound has formula (V-IIh): [ka] or a pharma- ceutically acceptable salt thereof.

[0124] In some embodiments, the compound has formula (V-IIi): [ka] or a pharma- ceutically acceptable salt thereof.

[0125] In some embodiments, the compound has formula (V-IIj): [ka] or a pharma- ceutically acceptable salt thereof.

[0126] In some embodiments, the compound has formula (V-IIk): [ka] or a pharma- ceutically acceptable salt thereof.

[0127] In some embodiments, the compound has the formula (V-IIL): [ka] or a pharma- ceutically acceptable salt thereof.

[0128] In some embodiments, the compound has the formula (V-IIm): [ka] or a pharma- ceutically acceptable salt thereof.

[0129] In some embodiments, the compound has formula (V-IIn) or formula (V-IIo) [ka] or a pharma- ceutically acceptable salt thereof.

[0130] In one aspect, the compound of formula (V-III) [ka] or a pharma- ceutically acceptable salt thereof.

[0131] In some embodiments, the pharmaceutical composition comprises a compound as described herein or a pharma- ceutically acceptable salt thereof, and a pharma- ceutically acceptable salt thereof. Add to Contains agents.

[0132] In some embodiments, the present invention relates to a method for treating a CNS-related disorder in a subject in need of such treatment. The present invention relates to a method for treating an adverse event, the method comprising administering to a subject an effective amount of a compound described herein or a pharmaceutical formulation thereof. In some embodiments, a method is provided herein comprising administering a physiologically acceptable salt thereof to a subject. So, CNS-related disorders are sleep disorders, mood disorders, schizophrenia spectrum disorders, and seizure disorders. , memory and / or cognitive impairment, movement disorders, personality disorders, autism spectrum disorders, pain pain, traumatic brain injury, vascular disease, substance abuse disorders and / or withdrawal syndromes, tinnitus, or In some embodiments, the CNS-related disorder is depression. In some embodiments, the CNS-related disorder is postpartum depression. In some embodiments, the major depressive disorder is a moderate major depressive disorder. In some embodiments, the major depressive disorder is a severe major depressive disorder. be.

[0133] In some embodiments, the compound is selected from the group consisting of compounds listed in Tables I-1, I-2, I-3, I-4, I-5, I-6, I-7, I-8, I-9, I-10, I-11, I-12, I-13, I-14, I-15, I-16, I-17, I-18, I-19, I-20, I-21, I-22, I-23, I-2 -1, the compounds specified in Table III-1, Table IV-1, and Table V-1. do.

[0134] In one aspect, the compounds described herein (e.g., Formula (II), Formula (II I), formula (II-I), formula (II-II), formula (III-I), formula (III-II), formula (IV-I), formula (IV-II), formula (IV-III), formula (VI), formula (V-II) or a pharma- ceutically acceptable salt of a compound of formula (V-III) is provided herein.

[0135] In one aspect, a compound described herein (e.g., a compound of formula (II), formula (I-II), formula (II-I), formula (II-II), formula (III-I), formula (III-II), formula (IV-I), formula (IV-II), formula (IV-III), formula (VI), formula (V-II), or formula (V-III) or a pharma- ceutically acceptable salt thereof, and a pharma- ceutically acceptable salt thereof, Add to Provided herein is a pharmaceutical composition comprising an agent. In certain embodiments, the compound of the present invention is provided in an effective amount in the pharmaceutical composition. In certain embodiments, the compound of the present invention is provided in a therapeutically effective amount. In certain embodiments, the compound of the present invention is provided in a prophylactically effective amount.

[0136] The compounds of the invention as described herein may, in certain embodiments, be GABA A GABA modulation effects receptors in a positive or negative manner Such compounds act as GABA receptor antagonists. A By its ability to regulate receptors As regulators of central nervous system (CNS) excitability, such as that mediated by It is expected that. Thus, in another aspect, in a subject in need of treatment for a CNS-related disorder, A method of treating an S-related disorder is provided, the method comprising administering to the subject an effective amount of a compound of the invention. In certain embodiments, the CNS-related disorder is a sleep disorder. Disorders, mood disorders, schizophrenia spectrum disorders, seizure disorders, memory and / or cognitive disorders injury, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular disease, The symptoms of these conditions include substance abuse disorder and / or withdrawal syndrome, tinnitus, or status epilepticus. In certain embodiments, the CNS-related disorder is depression. In certain embodiments, the CNS-related disorder is postpartum depression. is major depressive disorder. In certain embodiments, major depressive disorder is moderate In certain embodiments, the major depressive disorder is a severe major depressive disorder. In certain embodiments, the compound is administered orally, subcutaneously, intravenously, or intravenously. In certain embodiments, the compound is administered orally. In certain embodiments, the compound is administered chronically. The compounds may be administered continuously, for example, by continuous intravenous infusion. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0137] Detailed Description of Specific Embodiments of the Invention As generally described herein, the present invention relates to compounds that are useful, for example, as GABA modulators. In certain embodiments, such compounds are provided. The subject may be a patient suffering from a CNS-related disorder (e.g., a disorder described herein, e.g., postpartum depression or major aspiration). It is expected that these compounds will be useful as therapeutic agents for treating depression, including depression and depression disorders. definition chemical definition

[0138] Definitions of certain functional groups and chemical terms are explained in detail below. Chemical elements are classified into the Periodic Table Table (CAS version, Handbook of Chemistry and Phys SICS, 75th Edition, inside cover), and specific functional groups are generally In addition, the general rules of organic chemistry and specific functional moieties are defined as follows: and reactivity, Thomas Sorrell, Organic Chemistry ,University Science Books,Sausalito,1999 Smith and March, March's Advanced Organic Chemistry, 5th Edition, John Wiley & Sons, Inc., New York,2001;Larock,Comprehensive Organic Transformations,VCH Publishers,Inc.,New York, 1989; and Carruthers, Some Modern Methods. ods of organic synthesis, 3rd ed., Cambridge University University Press, Cambridge, 1987.

[0139] Isomers (e.g., stereoisomers) can be separated by methods known to those skilled in the art, such as chiral high pressure liquid chromatography. Can they be isolated from the mixture by chemical methods (including HPLC as well as the formation of chiral salts)? or the preferred isomer can be prepared by asymmetric synthesis. For example, Jacques et al. , Enantiomers, Racemates and Resolutions(W iley Interscience, New York, 1981);Wilen et al. Tetrahedron 33:2725(1977); Eliel, Stereoch emissions of Carbon Compounds(McGraw-Hill, NY, 1962); and Wilen, Tables of Resolving Ag ents and Optical Resolutions p.268(ELE liel editor, Univ. of Notre Dame Press, Notre Da me, IN 1972. The present invention further relates to compounds as described herein. as individual isomers substantially free of other isomers, and / or as various isomeric As a mixture, includes.

[0140] "Stereoisomers": Two or more isomers that have the same molecular formula but differ in the nature or sequence of bonds of their atoms or in space. It should also be understood that compounds that differ in the arrangement of atoms in the molecule are referred to as "isomers." Isomers that differ in the arrangement of their atoms in space are called "stereoisomers." Stereoisomers that are not For example, if a compound has an asymmetric center, it is called an "enantiomer." If it has a core, it is bonded to four different groups, allowing a pair of enantiomers. Enantiomers can be characterized by the absolute configuration of their asymmetric center and Either the molecule is represented by the R and S ordering rules of Hoffman and Prelog, or the molecule is It is represented by the way in which the plane of polarized light is rotated, and is called dextrorotatory or levorotatory (i.e., respectively). Chiral compounds are represented as individual enantiomers. It can exist either as an enantiomeric form or as a mixture thereof. A mixture containing a mer is called a "racemic mixture."

[0141] As used herein, an enantiomerically pure compound refers to a compound that is a mixture of the other enantiomer of the compound. Substantially free of isomers or stereoisomers (i.e., enantiomeric excess). In other words, the "S" form of the compound is substantially free of the "R" form of the compound, and therefore the "R" form of the compound is The term "enantiomerically pure" or "pure enantiomers" "-" means that the compound is more than 75% by weight, more than 80% by weight, more than 85% by weight, more than 90% by weight, more than 91% by weight, More than 92% by weight, more than 93% by weight, more than 94% by weight, more than 95% by weight, more than 96% by weight, More than 97% by weight, more than 98% by weight, more than 98.5% by weight, more than 99% by weight, more than 99.2% by weight, 9 More than 9.5% by weight, more than 99.6% by weight, more than 99.7% by weight, more than 99.8% by weight or more than 99. It means that the mixture contains more than 9% by weight of an enantiomer. In certain embodiments, the weight is: Based on the total weight of all enantiomers or stereoisomers of a compound.

[0142] As used herein, the term "diastereomeric purity" refers to the degree to which the indicated compound and Compounds with the indicated absolute stereochemistry expressed as a percentage of the total amount of diastereomers The term "diastereomerically pure" refers to a compound that is greater than 75% by weight. %, more than 80% by weight, more than 85% by weight, more than 90% by weight, more than 91% by weight 92% by weight or more, 93% by weight or more, 94% by weight or more, 95% by weight or more More than 96% by weight, more than 97% by weight, more than 98% by weight, 98.5% by weight More than, more than 99% by weight, more than 99.2% by weight, more than 99.5% by weight, 99 More than 99.6% by weight, more than 99.7% by weight, more than 99.8% by weight, or more than 99. Diastereomeric purity means that the diastereomer contains more than 9% by weight of that diastereomer. Methods for determining diastereomeric and enantiomeric purity are well known in the art. Any analytical method capable of quantitatively distinguishing between a compound and its diastereomers (high resolution, high ... This can be determined by high performance liquid chromatography (HPLC, etc.).

[0143] In the compositions provided herein, the enantiomerically pure compounds may be present together with other active or inactive ingredients. For example, a pharmaceutical composition containing an enantiomerically pure R-compound may contain, for example, about 90% Add to In certain embodiments, the enantiomerically pure R-compound in such a composition may, for example, comprise at least about 95% by weight of the R-compound and at most about 5% by weight of the S-compound, based on the total weight of the compound. For example, a pharmaceutical composition comprising an enantiomerically pure S-compound may, for example, comprise about 90% by weight of the R-compound and at most about 5% by weight of the S-compound. Add toThe active ingredient may comprise a small amount of the agent and about 10% of the enantiomerically pure S-compound. In certain embodiments, the enantiomerically pure S-compound in such a composition may comprise, for example, at least about 95% by weight of the S-compound and at most about 5% by weight of the R-compound, based on the total weight of the compound. In certain embodiments, the active ingredient may comprise a small amount of the agent and about 10% of the enantiomerically pure S-compound. In certain embodiments, the enantiomerically pure S-compound in such a composition may comprise, for example, at least about 95% by weight of the S-compound and at most about 5% by weight of the R-compound, based on the total weight of the compound. Add to may be formulated with an agent or carrier, or Add to The composition may be formulated without an agent or carrier.

[0144] The articles "a" and "an" refer to one or more grammatical objects of the article ( (i.e., at least one of). "An analogue" means one analogue or more than one analogue. It means analog.

[0145] When a range of values ​​is listed, it is intended to encompass each value and subrange within the range. For example, "C 1~6 Alkyl" is C 1 , C 2 , C 3 , C 4 , C 5 , C 6 , C 1~6 , C 1~5 , C 1~4 , C 1~3 , C 1~2 , C 2~6 , C 2~5 , C 2~4 , C 2~3 , C 3~6 , C 3~5 , C 3~4 , C 4~6 , C 4~5 , and C 5~6 Aruki This is intended to encompass all

[0146] The following terms are intended to have the meanings set forth below and are used herein as defined by the appended claims. It is helpful in understanding the specification and the intended scope of the invention.

[0147] "Alkyl" means a straight-chain or branched saturated hydrocarbon group having 1 to 20 carbon atoms. Radical ("C 1~20 In some embodiments, alkyl The group has 1 to 12 carbon atoms ("C 1~12 In some embodiments, In the above, the alkyl group has 1 to 10 carbon atoms ("C 1~10 "alkyl"). In some embodiments, an alkyl group has 1 to 9 carbon atoms ("C 1~9 a In some embodiments, the alkyl group has 1 to 8 carbon atoms (e.g., "alkyl"). "C 1~8 In some embodiments, an alkyl group is a 1 to 7 carbon atom. Has children ("C 1~7 In some embodiments, the alkyl group is selected from 1 to 2. 6 carbon atoms (also referred to herein as "lower alkyl"). 1~6 Alki In some embodiments, the alkyl group has 1 to 5 carbon atoms ("C 1~5 In some embodiments, an alkyl group contains 1 to 4 carbon atoms. ("C 1~4 In some embodiments, the alkyl group is 1 to 3 ("C 1~3 In some embodiments, the alkyl group is , having 1 to 2 carbon atoms ("C 1~2 In some embodiments, An alkyl group has one carbon atom ("C 1 In some embodiments, The alkyl group has 2 to 6 carbon atoms ("C 2~6 "Alkyl"). C 1~6 a An example of an alkyl group is methyl (C 1 ), ethyl (C 2 ), n-propyl (C 3 ), Iso Propyl (C 3 ), n-Butyl (C 4 ), tert-Butyl (C 4 ), sec-Butyl ( C 4 ), iso-butyl (C 4 ), n-pentyl (C 5 ), 3-pentanyl (C 5 ),a Mill (C 5 ), neopentyl (C 5 ), 3-methyl-2-butanyl (C 5 ), 3rd class Ami Lu (C 5 ) and n-hexyl (C 6 Further examples of alkyl groups include: , n-heptyl (C 7 ), n-octyl (C 8 ) etc. Unless otherwise specified and each occurrence of an alkyl group is independently optionally substituted, i.e., unsubstituted. ("unsubstituted alkyl") or one or more substituents; e.g., 1 to 5 substituted with one, two, three or one substituents ("substituted alkyl"); In certain embodiments, the alkyl group is an unsubstituted C 1~10 Alkyl (e.g., - CH 3 In certain embodiments, the alkyl group is a substituted C 1~10 Alkyl A common abbreviation for alkyl is Me(-CH 3 ), Et(-CH 2 CH 3 ) , iPr(-CH(CH 3) 2 ), nPr(-CH 2 CH 2 CH 3 ), n-Bu(-CH 2 CH 2 CH 2 CH 3 ), or i-Bu(-CH 2 CH(CH 3 ) 2 ) are mentioned.

[0148] "Alkylene" refers to an alkyl group in which two hydrogens have been removed to produce a divalent radical. and may be substituted or unsubstituted. Unsubstituted alkylene groups include methylene (-C H 2 -), ethylene (-CH 2 CH 2 -), propylene (-CH 2 CH 2 CH 2 -), B Chilene (-CH 2 CH 2 CH 2 CH 2 -), pentylene (-CH 2 CH 2 CH 2 CH 2 C H 2 -), and hexylene (-CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 -) are some examples. Exemplary embodiments include, but are not limited to, one or more The alkylene group substituted with an alkyl (methyl) group includes substituted methylene (-CH(CH 3 )-, (-C(CH 3 ) 2 -), substituted ethylene (-CH(CH 3 )CH 2 -, -CH 2 CH(CH 3 )-, -C(CH 3 ) 2 CH 2 -, -CH 2 C(CH 3 ) 2 -), replacement program Pyrene (-CH(CH 3 )CH 2 CH 2 -, -CH 2 CH(CH 3 )CH 2 -, -CH 2 CH 2 CH(CH 3 )-, -C(CH 3 ) 2 CH 2 CH 2 -, -CH 2 C(CH 3 ) 2 C H 2 - and -CH 2 CH 2 C(CH 3 ) 2 -) and others, but are not limited to these. When a range or number of carbons is given for a particular alkylene group, it is within the stated range. The or number is understood to refer to the range or number of carbons in a divalent linear carbon chain. , which may be substituted with one or more substituents described herein, or It may be a substitution.

[0149] "Alkenyl" means an alkyl group having 2 to 20 carbon atoms and one or more carbon atoms. -carbon double bonds (e.g., 1, 2, 3 or 4 carbon-carbon double bonds), and optionally Optionally, one or more carbon-carbon triple bonds (e.g., 1, 2, 3 or 4 A radical of a straight or branched chain hydrocarbon group containing a carbon-carbon triple bond ("C 2~2 0In certain embodiments, alkenyl refers to any In some embodiments, an alkenyl group is a 2 to 10 carbon atom. Has children ("C 2~10 In some embodiments, the alkenyl group is Having 2 to 9 carbon atoms ("C 2~9 alkenyl). Alkenyl groups have 2 to 8 carbon atoms ("C 2~8 Some fruits are In embodiments, the alkenyl group has 2 to 7 carbon atoms ("C 2~7 Arken In some embodiments, the alkenyl group has 2 to 6 carbon atoms (" C 2~6 In some embodiments, the alkenyl group is a 2 to 5 carbon atoms ("C 2~5 In some embodiments, the alkenyl group is Having 2 to 4 carbon atoms ("C 2~4 alkenyl). An alkenyl group has 2 to 3 carbon atoms ("C 2~3 Some fruits are In embodiments, the alkenyl group has two carbon atoms ("C 2 alkenyl). 1 One or more carbon-carbon double bonds may be internal (e.g., 2-butene). C may be either central (e.g., 1-butenyl) or terminal (e.g., 1-butenyl). 2~4 Examples of alkenyl groups As an example, ethenyl (C 2 ), 1-propenyl (C 3 ), 2-propenyl (C 3 ), 1- Butenyl (C 4 ), 2-butenyl (C 4 ), butadienyl (C 4) etc. 2~6 Examples of alkenyl groups include the above-mentioned C 2~4 Alkenyl groups, as well as pentenyl ( C 5 ), pentadienyl (C 5 ), hexenyl (C 6 ) and the like. Further examples include heptenyl (C 7 ), octenyl (C 8 ), octatrienyl (C 8 Unless otherwise specified, each occurrence of an alkenyl group independently represents Optionally substituted, i.e., unsubstituted ("unsubstituted alkenyl") or one or more substituents, for example, 1 to 5 substituents, 1 to 3 substituents or In certain embodiments, the alkenyl is substituted with one substituent ("substituted alkenyl"). The aryl group is an unsubstituted C 2~10 In certain embodiments, the alkene is an alkenyl. The yl group is a substituted C 2~10 It is alkenyl.

[0150] "Alkynyl" means an alkyl group having 2 to 20 carbon atoms, one or more carbon-carbon triple bonds (e.g., 1, 2, 3 or 4 carbon-carbon triple bonds), and optionally , one or more carbon-carbon double bonds (e.g., 1, 2, 3 or 4 carbon -carbon double bond) ("C 2~20 a In certain embodiments, alkenyl refers to any double aryl group. In some embodiments, an alkynyl group contains 2 to 10 carbon atoms. ("C 2~10 In some embodiments, the alkynyl group is ~9 carbon atoms ("C 2~9 In some embodiments, alkynyl is The quinyl group has 2 to 8 carbon atoms ("C 2~8 alkynyl). In certain embodiments, the alkynyl group has 2 to 7 carbon atoms ("C 2~7 Alkynyl" In some embodiments, the alkynyl group has 2 to 6 carbon atoms ("C 2 ~6 In some embodiments, the alkynyl group is a 2 to 5 carbon atom alkynyl group. ("C 2~5 In some embodiments, the alkynyl group is having 4 to 5 carbon atoms ("C 2~4 In some embodiments, alkynyl is The quinyl group has 2 to 3 carbon atoms ("C 2~3 alkynyl). In this embodiment, the alkynyl group has two carbon atoms ("C 2 alkynyl). Or more carbon-carbon triple bonds may be present internally (e.g., 2-butynyl). ) or at the end (e.g., 1-butynyl). 2~4 Examples of alkynyl groups include The ethynyl group (C 2 ), 1-propynyl (C 3 ), 2-propynyl (C 3 ), 1-Buty Nil (C 4 ), 2-butynyl (C 4 ) but are not limited to these. 2~ 6 Examples of alkenyl groups include the above-mentioned C 2~4 Alkynyl groups, as well as pentynyl (C 5 ), Hexynyl (C 6Further examples of alkynyl include heptynyl. Lu (C 7 ), Octynyl (C 8 ), etc. Unless otherwise specified, alkynyl Each occurrence of the group is independently optionally substituted, i.e., unsubstituted ("unsubstituted alkyl"). alkynyl) or one or more substituents; for example, 1 to 5 substituents substituted with 1 to 3 substituents or 1 substituent ("substituted alkynyl"). In certain embodiments, the alkynyl group is an unsubstituted C 2~10 Alkynyl. In one embodiment, the alkynyl group is a substituted C 2~10 It is alkynyl.

[0151] The term "heteroalkyl" as used herein refers to one or more heterocyclic groups in a parent chain. More than one (e.g., one, two, three, or four) heteroatoms (e.g., oxygen, sulfur, nitrogen, boron, silicon, phosphorus), where one or more of The heteroatoms are inserted between adjacent carbon atoms in the parent carbon chain and / or have one or more Or more heteroatoms are inserted between the carbon atom and the parent molecule (i.e., between the points of attachment). In certain embodiments, the alkyl group is an alkyl group, as defined herein, Heteroalkyl groups are groups having 1 to 10 carbon atoms and 1, 2, 3, or 4 heteroatoms. A saturated group having a heterocyclic group ("hetero C 1~10 In some embodiments, the term "alkyl" refers to , heteroalkyl groups are groups having 1 to 9 carbon atoms and 1, 2, 3, or 4 heteroatoms. A saturated group having a heterocyclic group ("hetero C 1~9 In some embodiments, the heteroaryl is a heteroaryl group. The alkyl group is a saturated alkyl group having 1 to 8 carbon atoms and 1, 2, 3, or 4 heteroatoms. KM("Hetero C 1~8 In some embodiments, the heteroalkyl group is , saturated groups having 1 to 7 carbon atoms and 1, 2, 3, or 4 heteroatoms ("heteroatoms"). Terror C 1~7 In some embodiments, the heteroalkyl group is 1 to 6 and 1, 2, or 3 heteroatoms ("hetero C 1~6 Alki In some embodiments, the heteroalkyl group is a heteroaryl group having 1 to 5 carbon atoms and 1 or a saturated group having two heteroatoms ("hetero C 1~5 Some are alkyl groups. In embodiments, a heteroalkyl group contains 1 to 4 carbon atoms and 1 or 2 heteroatoms. A saturated group having a heterocyclic group ("hetero C 1~4 In some embodiments, heteroaryl is a heteroaryl group. An alkyl group is a saturated group having one to three carbon atoms and one heteroatom ("hetero C 1~3 In some embodiments, the heteroalkyl group is a 1 to 2 carbon A saturated group having one heteroatom and one heteroatom ("hetero C 1~2 "alkyl"). In some embodiments, the heteroalkyl group has 1 carbon atom and 1 heteroatom. Saturated groups ("hetero C 1 In some embodiments, the heteroalkyl group is , a saturated group having 2 to 6 carbon atoms and 1 or 2 heteroatoms ("hetero C 2~ 6 Unless otherwise specified, each occurrence of a heteroalkyl group is independent. and is unsubstituted ("unsubstituted heteroalkyl") or contains one or more substituents. ("substituted heteroalkyl"). In certain embodiments, the heteroalkyl The aryl group is an unsubstituted heterocyclic 1~10 In certain embodiments, heteroaryl is heteroaryl. The alkyl group is a substituted heterocyclic C 1~10 It is an alkyl.

[0152] "Aryl" means an aromatic ring system having 6 to 14 ring carbon atoms and 0 heteroatoms. Monocyclic or polycyclic (e.g., bicyclic or tricyclic) 4n+2 aromatic ring systems ( For example, radixins having 6, 10 or 14 pi electrons shared in a cyclic arrangement Cal ("C 6~14 In some embodiments, an aryl group is , having six ring carbon atoms ("C 6 aryl"; e.g., phenyl). In the formula (I), the aryl group has 10 ring carbon atoms ("C 10 aryl"; e.g. naphthyl, such as 1-naphthyl and 2-naphthyl. In some embodiments, aryl The group has 14 ring carbon atoms ("C 14 aryl"; e.g., anthracyl). "Aryl" refers to a group in which an aryl ring, as defined above, is bonded to one or more carbocyclic rings. Also included are ring systems fused to an aryl or heterocyclyl group, where the bonded radical or The point of attachment may be on an aryl ring, in which case the number of carbon atoms will continue to be determined by the aryl group. The number of carbon atoms in the ring system is noted. Exemplary aryl groups include aceanthrylene, aceanthrylene, Cenaphthylene, acephenanthrylene, anthracene, azulene, benzene, chrysene, Coronene, fluoranthene, fluorene, hexacene, hexaphene, hexalene, as -Indacene, s-indacene, indane, indene, naphthalene, octacene, octacene Phen, octalene, ovalene, penta-2,4-diene, pentacene, pentalene, pene perylene, phenalene, phenanthrene, picene, pleiadene, pyrene, Included are groups derived from pyranthrene, rubicene, triphenylene, and trinaphthalene. In particular, the aryl group may be phenyl, naphthyl, indenyl, or the like. and tetrahydronaphthyl. Unless otherwise specified, each occurrence of an aryl group is Each of the aryl groups is independently optionally substituted, i.e., unsubstituted ("unsubstituted aryl"). ) or substituted with one or more substituents ("substituted aryl"). In certain embodiments, the aryl group is an unsubstituted C 6~14 It is aryl. In one embodiment, the aryl group is a substituted C 6~14 It is aryl.

[0153] In certain embodiments, the aryl group is halo, C 1 ~C 8 Alkyl, C 1 ~C 8 Haloalkyl, cyano, hydroxy, C 1 ~C 8 selected from alkoxy and amino , substituted with one or more groups.

[0154] Representative examples of substituted aryl include: [ka] Here, R 56 and R 57 can be hydrogen, and R 56 and R 57 At least One is, independently, C 1 ~C 8 Alkyl, C 1 ~C 8 Haloalkyl, 4-10 membered heptane Rocyclyl, alkanoyl, C 1 ~C 8 Alkoxy, heteroaryloxy, alkyla amino, arylamino, heteroarylamino, NR 58 COR 59 , N.R. 58 SOR 5 9 , N.R. 58 SO 2 R 59 , COO alkyl, COO aryl, CONR 58 R 59 , C ONR 58 OR 59 , N.R. 58 R 59 , S.O. 2 NR 58 R 59 , S-alkyl, SO-alkyl Kill, SO 2 Alkyl, S aryl, SO aryl, SO 2 aryl; or R 56 and R 57 is linked to 5-8 atoms (N, O or or S) containing one or more heteroatoms selected from the group or unsaturated). 60 and R 61 are independently hydrogen, C 1 ~C 8 Alki Lu, C 1 ~C 4 Haloalkyl, C 3 ~C 10 Cycloalkyl, 4-10 membered heterocyclyl , C 6 ~C 10 Aryl, Substituted C 6 ~C10 Aryl, 5-10 membered heteroaryl or It is a substituted 5-10 membered heteroaryl.

[0155] "Fused aryl" refers to a fused aryl group that is connected to a second aryl or heteroaryl ring or a carboxyl group. It refers to an aryl that shares two ring carbons with an aryl or heterocyclyl ring.

[0156] "Heteroaryl" means an aryl group having ring carbon atoms and one to four ring heteroatoms provided in an aromatic ring system. 5-10 membered monocyclic or bicyclic 4n+2 aromatic ring systems (e.g., in a cyclic arrangement) (having 6 or 10 π electrons shared between each atom) The heteroatoms are independently selected from nitrogen, oxygen and sulfur ("5- to 10-membered heteroaryls"). In heteroaryl groups that contain one or more nitrogen atoms, the point of attachment is It may be a carbon or nitrogen atom, if valence permits. Heteroaryl bicyclic ring systems include One or both rings may contain one or more heteroatoms. "Heteroaryl" refers to a heteroaryl ring, as defined above, which is bonded to one or more carbocyclic rings. and ring systems fused to a aryl or heterocyclyl group, where the point of attachment is at the heteroaromatic on the aryl ring, in which case the number of ring members continues to be determined by the heteroaryl ring system. "Heteroaryl" refers to a heteroaryl as defined above. Also included are ring systems in which an aryl ring is fused to one or more aryl groups, where the point of attachment is is present on an aryl or heteroaryl ring, and in such cases the number of ring members indicates the number of ring members in a fused (aryl / heteroaryl) ring system. Bicyclic heteroaryl groups containing no heteroatoms (e.g., indolyl, quinolinyl, carbaryl, bazolyl, etc.), the point of attachment may be on either ring, i.e., on a ring containing a heteroatom (e.g. , 2-indolyl) or in a ring that does not contain a heteroatom (e.g., 5-indolyl) possible.

[0157] In some embodiments, a heteroaryl group has ring carbon atoms and 1 to 4 ring heteroatoms. A 5- to 10-membered aromatic ring system in which each heteroatom is provided in the aromatic ring system. independently selected from nitrogen, oxygen and sulfur ("5- to 10-membered heteroaryl"). In some embodiments, a heteroaryl group contains ring carbon atoms and 1 to 4 ring heteroatoms. is provided to the aromatic ring system, wherein each heteroatom is independently In some embodiments, the heteroaryl is selected from nitrogen, oxygen, and sulfur ("5- to 8-membered heteroaryl"). In the form, a heteroaryl group is one in which the ring carbon atoms and 1 to 4 ring heteroatoms are in an aromatic ring. A 5-6 membered aromatic ring system is provided in the system, where each heteroatom is independently selected from the group consisting of nitrogen, In some embodiments, the aryl group is selected from the group consisting of 5- to 6-membered heteroaryl. In the present invention, the 5-6 membered heteroaryl is a heteroaryl having 1-3 ring members selected from nitrogen, oxygen and sulfur. In some embodiments, the 5-6 membered heteroaryl has nitrogen, oxygen and and sulfur. 6-membered heteroaryl has one ring heteroatom selected from nitrogen, oxygen, and sulfur. Unless otherwise specified, each occurrence of a heteroaryl group is independently an optional substituent. Heteroaryl is substituted, i.e., unsubstituted ("unsubstituted heteroaryl") or has one or more In certain embodiments, the heteroaryl group is substituted with more than one substituent ("substituted heteroaryl"). In certain embodiments, the heteroaryl group is an unsubstituted 5- to 14-membered heteroaryl. In the embodiment, the heteroaryl group is a substituted 5-14 membered heteroaryl.

[0158] Exemplary 5-membered heteroaryl groups containing one heteroatom include pyrrolyl, furanyl, and the like. Examples containing two heteroatoms include, but are not limited to, phenyl and thiophenyl. Exemplary 5-membered heteroaryl groups include imidazolyl, pyrazolyl, oxazolyl, isopropyl, phenyl ... Examples include, but are not limited to, xazolyl, thiazolyl and isothiazolyl. Exemplary 5-membered heteroaryl groups containing 5 heteroatoms include triazolyl, oxazolyl, Examples include, but are not limited to, azolyl and thiadiazolyl. 4 heteroatoms Exemplary 5-membered heteroaryl groups include, but are not limited to, tetrazolyl. Exemplary 6-membered heteroaryl groups containing one heteroatom include pyridinyl. Exemplary 6-membered heteroaryls containing two heteroatoms include, but are not limited to, Examples of alkyl groups include, but are not limited to, pyridazinyl, pyrimidinyl, and pyrazinyl. Exemplary 6-membered heteroaryl groups containing 3 or 4 heteroatoms include: These include, but are not limited to, triazinyl and tetraazinyl, respectively. Exemplary 7-membered heteroaryl groups containing heteroatoms include azepinyl, oxepinyl, and Exemplary 5,6-bicyclic heteroaryls include, but are not limited to, thiepinyl and thiepinyl. The aryl group includes indolyl, isoindolyl, indazolyl, benzotriazolyl, Benzothiophenyl, isobenzothiophenyl, benzofuranyl, benzisofuranyl, Benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzoxadiazol Zolyl, benzothiazolyl, benzisothiazolyl, benzothiadiazolyl, indolizine Exemplary 6,6-bicyclic heterocyclic rings include, but are not limited to, phenyl and purinyl. The aryl group includes naphthyridinyl, pteridinyl, quinolinyl, isoquinolinyl, Examples of such aryl groups include cinnolinyl, quinoxalinyl, phthalazinyl, and quinazolinyl. Not limited to.

[0159] Representative examples of heteroaryl include those of the formula: [ka] where each Z is carbonyl, N, NR 65 , O and S; R 65 are independently hydrogen, C 1 ~C 8 Alkyl, C 3 ~C 10 Cycloalkyl, 4-10 C 6 ~C 10 aryl and 5-10 membered heteroaryl.

[0160] "Carbocyclyl" or "carbocyclic" means a ring system having 3 to 10 ring carbon atoms ( "C 3~10 "carbocyclyl") and non-aromatic cyclic hydrocarbons with 0 heteroatoms In some embodiments, the carbocyclyl group is a radical of the ("C 3~8 In some embodiments, the carbocyclyl A bocyclyl group has 3 to 6 ring carbon atoms ("C3~6 Carbocyclyl). In some embodiments, the carbocyclyl group has 3 to 6 ring carbon atoms ("C 3 ~6 In some embodiments, the carbocyclyl group is a 5 to 10 Having ring carbon atoms ("C 5~10 Carbocyclyl). Exemplary C 3~6 Carbocycli The cyclopropyl group is 3 ), cyclopropenyl (C 3 ), cyclobutyl (C 4 ), cyclobutenyl (C 4 ), cyclopentyl (C 5 ), cyclopentenyl (C 5 ), Cyclohexyl (C 6 ), cyclohexenyl (C 6 ), cyclohexadienyl (C 6 ) Examples of C 3~8 The carbocyclyl group is The above C 3~6 Carbocyclyl groups, as well as cycloheptyl (C 7 ), cycloheptenyl (C 7 ), cycloheptadienyl (C 7 ), cycloheptatrienyl (C 7 ), Cyclo C 8 ), cyclooctenyl (C 8 ), bicyclo[2.2.1]heptanyl (C 7 ), bicyclo[2.2.2]octanyl (C 8 ) but are not limited to these. An example of C 3~10 The carbocyclyl group is the above-mentioned C 3~8 Carbocyclyl groups, and cyclononyl (C 9 ), cyclononenyl (C9 ), cyclodecyl (C 10 ), S Clodecenyl (C 10 ), octahydro-1H-indenyl (C 9 ), Decahydronaphthalene Lenil (C 10 ), spiro[4.5]decanyl (C 10 ) are examples of but are not limited to these. As the above examples are illustrated, in certain embodiments, carbocyclyl The group may be monocyclic ("monocyclic carbocyclyl") or may be a fused ring system, bridged ring system or contains spirocyclic ring systems (e.g., bicyclic systems ("bicyclic carbocyclyl")) and may be saturated. "Carbocyclyl" means a carbocyclyl group as defined above. The bocyclyl ring is fused to one or more aryl or heteroaryl groups. Also included are ring systems in which the point of attachment is on the carbocyclyl ring, in which case the carbon The numbers continue to refer to the number of carbons in the carbocyclic ring system. Each occurrence of the alkyl group is independently optionally substituted, i.e., unsubstituted ("unsubstituted"). carbocyclyl) or substituted with one or more substituents ("substituted In certain embodiments, the carbocyclyl group is an unsubstituted C 3~ 10 In certain embodiments, the carbocyclyl group is a substituted C 3~10 It is a carbocyclyl.

[0161] In some embodiments, "carbocyclyl" refers to a single ring having 3 to 10 ring carbon atoms. Cyclic saturated carbocyclyl groups ("C 3~10 In some embodiments, In the formula (I), the cycloalkyl group has 3 to 8 ring carbon atoms ("C 3~8 Cycloa In some embodiments, a cycloalkyl group has 3 to 6 ring carbon atoms. ("C 3~6 In some embodiments, the cycloalkyl group is , having 5 to 6 ring carbon atoms ("C 5~6 In some embodiments, In this case, a cycloalkyl group has 5 to 10 ring carbon atoms ("C 5~10 Cycloal "Kill"). 5~6 Examples of cycloalkyl groups include cyclopentyl (C 5 ) and Sik Rohexyl (C 5 ) are listed. C 3~6 Examples of cycloalkyl groups include the above-mentioned C 5 ~6 Cycloalkyl groups, as well as cyclopropyl (C 3 ) and cyclobutyl (C 4 )but C 3~8 Examples of cycloalkyl groups include the above-mentioned C 3~6 Cycloalkyl group , and cycloheptyl (C 7 ) and cyclooctyl (C 8 ) can be mentioned. Unless specified, each occurrence of a cycloalkyl group is independently unsubstituted ("unsubstituted cycloalkyl groups"). or substituted with one or more substituents ("substituted cycloalkyl"); In certain embodiments, the cycloalkyl group is an unsubstituted C 3~10 In certain embodiments, the cycloalkyl group is a substituted C 3~ 10 It is cycloalkyl.

[0162] "Heterocyclyl" or "heterocyclic" means a ring system having ring carbon atoms and 1 to 4 ring heteroatoms. refers to a 3- to 10-membered non-aromatic ring system radical having heteroatoms, where each heteroatom is Independently selected from nitrogen, oxygen, sulfur, boron, phosphorus and silicon ("3 to 10-membered Heterocyclyl groups containing one or more nitrogen atoms In this case, the point of attachment may be a carbon or nitrogen atom, where valence allows. The group may be a monocyclic ring system ("monocyclic heterocyclyl") or a fused ring system, bridged ring system or spinel. It may be a monocyclic ring system (e.g., a bicyclic system ("bicyclic heterocyclyl")) and may be saturated. Heterocyclyl bicyclic ring systems may have one or both rings that are unsaturated or partially unsaturated. It may contain one or more heteroatoms. "Heterocyclyl" is defined above. Ring systems in which such a heterocyclyl ring is fused to one or more carbocyclyl groups. wherein the point of attachment is on the carbocyclyl or heterocyclyl ring or on any of the groups defined above. The heterocyclyl ring as defined herein may be substituted with one or more aryl or heteroaryl groups. on a ring system fused to a heterocyclyl group, where the point of attachment is on the heterocyclyl ring; In such cases, the number of ring members continues to refer to the number of ring members in the heterocyclyl ring system. Unless otherwise specified, each occurrence of heterocyclyl is independently, optionally Substituted, i.e., unsubstituted ("unsubstituted heterocyclyl") or containing one or is substituted with more substituents ("substituted heterocyclyl"). In the above, the heterocyclyl group is an unsubstituted 3- to 10-membered heterocyclyl. In embodiments, the heterocyclyl group is a substituted 3- to 10-membered heterocyclyl.

[0163] In some embodiments, a heterocyclyl group has ring carbon atoms and 1 to 4 ring heterocycles. A 5-10 membered non-aromatic ring system having atoms, where each heteroatom is independently selected from nitrogen, , oxygen, sulfur, boron, phosphorus and silicon ("5- to 10-membered heterocyclyl In some embodiments, a heterocyclyl group has ring carbon atoms and 1 to 4 ring halves. A 5-8 membered non-aromatic ring system having heteroatoms, where each heteroatom is independently selected from nitrogen and In some embodiments, the aryl group is selected from nitrogen, oxygen, and sulfur ("5- to 8-membered heterocyclyl"). In the above, the heterocyclyl group is a 5-6 ring carbon atom and 1-4 ring heteroatoms. and wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur. ("5- to 6-membered heterocyclyl"). In some embodiments, the 5- to 6-membered heterocyclyl A cyclyl has 1 to 3 ring heteroatoms selected from nitrogen, oxygen and sulfur. In some embodiments, the 5- to 6-membered heterocyclyl is selected from nitrogen, oxygen, and sulfur. In some embodiments, the 5- or 6-membered heterocyclyl has one ring heteroatom selected from nitrogen, oxygen and sulfur.

[0164] Exemplary 3-membered heterocyclyl groups containing one heteroatom include azirdinyl (az irdinyl), oxiranyl, and thiorenyl. 1 Exemplary 4-membered heterocyclyl groups containing 4 heteroatoms include azetidinyl, oxetane, Examples containing one heteroatom include, but are not limited to, thietanyl and thietanyl. Exemplary 5-membered heterocyclyl groups include tetrahydrofuranyl, dihydrofuranyl, tetrahydrofuranyl, Dihydrothiophenyl, dihydrothiophenyl, pyrrolidinyl, dihydropyrrolyl and Pyrrolyl-2,5-dione, but not limited to, pyrrolyl-2,5-dione, containing two heteroatoms. Exemplary 5-membered heterocyclyl groups include dioxolanyl, oxasulfuranyl, disulfanyl, These include, but are not limited to, rufuranyl and oxazolidin-2-one. Exemplary 5-membered heterocyclyl groups containing a heteroatom include triazolinyl, oxazolinyl, Examples of heteroaryl include, but are not limited to, azolinyl and thiadiazolinyl. Exemplary 6-membered heterocyclyl groups containing the atoms include piperidinyl, tetrahydropyranyl, Examples of aryl include, but are not limited to, dihydropyridinyl, dihydropyridinyl, and thianyl. Exemplary 6-membered heterocyclyl groups containing a heteroatom include piperazinyl, morpholinyl, Examples of heteroaryls include, but are not limited to, dithianyl and dioxanyl. Exemplary 6-membered heterocyclyl groups include, but are not limited to, triazinanyl. Exemplary seven-membered heterocyclyl groups containing one heteroatom include azepanyl, Examples include, but are not limited to, oxepanyl and thiepanyl. Exemplary 8-membered heterocyclyl groups include azocanyl, oxecanyl, and thiocanyl. C 6 Exemplary 5-membered aryl rings fused to aryl rings The terecyclyl group (also referred to herein as a 5,6-bicyclic heterocyclic ring) includes, for example, isopropyl alcohol ... dolinyl, isoindolinyl, dihydrobenzofuranyl, dihydrobenzothienyl, benzoyl Examples of aryl ring fused aryl include, but are not limited to, oxazolinonyl. Exemplary 6-membered heterocyclyl groups (also referred to herein as 6,6-bicyclic heterocyclic rings) Examples of the quinolinyl group include tetrahydroquinolinyl and tetrahydroisoquinolinyl. The present invention is not limited to these.

[0165] A "nitrogen-containing heterocyclyl" group is a 4- to 7-membered non-aromatic heterocyclic ring system that contains at least one nitrogen atom. aromatic cyclic groups, such as, but not limited to, morpholine, piperidine (e.g., 2-piperidinyl, 3-piperidinyl, and 4-piperidinyl), pyrrolidine (e.g. , 2-pyrrolidinyl and 3-pyrrolidinyl), azetidine, pyrrolidone, imidazoline , imidazolidinone, 2-pyrazoline, pyrazolidine, piperazine, and N-alkyl Specific examples include azetidine, piperazine, Lidone, and piperazone.

[0166] "Hetero" when used to describe a compound or a group present on a compound One or more carbon atoms in the compound or group are heteroatoms of nitrogen, oxygen, or sulfur. Hetero means that the hetero atom is replaced by any of the above hydrocarbyl groups. can also be applied to the above (for example, alkyl having 1 to 5, particularly 1 to 3, heteroatoms, For example, heteroalkyl, cycloalkyl, such as heterocyclyl, aryl, such as , heteroaryl, and cycloalkenyl, such as cycloheteroalkenyl).

[0167] "Acyl" means -C(O)R 20 This refers to the radical, where R 20 is hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted arylene, as defined herein. aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heterephthalic acid. "Alkanoyl" is R 20 is an acyl group, which is a group other than hydrogen. Representative acyl groups include formyl (-CHO), acetyl (-C(=O)CH 3 ), Cyclohexylcarbonyl, cyclohexylmethylcarbonyl, benzoyl (-C(=O )Ph), benzylcarbonyl (-C(=O)CH 2 Ph), --C(O)-C 1 -C 8 Alkyl, -C(O)-(CH 2 ) t (C 6 -C 10 aryl), -C(O)-(CH 2 ) t (5-10 membered heteroaryl), -C(O)-(CH 2 ) t (C 3 -C 10 Cycloa -C(O)-(CH 2 ) t (4-10 membered heterocyclyl) (t is 0-4 In certain embodiments, the aryl groups include, but are not limited to, R 21 is a halo or hydroxy substituted C 1 ~C 8 Alkyl; or C 3 ~C 1 0 Cycloalkyl, 4-10 membered heterocyclyl, C 6 ~C 10 Aryl, arylalkoxy aryl, 5-10 membered heteroaryl or heteroarylalkyl, each of which is an unsubstituted exchange C 1 ~C4 Alkyl, halo, unsubstituted C 1 ~C 4 Alkoxy, unsubstituted C 1 ~C 4 Haloal Kill, Non-Replacement C 1 ~C 4 Hydroxyalkyl or unsubstituted C 1 ~C 4 Haloalkoxy or hydroxy).

[0168] "Alkoxy" means -OR 29 The R 29 is a substitution or non- Substituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl. Particular alkoxy groups are meth Oxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, tert-butoxy , sec-butoxy, n-pentoxy, n-hexoxy and 1,2-dimethylbutoxy Particular alkoxy groups are lower alkoxy, i.e. alkoxy groups having 1 to 6 carbon atoms. Further particular alkoxy groups have 1 to 4 carbon atoms.

[0169] In certain embodiments, R 29 is amino, substituted amino, C 6 ~C 10 Aryl , aryloxy, carboxyl, cyano, C 3 ~C 10 Cycloalkyl, 4 to 10 membered Tetracyclyl, halogen, 5-10 membered heteroaryl, hydroxyl, nitro, thioaryl Koxy, thioaryloxy, thiol, alkyl-S(O)-, aryl-S(O)- , alkyl-S(O) 2 - and aryl-S(O) 2 -One selected from the group consisting of or more substituents, for example 1 to 5 substituents, in particular 1 to 3 substituents, especially An exemplary "substituted alkoxy" group is -O-( CH 2 ) t (C 6 ~C 10 Aryl), -O-(CH 2 ) t (5-10 membered heteroaryl ), -O-(CH 2 ) t (C 3 ~C 10 Cycloalkyl) and -O-(CH 2 ) t (4 10-10 membered heterocyclyl), where t is 0 to 4 and any aryl, heteroaryl, cycloalkyl or heteroaryl group present. The cyclyl group is itself an unsubstituted C 1 ~C 4 Alkyl, halo, unsubstituted C 1 ~C 4 Arco oxy, unsubstituted C 1 ~C 4 Haloalkyl, unsubstituted C 1 ~C 4 Hydroxyalkyl or non-substituted exchange C 1 ~C 4 A particular example of a substituted alkoxy group is alkoxy. The "substituted alkoxy" group is -OCF 3 , -OCH 2 CF 3 , -OCH 2 Ph, -OCH 2 - Cyclopropyl, -OCH 2 CH 2 OH and -OCH 2 CH2 NMe 2 It is.

[0170] "Amino" means -NH 2 It refers to radicals.

[0171] An "oxo group" refers to -C(=O)-.

[0172] "Substituted amino" refers to a group of the formula -N(R 38 ) 2 where R 38 teeth , hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted Substituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or amino-protected group, where R 38 At least one of is not hydrogen. For each R 38 are independently hydrogen, C 1 ~C 8 Alkyl, C 3 ~C 8 Alkenyl, C 3 ~C 8 Alkynyl, C 6 ~C 10 Aryl, 5-10 membered heteroaryl, 4-10 membered heteraryl Rocyclyl or C 3 ~C 10 Cycloalkyl; or substituted with halo or hydroxy C 1 ~C 8 Alkyl; halo or hydroxy substituted C 3 ~C 8 Alkenyl ;Halo or hydroxy substituted C 3 ~C 8 Alkynyl, or -(CH 2 ) t (C 6 ~C 10 Aryl), -(CH 2 ) t (5-10 membered heteroaryl), -(CH 2 ) t (C 3 ~C 10 Cycloalkyl) or -(CH 2 ) t (4-10 membered heterocyclyl ), where t is an integer from 0 to 8, each of which is selected from unsubstituted C 1 ~C 4 Alkyl, halo, unsubstituted C 1 ~C 4 Alkoxy, unsubstituted C 1 ~C 4 Haloalkyl, non-substituted exchange C 1 ~C 4 Hydroxyalkyl or unsubstituted C 1 ~C 4 Haloalkoxy or Hydro or both R 38 The groups taken together form an alkylene group. Form.

[0173] Exemplary "substituted amino" groups include -NR 39 -C 1 ~C 8 Alkyl, -NR 39 - (CH 2 ) t (C 6 ~C 10 Aryl), -NR 39 -(CH 2 ) t (5-10 membered hetero Aryl), -NR 39 -(CH 2 ) t (C 3 ~C 10 Cycloalkyl) and -NR 3 9 -(CH 2 )t (4- to 10-membered heterocyclyl), but are not limited thereto. where t is an integer from 0 to 4, for example, 1 or 2, and each R 39 is independently Or C 1 ~C 8 any alkyl group present may itself be selected from the group consisting of halo, substituted or unsubstituted amino or hydroxy; any aryl present, The heteroaryl, cycloalkyl or heterocyclyl group may itself be an unsubstituted C 1 ~ C 4 Alkyl, halo, unsubstituted C 1 ~C 4 Alkoxy, unsubstituted C 1 ~C 4 Haloalkyl, non substitution C 1 ~C 4 Hydroxyalkyl or unsubstituted C 1 ~C 4 Haloalkoxy or hydroxy For the avoidance of doubt, the term "substituted amino" is defined below. As described above, alkylamino, substituted alkylamino, alkylarylamino, substituted a alkylarylamino, arylamino, substituted arylamino, dialkylamino and Substituted amino includes both mono- and di-substituted amino groups. Includes:

[0174] "Carboxy" refers to the -C(O)OH radical.

[0175] "Cyano" refers to the -CN radical.

[0176] "Halo" or "halogen" means fluoro (F), chloro (Cl), bromo (Br) In certain embodiments, a halo group refers to fluoro or iodo (I). is either chloro.

[0177] "Haloalkyl" means an alkyl group substituted with one or more halogens. A typical haloalkyl group is a trifluoroalkyl group. Methyl, difluoromethyl, fluoromethyl, chloromethyl, dichloromethyl, dibromo ethyl, tribromomethyl, and tetrafluoroethyl. Not limited.

[0178] "Hydroxy" refers to the radical -OH.

[0179] "Nitro" means -NO 2 It refers to radicals.

[0180] "Thioketo" refers to the =S group.

[0181] Alkyl, alkenyl, alkynyl, carbocyclyl, as defined herein The heterocyclyl, aryl and heteroaryl groups are optionally substituted (e.g., For example, "substituted" or "unsubstituted" alkyl, "substituted" or "unsubstituted" alkenyl, "substituted" or "unsubstituted" alkynyl, "substituted" or "unsubstituted" carbocyclyl, "Substituted" or "unsubstituted" heterocyclyl, "substituted" or "unsubstituted" aryl or "Substituted" or "unsubstituted" heteroaryl groups. In general, the term "substituted" refers to Regardless of whether or not preceded by the term "optionally," certain groups (e.g., carbon or At least one hydrogen atom present on the aryl group (e.g., nitrogen atom) may be replaced with an acceptable substituent, e.g., When reacted with a compound, it becomes stable, e.g., a compound that undergoes spontaneous transformation (e.g., rearrangement, cyclization, elimination or It means that the substituents can be replaced with those that produce compounds that do not undergo any other reaction. Unless otherwise indicated, a "substituted" group refers to one or more substitutions on the group. Has substituents at any available position, and two or more positions in any given structure may be substituted. When present, the substituents may be the same or different at each position. "May be modified in any manner that results in the formation of a stable compound" includes all permissible substituents of organic compounds, and any substituents that may be modified in any manner that results in the formation of a stable compound. It is intended to include substitution with any of the substituents described herein. Any and all such combinations are contemplated to arrive at the object of the present invention. For this purpose, a heteroatom such as nitrogen satisfies the valence of the heteroatom, resulting in a stable Hydrogen substituents and / or any of the substituents as described herein may form the specified moiety. It may have suitable substituents.

[0182] Exemplary carbon atom substituents include halogen, -CN, -NO 2 , -N 3 , -SO 2 H , -SO 3 H, -OH, -OR aa , -ON(R bb ) 2 , -N(R bb ) 2 , -N(R bb ) 3 + X - , -N(OR cc )R bb , -SH, -SR aa , -SSR cc , -C( =O)R aa , -CO 2 H, -CHO, -C(OR cc )2 、-CO 2 R aa 、-OC( =O)R aa 、-OCO 2 R aa 、-C(=O)N(R bb ) 2 、-OC(=O)N(R bb ) 2 、-NR bb C(=O)R aa 、-NR bb CO 2 R aa 、-NR bb C(=O )N(R bb ) 2 、-C(=NR bb )R aa 、-C(=NR bb )OR aa 、-OC( =NR bb )R aa 、-OC(=NR bb )OR aa 、-C(=NR bb )N(R bb ) 2 、-OC(=NR bb )N(R bb ) 2 、-NR bb C(=NR bb )N(R bb ) 2 、-C(=O)NR bb SO 2 R aa 、-NR bb SO 2 R aa 、-SO 2 N(R bb ) 2 、-SO 2 R aa 、-SO 2 OR aa 、-OSO 2 R aa 、-S(=O)R aa 、-O S(=O)Raa 、-Si(R aa ) 3 、-OSi(R aa ) 3 -C(=S)N(R b b ) 2 、-C(=O)SR aa 、-C(=S)SR aa 、-SC(=S)SR aa 、-S C(=O)SR aa 、-OC(=O)SR aa 、-SC(=O)OR aa 、-SC(=O )R aa 、-P(=O) 2 R aa 、-OP(=O) 2 R aa 、-P(=O)(R aa ) 2 、-OP(=O)(R aa ) 2 、-OP(=O)(OR cc ) 2 、-P(=O) 2 N(R bb ) 2 、-OP(=O) 2 N(R bb ) 2 、-P(=O)(NR bb ) 2 、-OP(= O)(NR bb ) 2 、-NR bb P(=O)(OR cc ) 2 、-NR bb P(=O)(N R bb ) 2 、-P(R cc ) 2 、-P(R cc ) 3 、-OP(R cc ) 2 、-OP(R c c ) 3 、-B(Raa ) 2 , -B(OR cc ) 2 , -BR aa (OR cc ), C 1~10 Alkyl, C 1~10 Haloalkyl, C 2~10 Alkenyl, C 2~10 Alkynyl, C 3~10 Carbocyclyl, 3-14 membered heterocyclyl, C 6~14 Aryl and 5-1 4-membered heteroaryl, where each alkyl, alkoxy, Nyl, alkynyl, carbocyclyl, heterocyclyl, aryl and heteroaryl are , independently 0, 1, 2, 3, 4 or 5 R dd or substituted with a carbon atom The two geminal hydrogens on the atom are the groups =O, =S, =NN(R bb ) 2 , =NNR bb C( =O)R aa , =NNR bb C(=O)OR aa , =NNR bb S(=O) 2 R aa , = NR bb OR =NOR cc Replaced by;

[0183] R aa Each occurrence of is independently 1~10 Alkyl, C 1~10 Haloalkyl, C 2~ 10 Alkenyl, C 2~10 Alkynyl, C 3~10 Carbocyclyl, 3-14 membered heterocyclic Cyclyl, C 6~14 aryl and 5-14 membered heteroaryl; There are two R aaThe groups are linked to form a 3- to 14-membered heterocyclyl or a 5- to 14-membered heteroaryl group. Form a ring in which each alkyl, alkenyl, alkynyl, carbocyclyl, heptyl, aryl and heteroaryl each independently represent 0, 1, 2, 3, 4 or 5 R dd substituted with a group;

[0184] R bb Each occurrence of is independently hydrogen, -OH, -OR aa , -N(R cc ) 2 , -CN , -C(=O)R aa , -C(=O)N(R cc ) 2 , -CO 2 R aa , -SO 2 R aa , -C(=NR cc ) OR aa , -C(=NR cc )N(R cc ) 2 , -SO 2 N(R c c ) 2 , -SO 2 R cc , -SO 2 OR cc , -SOR aa , -C(=S)N(R cc ) 2 , -C(=O)SR cc , -C(=S)SR cc , -P(=O) 2 R aa , -P(=O )(R aa ) 2 , -P(=O) 2 N(R cc ) 2 , -P(=O)(NR cc ) 2 , C 1~ 10 Alkyl, C1~10 Haloalkyl, C 2~10 Alkenyl, C 2~10 Alkynyl , C 3~10 Carbocyclyl, 3-14 membered heterocyclyl, C 6~14 Aryl and 5 1 to 14-membered heteroaryl, or two R bb The groups are linked together to form 3 to 14 5-14 membered heterocyclyl or 5-14 membered heteroaryl ring, wherein each alkyl, Alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl and heteroaryl Each group may independently contain 0, 1, 2, 3, 4, or 5 R dd substituted with a group;

[0185] R cc Each occurrence of is independently hydrogen, C 1~10 Alkyl, C 1~10 Haloalkyl, C 2~10 Alkenyl, C 2~10 Alkynyl, C 3~10 Carbocyclyl, 3-14 membered Heterocyclyl, C 6~14 aryl and 5- to 14-membered heteroaryl; , or two R cc The groups are linked to form a 3- to 14-membered heterocyclyl or a 5- to 14-membered heterocyclic aryl ring, wherein each alkyl, alkenyl, alkynyl, carbocyclyl , heterocyclyl, aryl and heteroaryl are independently 0, 1, 2, 3, 4 or or 5 R dd substituted with a group;

[0186] R dd Each occurrence of is independently a halogen, -CN, -NO 2 , -N 3 , -SO 2 H, - SO 3 H, -OH, -OR ee , -ON(Rff ) 2 、-N(R ff ) 2 、-N(R ff ) 3 + X - 、-N(OR ee )R ff 、-SH、-SR ee 、-SSR ee 、-C(=O )R ee 、-CO 2 H、-CO 2 R ee 、-OC(=O)R ee 、-OCO 2 R ee 、- C(=O)N(R ff ) 2 、-OC(=O)N(R ff ) 2 、-NR ff C(=O)R e e 、-NR ff CO 2 R ee 、-NR ff C(=O)N(R ff ) 2 、-C(=NR ff )OR ee 、-OC(=NR ff )R ee 、-OC(=NR ff )OR ee 、-C(=N R ff )N(R ff ) 2 、-OC(=NR ff )N(R ff ) 2 、-NR ff C(=NR ff )N(R ff ) 2 、-NR ff SO 2 R ee 、-SO 2 N(R ff ) 2 、-SO2 R ee , -SO 2 OR ee , -OSO 2 R ee , -S(=O)R ee , -Si(R ee ) 3 , -OSi(R ee ) 3 , -C(=S)N(R ff ) 2 , -C(=O)SR ee , -C( =S)SR ee , -SC(=S)SR ee , -P(=O) 2 R ee , -P(=O)(R e e ) 2 , -OP(=O)(R ee ) 2 ,-OP(=O)(OR ee ) 2 , C 1~6 Alki Lu, C 1~6 Haloalkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cal Bocyclyl, 3-10 membered heterocyclyl, C 6~10 Aryl, 5-10 membered heteroaryl wherein each of alkyl, alkenyl, alkynyl, carbocyclyl, heptyl, aryl and heteroaryl each independently represent 0, 1, 2, 3, 4 or 5 R's gg substituted with a group or two geminal R dd The substituents together = Can form O or =S;

[0187] R ee Each occurrence of is independently 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 a Lukenil, C 2~6 Alkynyl, C 3~10 Carbocyclyl, C 6~10 Aryl, 3~ 10-membered heterocyclyl and 3- to 10-membered heteroaryl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl and hetero Aryl is independently 0, 1, 2, 3, 4 or 5 R gg substituted with a group;

[0188] R ff Each occurrence of is independently hydrogen, C 1~6 Alkyl, C 1~6 Haloalkyl, C 2 ~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Carbocyclyl, 3-10 membered heterocyclic Krill, C. 6~10 aryl and 5-10 membered heteroaryl; or The Two R's ff The groups are linked to form a 3- to 14-membered heterocyclyl or a 5- to 14-membered heteroaryl group. wherein each of alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclic, Cyclyl, aryl and heteroaryl each independently represent 0, 1, 2, 3, 4 or 5 R gg substituted with a group;

[0189] R gg Each occurrence of is independently a halogen, -CN, -NO 2 , -N 3 , -SO 2 H, - SO 3 H, -OH, -OC 1~6 Alkyl, -ON(C 1~6 Alkyl) 2 , -N(C 1 ~6 Alkyl) 2 , -N(C1~6 Alkyl) 3 + X - , -NH(C 1~6 Alkyl) 2 + X - , -NH 2 (C 1~6 Alkyl) + X - , -NH 3 + X - , -N(OC 1~6 Al Kill)(C 1~6 alkyl), -N(OH)(C 1~6 alkyl), -NH(OH), - SH, -SC 1~6 Alkyl, -SS(C 1~6 alkyl), -C(=O)(C 1~6 a Rukill), -CO 2 H, -CO 2 (C 1~6 alkyl), -OC(=O)(C 1~6 Al Kill), -OCO 2 (C 1~6 alkyl), -C(=O)NH 2 , -C(=O)N(C 1 ~6 Alkyl) 2 , -OC(=O)NH(C 1~6 alkyl), -NHC(=O)(C 1 ~6 alkyl), -N(C 1~6 Alkyl)C(=O)(C 1~6 alkyl), -NHC O 2 (C 1~6 alkyl), -NHC(=O)N(C 1~6 Alkyl) 2 , -NHC(= O)NH(C 1~6 alkyl), -NHC(=O)NH 2 , -C(=NH)O(C 1~6 alkyl), -OC(=NH)(C 1~6 alkyl), -OC(=NH)OC 1~6 Al Kill, -C(=NH)N(C 1~6 Alkyl) 2 , -C(=NH)NH(C 1~6 Alki -C(=NH)NH 2 , -OC(=NH)N(C 1~6 Alkyl) 2 , -OC(N H)NH(C 1~6 alkyl), -OC(NH)NH 2 , -NHC(NH)N(C 1~6 Alkyl) 2 , -NHC(=NH)NH 2 , -NHSO 2 (C 1~6 Alkyl), -SO 2 N(C 1~6 Alkyl) 2 , -SO 2 NH(C 1~6 Alkyl), -SO 2 NH 2 , - SO 2 C 1~6 Alkyl, -SO 2 O.C. 1~6 Alkyl, -OSO 2 C 1~6 Alkyl, -SOC 1~6 Alkyl, -Si(C 1~6 Alkyl) 3 , -OSi(C 1~6 Alkyl ) 3 -C(=S)N(C 1~6 Alkyl) 2 , C(=S)NH(C 1~6 alkyl), C(=S)NH 2 , -C(=O)S(C 1~6 Alkyl), -C(=S)SC 1~6 Al Kill, -SC(=S)SC 1~6 Alkyl, -P(=O)2 (C 1~6 alkyl), -P (=O)(C 1~6 Alkyl) 2 , -OP(=O)(C 1~6 Alkyl) 2 , -OP(= O)(OC 1~6 Alkyl) 2 , C 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 a Lukenil, C 2~6 Alkynyl, C 3~10 Carbocyclyl, C 6~10 Aryl, 3~ 10-membered heterocyclyl, 5- to 10-membered heteroaryl, or two geminal R gg The substituents may be taken together to form =O or =S; where X - is against I It's on.

[0190] A "counterion" or "anionic counterion" is a cation that maintains electrical neutrality. A counterion is a negatively charged group associated with a neutral quaternary amino group. Exemplary counterions include halo Genide ions (e.g., F - , Cl - , Br - , I - ), NO 3 - , ClO 4 - , O.H. - , H 2 PO 4 - , HSO 4 - , sulfonate ions (e.g., methanesulfonate, trimethylsulfonate, Trifluoromethanesulfonate, p-toluenesulfonate, benzenesulfonate, 1 0-Camphorsulfonate, Naphthalene-2-sulfonate, Naphthalene-1-sulfonate sulfonic acid-5-sulfonate, ethane-1-sulfonic acid-2-sulfonate, etc.) and carboxylate ions (e.g., acetate, ethanoate, propanoate, benzoate Examples of tartrates include glycerate, lactate, tartrate, and glycolate.

[0191] These and other exemplary substituents are described in detail in the detailed description and claims. The present invention is not to be construed in any manner whatsoever as a result of the exemplary enumeration of substituents set forth above. This disclosure is not intended to be limiting.

[0192] Other definitions As used herein, the term "modulation" refers to the inhibition or suppression of GABA receptor function. refers to synergy. A "modulator" (e.g., a modulator compound) is, for example, GAB A receptor agonists, partial agonists, antagonists, or partial antagonists It can be.

[0193] "Pharmaceutically acceptable" means any product approved by any federal or state government regulatory agency or any country other than the United States. Approved or approvable by the appropriate authority or in accordance with the United States Pharmacopeia or other generally recognized pharmacopoeias for use in animals (more specifically, humans). means that it is described in

[0194] A "pharmaceutical acceptable salt" refers to a compound that is pharmaceutical acceptable and has the desired therapeutic effect on the parent compound. In particular, such salts are non-toxic and have no toxicity. , inorganic or organic acid addition salts and inorganic or organic base addition salts. Specifically, such salts include: (1) salts of inorganic acids, such as hydrochloric acid, hydrobromic acid, and sulfuric acid; , nitric acid, phosphoric acid, etc.; or organic acids, e.g. acetic acid, propionic acid, hexa Acid, cyclopentanepropionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, succinic acid Acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, 3-(4-hydroxybutyric acid, (oxybenzoyl)benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonate sulfonic acid, 1,2-ethanedisulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid Sulfonic acid, 4-chlorobenzenesulfonic acid, 2-naphthalenesulfonic acid, 4-toluenesulfonic acid camphorsulfonic acid, camphorsulfonic acid, 4-methylbicyclo[2.2.2]-oct-2-ene -1-Carboxylic acid, glucoheptonic acid, 3-phenylpropionic acid, trimethylacetic acid, Tertiary butyl acetate, lauryl sulfate, gluconic acid, glutamic acid, hydroxynaphthoic acid, (2) Acid addition salts formed with licylic acid, stearic acid, muconic acid, etc.; or (3) the parent compound The acidic protons present in the or aluminum ions; or an organic base, e.g. ethanol. It is also used in combination with diethanolamine, diethanolamine, triethanolamine, N-methylglucamine, etc. Further salts include, by way of example only, salts formed when sodium Umium, potassium, calcium, magnesium, ammonium, tetraalkylammonium and, if the compound contains a basic functional group, salts of non-toxic organic or inorganic acids, For example, hydrochloride, hydrobromide, tartrate, mesylate, acetate, maleate, oxalate The term "pharmacologically acceptable cation" refers to an acceptable salt of an acidic functional group. Such cations include sodium cation, potassium cation, cation, calcium cation, magnesium cation, ammonium cation, ther For example, Berge et al., J. See Pharm. Sci. (1977) 66(1):1-79.

[0195] The term "prodrug" refers to a therapeutically inactive compound that is converted under physiological conditions into a therapeutically active agent of the present invention. One method of making a prodrug is to produce a compound that reacts with physiological conditions and is an active compound. and hydrolyzing or cleaving the desired molecule at the targeted in vivo site of action, and then designing the selected moiety to provide that therapeutic effect. The prodrug is converted by the enzymatic activity of the subject.

[0196] In an alternative embodiment, the present invention provides a compound represented by formula (II), formula (I-II), formula (II-I), formula ( II-II), Formula (III-I), Formula (III-II), Formula (IV-I), Formula (IV-I I), formula (IV-III), formula (VI), formula (V-II), or formula (V-III) The present invention provides a prodrug of a compound represented by formula (II), formula (I- II), formula (II-I), formula (II-II), formula (III-I), formula (III-II), Formula (IV-I), Formula (IV-II), Formula (IV-III), Formula (VI), Formula (V-II ), or containing a cleavable moiety on the C3 hydroxy shown in the compound of formula (V-III) nothing.

[0197] "Tautomers" refer to interchangeable forms of a particular compound structure and are not soluble in water. It refers to a compound in which the displacement of elementary atoms and electrons varies. Therefore, the two structures are and can be in equilibrium with the transfer of an atom (usually H). For example, enols and ketones Tautomers are rapidly interconverted by treatment with either acid or base, hence the term tautomers. Another example of tautomerism is the phenyl nitrile which is similarly formed in the presence of acid or base. Tautomers are the acid and nitro forms of methyl methacrylate. Tautomers are the most suitable chemical form for a compound of interest. This may be associated with gain of reactivity and biological activity.

[0198] The "subjects" to which administration is contemplated include humans (i.e., any age group, e.g., children, Subjects (e.g., infants, children, adolescents) or adult subjects (e.g., young adults, middle-aged adults, or elderly adult male or female) and / or non-human animals, e.g., mammals (e.g. For example, primates (e.g., cynomolgus monkeys, rhesus monkeys), cattle, pigs, horses, sheep, goats, rodents, cats and / or dogs). In certain embodiments, the subject is a human. It is a non-human animal.

[0199] In certain embodiments, the substituent present on the oxygen atom is an oxygen protecting group (hydroxyl The oxygen protecting group is -R aa , -N(R bb ) 2 , -C (=O)SR aa , -C(=O)R aa , -CO 2 R aa , -C(=O)N(R bb ) 2 , -C(=NR bb )R aa , -C(=NR bb ) OR aa , -C(=NR bb )N(R bb ) 2 , -S(=O)R aa , -SO 2 R aa , -Si(R aa ) 3 , -P(R cc ) 2 , -P(R cc ) 3 , -P(=O) 2 R aa , -P(=O)(R aa ) 2 , -P(=O )(OR cc ) 2 , -P(=O) 2 N(R bb ) 2 , and -P(=O)(NR bb ) 2 (where R aa , R bb , and R cc is as defined herein) Oxygen protecting groups include, but are not limited to, those well known in the art. cting Groups in Organic Synthesis,TWGr eene and PGMWuts,3 rd edition, John Wil , 1999 (incorporated herein by reference). Some of the things mentioned are:

[0200] Exemplary oxygen protecting groups include methyl, methoxymethyl (MOM), 2-methoxyethyl (2-methoxyethyl) and 2-methoxyethyl (2-methoxyethyl) groups. Toxomethyl (MEM), benzyl (Bn), triisopropylsilyl (TIPS), -Butyldimethylsilyl (TBDMS), t-Butylmethoxyphenylsilyl (TBMP S), methanesulfonate (mesylate), and tosylate (Ts). Not limited to these.

[0201] In certain embodiments, the substituent present on the sulfur atom is a sulfur protecting group (thiol protecting group). The sulfur protecting group is -R aa , -N(R bb ) 2 , -C(= O)SR aa , -C(=O)R aa , -CO 2 R aa , -C(=O)N(R bb ) 2 , - C(=NR bb )R aa , -C(=NR bb ) OR aa , -C(=NR bb )N(R bb ) 2 , -S(=O)R aa , -SO 2 R aa , -Si(R aa ) 3 , -P(R cc ) 2 , -P(R cc ) 3 , -P(=O) 2 R aa , -P(=O)(R aa ) 2 , -P(=O)( OR cc ) 2 , -P(=O) 2 N(R bb ) 2 , and -P(=O)(NR bb ) 2 The These include, but are not limited to, R aa , R bb , and R cc is used herein Sulfur protecting groups are well known in the art and are as defined in Groups in Organic Synthesis,TW Greene and PGMWuts,3 rd edition, John Wiley & So ns, 1999, which is incorporated herein by reference. Can be obtained.

[0202] In certain embodiments, the substituent present on the nitrogen atom is an amino protecting group (see herein). (also called nitrogen protecting group). Amino protecting groups include -OH, -OR aa , -N (R cc ) 2 , -C(=O)R aa , -C(=O)OR aa , -C(=O)N(R cc ) 2 , -S(=O) 2 R aa , -C(=NR cc )R aa , -C(=NR cc ) OR aa , -C(=NR cc )N(R cc ) 2 , -SO 2 N(R cc ) 2 , -SO 2 R cc , -SO 2 OR cc , -SOR aa , -C(=S)N(R cc ) 2 , -C(=O)SR cc , -C (=S)SR cc , C 1~10 Alkyl, C 2~10 Alkenyl, C 2~10 Alkynyl , C 3~10 Carbocyclyl, 3-14 membered heterocyclyl, C 6~14 Aryl, and 5-14 membered heteroaryl groups, but are not limited thereto, where alkyl, a Alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl Each of the groups may independently contain 0, 1, 2, 3, 4, or 5 R dd is substituted with a group, Here, R aa , R bb , R cc , and R dd is as defined herein Amino protecting groups are well known in the art and are described in Organic Synthesis,TW Greene and PGMW uts,3 rd edition, John Wiley & Sons, 1999 (see (herein incorporated by reference in its entirety).

[0203] Exemplary amino protecting groups include amide groups (e.g., -C(=O)R aa )(Holma amido and acetamido); carbamate groups (e.g. For example, -C(=O)OR aa ) (9-Fluorenylmethylcarbamate (Fmoc), t -butyl carbamate (BOC), and benzyl carbamate (Cbz). but not limited to; sulfonamide groups (e.g., -S(=O) 2 R aa )(p -toluenesulfonamide (Ts), methanesulfonamide (Ms), and N-[2- (Trimethylsilyl)ethoxy]methylamine (SEM) Examples of suitable ion exchange membranes include, but are not limited to, those that are not suitable for use in a cellular environment.

[0204] Disease, disorder, and condition are used interchangeably herein.

[0205] As used herein, unless otherwise specified, the term "treat" refers to "," "treating" and "treatment" refer to It is performed while the body is suffering from a particular disease, disorder or condition, and is associated with that disease, disorder or condition. or to slow or retard the progression of a disease, disorder or condition. In an alternative embodiment, the present invention contemplates the act of improving the quality of life of a subject by treating a particular disease, disorder, or condition. Administration of the compounds of the invention as a prophylactic before the onset of a condition or disease is contemplated.

[0206] In general, an "effective amount" of a compound is that amount of a compound that is sufficient to elicit a desired biological response, e.g., CN This refers to an amount sufficient to treat S-related disorders, not an amount sufficient to induce anesthesia or sedation. As will be appreciated by those of skill in the art, an effective amount of a compound of the present invention will be the target objective, the pharmacokinetics of the compound, the disease being treated, the mode of administration, and the age, weight, and / or other characteristics of the subject. The effective amount may vary depending on factors such as the patient's condition, health status, and status. Includes preventive measures.

[0207] As used herein, unless otherwise specified, a "therapeutically effective amount" of a compound means Provides a therapeutic benefit in the treatment of a disease, disorder, or condition or Delay or minimize one or more symptoms associated with an injury or condition A therapeutically effective amount of a compound is an amount sufficient to treat a disease, disorder, or condition. The amount of therapeutic agent, alone or in combination with other therapies, that provides a therapeutic benefit in The term "therapeutically effective amount" means an amount that improves the overall treatment, symptoms or severity of a disease or condition. is an amount that reduces or avoids the cause, or that enhances the therapeutic efficacy of another therapeutic agent. It may include.

[0208] As used herein, unless otherwise specified, a "prophylactically effective amount" of a compound means A disease, disorder or condition, or one or more of the following associated with that disease, disorder or condition: This is an amount sufficient to prevent more than one symptom or to prevent its recurrence. A prophylactically effective amount of a compound is an amount that provides a prophylactic benefit in the prevention of the disease, disorder or condition. The term "prophylactically effective" refers to the amount of a therapeutic agent, alone or in combination with another agent, that satisfies the The term "amount" can include an amount that improves overall prophylaxis or an amount that enhances the prophylactic efficacy of another prophylactic agent. do. compound

[0209] In one aspect, a compound represented by formula (II): [ka] or a pharma- ceutically acceptable salt thereof, In formula (II), t is 1 or 2; R 7 is hydrogen or methyl, or [ka] If is a double bond, R 7 does not exist; R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; can be; R 9 is hydrogen or substituted or unsubstituted alkyl; R 6a and R 6b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted a is alkynyl or R 6a and R 6b together form an oxo (=O) group ; R 11a , R 11b , R 15a , R 15b , R 16a , R 16b , R 17a , R 17b , R 18a , R 18b , R 19a , or R 19b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl , substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl, an oxygen protecting group when bonded to an oxygen atom, a nitrogen atom A nitrogen protecting group when attached to a cyclic ring or two R D1 Groups may be substituted together or R forms an unsubstituted heterocyclic ring; 11a and R 11b , R 15a and R 15 b , R 16a and R 16b , R 17a and R 17b , and R 18a and R 18 b any one of these taken together form an oxo (=O) group; R 5a , R 5b , R 8 , and R 13 Each of the groups is independently hydrogen, halogen, sialyte, or arginine. , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -SR A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , - OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -C(=O) N(R A1 ) 2 , -OC(=O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O ) OR A1, -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O )R A1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O)N (R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 ,or -S(=O) 2 OR A1 where R A1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, Substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or Unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen protection when bonded to an oxygen atom -protecting groups, sulfur protecting groups when attached to a sulfur atom, nitrogen protecting groups when attached to a nitrogen atom, SO 2 R A2 , -C(O)R A2 or two R A1 Substitutions are also possible when groups are combined. or an unsubstituted heterocyclic or heteroaryl ring; R A2 is a substitution or non- Substituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; or R 8 and R 13 together form an oxo (=O) group, where R 8 and R 13 When taken together, they form an oxo (=O) group, R 3 is a substituted or unsubstituted alkoxy group. alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted Substituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; Here, R 5a , R 5b , R 8 , and R 13 At least one of the following is selected from the group consisting of ethyl, substituted aryl, alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted Substituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl , substituted or unsubstituted heteroaryl, -OR A1 , -SR A1 , -N(R A1 ) 2 , - N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -C(=O)N(R A1 ) 2 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -OC(= O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O)OR A1 , -SC(=O) S.R. A1 , -SC(=O)N(R A1 )2 , -NHC(=O)R A1 , -NHC(=O) OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O ) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 So. Must be; Here, R 8 and R 13 and cannot both be methyl; Where: [ka] represents a single bond or a double bond, and when a double bond is present in ring B, R 6a or R 6 b and R 7 does not exist. Formula (II): Group R 15a and R 15b

[0210] In some cases, R 15a and R 15b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -O C(=O)R D1 , -NH2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 in where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0211] In some cases, R 15a and R 15b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl.

[0212] In some cases, R 15a and R 15b each independently represents hydrogen, a substituted or unsubstituted Substituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; be.

[0213] In some cases, R 15a and R 15b are both hydrogen.

[0214] In some embodiments, R 15a and R 15b each independently represents hydrogen or an optionally substituted Preferably it is unsubstituted alkyl.

[0215] In some embodiments, R 15a and R 15b each independently represents hydrogen, C 1 ~C 6 a Rukill, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, Or -OH.

[0216] In some embodiments, R 15a or R 15b But -CH 3 , -CH 2 CH 3 , -OH , -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II): group R 16a and R 16b

[0217] In some cases, R 16a or R 16b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -O C(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 in where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0218] In some cases, R 16a or R 16b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl.

[0219] In some cases, R 16a or R 16b each independently represents hydrogen, a substituted or unsubstituted Substituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2,or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; be.

[0220] In some cases, R 16a and R 16b are hydrogen. In a further embodiment, , R 16a and R 16b are each independently hydrogen or substituted or unsubstituted alkyl; be.

[0221] In some cases, R 16a and R 16b each independently represents hydrogen, C 1 ~C 6 Alki Lu, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, also is -OH. In some other aspects, R 16a or R 16b But -CH 3 , -CH 2 CH 3 , -OH, -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II): group R 17a and R 17b

[0222] In some embodiments, R 17a or R 17b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl.

[0223] In some further embodiments, R 17a or R 17b each independently represents hydrogen, halo aryl, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene Nil, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl aryl, or substituted or unsubstituted heteroaryl.

[0224] In some cases, R 17a or R 17b each independently represents hydrogen, a substituted or unsubstituted Substituted alkyl, -OR D1 , -OC(=O)RD1 , -NH 2 , -N(R D1 ) 2 ,or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; In some cases, R 17a and R 17b are both hydrogen.

[0225] In some cases, R 17a and R 17b each independently represents hydrogen or a substituted or In some aspects, R 17a and R 17b Each of these independently represents water. Basic, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or -OH.

[0226] In some cases, R 17a or R 17b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II): group R 18a and R 18b

[0227] In some cases, R 18a or R18b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -O C(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 in where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0228] In some embodiments, R 18a or R 18b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl.

[0229] In some embodiments, R 18a or R 18b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0230] In some further embodiments, R 18a and R 18b are both hydrogen.

[0231] In some cases, R 18a and R 18b each independently represents hydrogen or a substituted or In some aspects, R 18a and R 18b Each of these independently represents water. Basic, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or -OH.

[0232] In some cases, R 18a or R 18b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II): group R 19a and R19b

[0233] In some embodiments, R 19a or R 19b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl.

[0234] In some further embodiments, R 19a or R 19b each independently represents hydrogen, halo aryl, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene Nil, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl aryl, or substituted or unsubstituted heteroaryl.

[0235] In some cases, R 19a or R 19b each independently represents hydrogen, a substituted or unsubstituted Substituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; be.

[0236] In some cases, R 19a and R 19b are both hydrogen.

[0237] In some cases, R 19a and R 19b each independently represents hydrogen or a substituted or It is an unsubstituted alkyl.

[0238] In some cases, R 19a and R 19b each independently represents hydrogen, C 1 ~C 6 Alki Lu, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, also is -OH.

[0239] In some cases, R 19a or R 19b But -CH 3 , -CH 2 CH3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II): group R 7

[0240] In some cases, R 7 is a hydrogen atom at the cis position. In some other aspects, R 7 But, Tran In some embodiments, R 7 However, it is a methyl group at the cis position. In certain embodiments, R 7 is a methyl in the trans position. Formula (II): Group t

[0241] In some embodiments, t is 1.

[0242] In some embodiments, t is 2. Formula (II): group R 3

[0243] In some embodiments, R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted substituted alkenyl, or substituted or unsubstituted alkynyl.

[0244] In some embodiments, R 3 is a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is a rule.

[0245] In some embodiments, R 3 is substituted or unsubstituted alkyl.

[0246] In some embodiments, R 3 is hydrogen. In some embodiments, R 3 is a substituted alkyl In some embodiments, R 3 is unsubstituted alkyl. In some embodiments, R 3 is methyl. Formula (II): Group R 9

[0247] In some cases, R 9 is hydrogen.

[0248] In some embodiments, R 9 is substituted alkyl. In some embodiments, R 9 But, It is a substituted alkyl.

[0249] In some embodiments, R 9 is methyl. In some embodiments, R 9 But, -OCH 3 In some cases, R 9 is ethyl. Formula (II): Group R 6a and R 6b

[0250] In some embodiments, R 6a and R 6b are independently hydrogen, halogen, substituted or Unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl It is.

[0251] In some cases, R 6a and R 6b are independently hydrogen or substituted or unsubstituted alkoxy. It's a kill.

[0252] In some cases, R 6a and R 6b are independently hydrogen or substituted alkyl. In some embodiments, R 6a and R 6b is independently hydrogen or unsubstituted alkyl.

[0253] In some cases, R 6a and R 6b are hydrogen. In some aspects, R 6a but , halo or alkyl; R 6b is hydrogen. In some embodiments, R 6a Oh BiR 6b Both are halos.

[0254] In some cases, R 6a and R 6b are both alkyl.

[0255] In some embodiments, R 6a and R 6b together form an oxo group. Formula (II): Group R 11a and R 11b

[0256] In some embodiments, R 11a or R 11b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl.

[0257] In some cases, R 11a or R 11b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl.

[0258] In some embodiments, R 11a or R 11b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0259] In some embodiments, R 11a and R 11b are both hydrogen.

[0260] In some further embodiments, R11a and R 11b are each independently hydrogen or It is a substituted or unsubstituted alkyl. Formula (II): Group R 8 and R 13

[0261] In some cases, R 8 or R 13 is a substituted or unsubstituted alkyl, substituted or unsubstituted Substituted alkenyl, substituted or unsubstituted alkynyl, -OR A1 , -SR A1 , -N(R A 1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -C(=O)N(R A1 ) 2 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , or -OC(=O)N(R A1 ) 2 where R A1 Each occurrence of is independently substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, It is a substituted or unsubstituted aryl, or a substituted or unsubstituted heteroaryl.

[0262] In some embodiments, R 8 or R 13 is a substituted or unsubstituted alkyl, -C(O) R A1 , -OC(=O)R A1 , -C(=O)N(R A1 ) 2 , or -OC(=O)O RA1 where R A1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted substituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, Or substituted or unsubstituted heteroaryl.

[0263] In some cases, R 8 or R 13 But -C(O)R A1 where R A1 Is, place It is an alkyl group.

[0264] In some embodiments, the alkyl is substituted with a heteroaryl.

[0265] In some further embodiments, the alkyl is substituted with a 5-membered heteroaryl. Formula (II): Group R 5a and R 5b

[0266] In some cases, R 5a and R 5b are each independently hydrogen, halogen, substituted or Unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted substituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -SR A1 , -N(R A 1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A 1, or -OC(=O)OR A1 where R A1 Each occurrence of is independently hydrogen , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted a alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0267] In some embodiments, R 5a and R 5b are each independently hydrogen, halogen, or substituted or unsubstituted. or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 ,Also -OC(=O)OR A1 where R A1 Each occurrence of may independently represent hydrogen, substitution, or or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl , substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or is unsubstituted heteroaryl.

[0268] In some cases, R 5a and R 5b are each hydrogen.

[0269] In some embodiments, the compound has the formula (I-Ia): [ka] or a pharma- ceutically acceptable salt thereof, Here, R1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted aryl tetracyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -O R A1 , -SR A1 , -N(R A1 ) 2 , -N(R A1 ), -OC(=O)R A1 , -O C(=O)OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC (=O)R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N (R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O) S.R. A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 The existence of each each independently represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid Oxygen protecting group when bonded to oxygen atom, sulfur protecting group when bonded to sulfur atom, nitrogen protecting group when bonded to nitrogen atom Nitrogen protecting group for binding or two R A1 The groups taken together are substituted or forming an unsubstituted heterocyclic or heteroaryl ring; R A2 is a substituted or unsubstituted substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyl, Unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl n is 0, 1, 2, or 3. do.

[0270] In some embodiments, the compound has the formula (I-Iab): [ka] or a pharma- ceutically acceptable salt thereof, R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or Unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -SR A1 , -N(R A1 ) 2 , -N(R A1 ), -OC(=O)R A1 , -OC(=O ) OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2, -SC(=O) R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A 1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , - SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen protecting group when bonded to a sulfur atom; sulfur protecting group when bonded to a nitrogen atom In the case of nitrogen protecting group or two R A1 The groups taken together are substituted or unsubstituted. forming a heterocyclic or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl; Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is substituted or unsubstituted heteroaryl; and n is 0, 1, 2, or 3.

[0271] In some embodiments, the compound has formula (I-Ib) or formula (I-Ibb): [ka] or a pharma- ceutically acceptable salt thereof.

[0272] In some embodiments, the compound has formula (I-Ic) or formula (I-Icb): [ka] or a pharma- ceutically acceptable salt thereof, R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or Unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -SR A1 , -N(R A1 ) 2 , -N(R A1 ), -OC(=O)R A1 , -OC(=O ) OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC(=O) R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1, -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A 1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , - SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen protecting group when bonded to a sulfur atom; sulfur protecting group when bonded to a nitrogen atom In the case of nitrogen protecting group or two R A1 The groups taken together are substituted or unsubstituted. forming a heterocyclic or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl; Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is substituted or unsubstituted heteroaryl; and n is 0, 1, 2, or 3.

[0273] In some embodiments, R 1 is a substituted or unsubstituted alkyl, aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic alkyl, It's a reel.

[0274] In some embodiments, R 1 but, [ka] and Here, R 20 Each occurrence of is independently a halogen, -NO 2 , -CN, -OR GA , - N(R GA ) 2 , -C(=O)R GA , -C(=O)OR GA , -OC(=O)R GA , -OC(=O)OR GA , -C(=O)N(R GA ) 2 , -N(R GA )C(=O)R G A , -OC(=O)N(R GA ) 2 , -N(R GA )C(=O)OR GA , -S(=O) 2 R GA , -S(=O) 2 OR GA , -OS(=O) 2 R GA , -S(=O) 2 N(R G A ) 2 , or -N(R GA )S(=O) 2 R GA ;Substituted or unsubstituted C 1~6 Alki , substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C2~6 Alkynyl, Substituted or unsubstituted C 3~4 Carbocyclyl, substituted or unsubstituted 3- to 4-membered heterocycles Rill or two R's if necessary GA together with the intervening atom, forms an unsubstituted 3- to 4-membered carbocyclic or heterocyclic ring; Here, R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, Substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, when bonded to oxygen oxygen protecting group when bonded to nitrogen, nitrogen protecting group when bonded to nitrogen, or two R GA Motogasuke together with the surrounding atoms form a substituted or unsubstituted carbocyclic or heterocyclic ring; e can be 0, 1, 2, 3, 4, or 5.

[0275] In some embodiments, R 1 but, [ka] and Here, R 20 Each occurrence of is independently a halogen, -NO 2 , -CN, -OR GA , - N(R GA ) 2 , -C(=O)R GA , -C(=O)OR GA , -OC(=O)R GA , -OC(=O)OR GA , -C(=O)N(R GA )2 , -N(R GA )C(=O)R G A , -OC(=O)N(R GA ) 2 , -N(R GA )C(=O)OR GA , -S(=O) 2 R GA , -S(=O) 2 OR GA , -OS(=O) 2 R GA , -S(=O) 2 N(R G A ) 2 , or -N(R GA )S(=O) 2 R GA ;Substituted or unsubstituted C 1~6 Alki , substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~4 Carbocyclyl, substituted or unsubstituted 3- to 4-membered heterocycles Rill or two R's if necessary GA together with the intervening atom, forms an unsubstituted 3- to 4-membered carbocyclic or heterocyclic ring; Here, R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, Substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, when bonded to oxygen oxygen protecting group when bonded to nitrogen, nitrogen protecting group when bonded to nitrogen, or two R GA Motogasuke together with the surrounding atoms form a substituted or unsubstituted carbocyclic or heterocyclic ring; e can be 0, 1, 2, 3, 4, or 5.

[0276] In some embodiments, the compound has formula (I-Id) or formula (I-Idb): [ka] is a compound of Here, R 10 are independently hydrogen, halogen, substituted or unsubstituted alkyl, hydroxyl Sil, or cyano.

[0277] In some embodiments, the compound has formula (I-Ie) or formula (I-Ieb): [ka] or a pharma- ceutically acceptable salt thereof, where e is 0, 1, 2, or 3; p is 0, 1, 2 or 3; R 5 Each of is independently halogen, alkyl, hydroxyl, or cyano.

[0278] In some embodiments, the compound has formula (I-If) or formula (I-Ifb): [ka] or a pharma- ceutically acceptable salt thereof, Here, R 10 are independently hydrogen, halogen, substituted or unsubstituted alkyl, hydroxyl Sil, or cyano.

[0279] In some embodiments, the compound has formula (I-Ig) or formula (I-Igb): [ka] or a pharma- ceutically acceptable salt thereof, where u is 0, 1, or 2; each X is independently -C(R N )-, -C(R N ) 2 -, -O-, -S-, -N-, or N(R N )-where R N is independent , hydrogen, substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR G A , -C(=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl , an oxygen protecting group when attached to oxygen, or a nitrogen protecting group when attached to nitrogen; or The Two R's GA The group, together with the intervening atoms, forms a substituted or unsubstituted heterocyclyl ring or forms a heteroaryl ring.

[0280] In some embodiments, the compound has formula (I-Ih) or formula (I-Ihb): [ka] or a pharma- ceutically acceptable salt thereof, Here, R 10 each independently represents a halogen, an alkyl, a hydroxyl, or a cyano. and m is 0, 1, 2, or 3.

[0281] In some embodiments, the compound has formula (I-Ii) or formula (I-Iib): [ka] or a pharma- ceutically acceptable salt thereof, where n is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -O-, -S-, -N-, or N(R N )-where R N is independent, Hydrogen, substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR GA , -C(=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R G A ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do.

[0282] In some embodiments, the compound has the formula (I-Ik) or the formula (I-Ikb): [ka] or a pharma- ceutically acceptable salt thereof, where s is 0, 1, or 2; R 12 is -N(R ab ) 2 where R ab each independently represents H, substituted or unsubstituted alkyl, -OR ab , -SO 2 (R 15 ), -C(O)R 15 where R 15 is a substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteraryl, cycloalkane, or a substituted or unsubstituted cycloalkane.

[0283] In one aspect, the compound has formula (I-II): [ka] or a pharma- ceutically acceptable salt thereof, wherein the compound is represented by formula (I-II): R 77 is hydrogen or methyl; R 23 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or is unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; ; R 29 is hydrogen or substituted or unsubstituted alkyl; R 26a and R 26b each independently represents hydrogen, halogen, cyano, hydroxyl, Substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted substituted alkynyl or R 26a and R 26b together form an oxo (=O) group. Forming; R 21a , R 21b , R 25a , R 25b , R 36a , R 36b , R 27a , R 27b , R 29a , or R 29b each independently represents hydrogen, halogen, cyano, hydroxyl , substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted hexane Tetracyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D 1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted Alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted substituted heteroaryl, oxygen protecting group when bonded to an oxygen atom, nitrogen protecting group when bonded to a nitrogen atom or two R D1 The groups taken together form a substituted or unsubstituted heterocyclic ring. or R 21a and R 21b , R 25a and R 25b , R 36a Oh BiR 36b , R 27a and R 27b , and R 29a and R 29b One of together form an oxo (=O) group; R 55a , R 55b , R 33a , and R 33b Each of the groups is independently hydrogen, halo. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted substituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -S R A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , -C(=O)N(R A1 ) 2 , -OC(=O)OR A1 , -OC (=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(= O)OR A1 , -SC(=O)SR A1, -SC(=O)N(R A1 ) 2 , -NHC(= O)R A1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O) N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O ) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 ,Also is -S(=O) 2 OR A1 where R A1 Each occurrence of may independently represent hydrogen, substitution, or or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl , substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or is unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen when bonded to an oxygen atom Protecting groups, sulfur protecting groups when attached to a sulfur atom, nitrogen protecting groups when attached to a nitrogen atom; -SO 2 R A2 , -C(O)R A2 or two R A1 Groups are substituted together or an unsubstituted heterocyclic or heteroaryl ring; R A2 is replaced or Unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted substituted aryl, or substituted or unsubstituted heteroaryl; Where: [ka] represents a single bond or a double bond, and when a double bond is present in ring B, R 26a or R 26b and R 77 is not present and a single bond is present in ring B, the hydrogen at C5 is The amino acid is in the beta or β position. Formula (I-II): Group R 25a and R 25b

[0284] In some embodiments, R 25a and R 25b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl.

[0285] In some embodiments, R 25a and R 25b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl.

[0286] In some embodiments, R 25a and R 25b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0287] In some embodiments, R 25a and R 25b are both hydrogen.

[0288] In some embodiments, R 25a and R 25b each independently represents hydrogen or an optionally substituted Preferably it is unsubstituted alkyl.

[0289] In some embodiments, R 25a and R 25b each independently represents hydrogen, C 1 ~C6 a Rukill, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, Or -OH.

[0290] In some embodiments, R 25a or R 25b But -CH 3 , -CH 2 CH 3 , -OH , -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (I-II): Group R 36a and R 36b

[0291] In some embodiments, R 36a or R 36b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl.

[0292] In some embodiments, R 36a or R 36b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl.

[0293] In some embodiments, R 36a or R 36b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0294] In some embodiments, R 36a and R 36b are both hydrogen.

[0295] In some embodiments, R 36a and R 36b each independently represents hydrogen or an optionally substituted Preferably it is unsubstituted alkyl.

[0296] In some embodiments, R 36a and R 36b each independently represents hydrogen, C 1 ~C 6 a Rukill, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, Or -OH.

[0297] In some embodiments, R 36a or R 36b But -CH 3 , -CH 2 CH 3 , -OH , -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (I-II): Group R 27a and R 27b

[0298] In some embodiments, R 27a or R 27b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl.

[0299] In some embodiments, R 27a or R 27b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl.

[0300] In some embodiments, R 27a or R 27b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0301] In some embodiments, R 27a and R 27b are both hydrogen.

[0302] In some embodiments, R 27a and R 27b each independently represents hydrogen or an optionally substituted Preferably it is unsubstituted alkyl.

[0303] In some embodiments, R 27a and R 27b are independently hydrogen, C 1 ~C 6 Alkyl , C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 alkoxyhalo, or -OH.

[0304] In some embodiments, R 27a or R 27b But -CH 3 , -CH 2 CH 3 , -OH , -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (I-II): Group R 29a and R 29b

[0305] In some embodiments, R 29a or R 29b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2, or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl.

[0306] In some embodiments, R 29a or R 29b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl.

[0307] In some embodiments, R 29a or R 29b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0308] In some embodiments, R 29a and R 29b are both hydrogen.

[0309] In some embodiments, R 29a and R 29b each independently represents hydrogen or an optionally substituted Preferably it is unsubstituted alkyl.

[0310] In some embodiments, R 29a and R 29b are independently hydrogen, C 1 ~C 6 Alkyl , C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 alkoxyhalo, or -OH.

[0311] In some embodiments, R 29a or R 29b But -CH 3 , -CH 2 CH 3 , -OH , -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (I-II): Group R 21a and R 21b

[0312] In some embodiments, R 21a or R 21b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl.

[0313] In some embodiments, R 21a or R 21b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl.

[0314] In some embodiments, R 21a or R 21b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)RD1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0315] In some embodiments, R 21a and R 21b are both hydrogen.

[0316] In some embodiments, R 21a and R 21b each independently represents hydrogen or an optionally substituted Preferably it is unsubstituted alkyl.

[0317] In some embodiments, R 21a and R 21b each independently represents hydrogen, C 1 ~C 6 a Rukill, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, Or -OH.

[0318] In some embodiments, R 21a or R 21b But -CH 3 , -CH 2 CH 3 , -OH , -OCH 3 , or -CH(CH 3 ) 2 It is.

[0319] In some embodiments, R 77 is a hydrogen at the cis position. 77 but , hydrogen in the trans position.

[0320] In some embodiments, R 77 is methyl in the cis position. 77 is a methyl in the trans position. Formula (I-II): Group R 23

[0321] In some embodiments, R 23 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted In some embodiments, R is a substituted alkenyl, or a substituted or unsubstituted alkynyl. 23 is a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. In terms of form, R 23 is substituted or unsubstituted alkyl.

[0322] In some embodiments, R 23 is hydrogen.

[0323] In some embodiments, R 23 is substituted alkyl. In some embodiments, R 23 but , unsubstituted alkyl.

[0324] In some embodiments, R 23 is methyl. Formula (I-II): Group R 29

[0325] In some embodiments, R 29 is hydrogen.

[0326] In some embodiments, R 29is substituted alkyl. In some embodiments, R 29 but , unsubstituted alkyl. In some embodiments, R 29 is methyl. In some embodiments, R 29 But, -OC H 3 In some embodiments, R 29 is ethyl. Formula (I-II): Group R 26a and R 26b

[0327] In some embodiments, R 26a and R 26b are independently hydrogen, halogen, or substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkyl It's Nil.

[0328] In some embodiments, R 26a and R 26b are independently hydrogen or a substituted or non- It is a substituted alkyl.

[0329] In some embodiments, R 26a and R 26b are independently hydrogen or substituted alkyl; be.

[0330] In some embodiments, R 26a and R 26b are independently hydrogen or unsubstituted alkyl In some embodiments, R 26a and R 26b is hydrogen. is R 26a is halo or alkyl, R 26b is hydrogen. So, R 26a and R 26b In some embodiments, both of R 26a Oh BiR26b In some embodiments, both of R 26a and R 26b One Together they form an oxo group. Formula (I-II): Group R 55a and R 55b

[0331] In some embodiments, R 55a or R 55b is a substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, -OR A1 , -SR A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC( =O)R A1 , -OC(=O)OR A1 , -C(=O)N(R A1 ) 2 , -OC(=O) S.R. A1 , or -OC(=O)N(R A1 ) 2 where R A1 Each existence is unique. In particular, hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic cyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. do.

[0332] In some embodiments, R 55a or R 55b is a substituted or unsubstituted alkyl, -C (O)R A1 , -OC(=O)R A1 , -C(=O)N(R A1 ) 2, or -OC(= O)OR A1 where R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted. Alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or is an unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl aryl, or substituted or unsubstituted heteroaryl.

[0333] In some embodiments, R 55a or R 55b But -C(O)R A1 where R A1 is a substituted alkyl. In some embodiments, the alkyl is substituted with a heteroaryl. In some embodiments, the alkyl is substituted with a 5-membered heteroaryl. Formula (I-II): Group R 33a and R 33b

[0334] In some embodiments, R 33a and R 33b each independently represents hydrogen, halogen, or substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl aryl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -SR A1 , - N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(= O)R A1 , or -OC(=O)OR A1 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or Unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0335] In some embodiments, R 33a and R 33b each independently represents hydrogen, halogen, or substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , Or -OC(=O)OR A1 where R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted aryl. or unsubstituted heteroaryl.

[0336] In some embodiments, R 33a and R 33b are each hydrogen.

[0337] In some embodiments, the compound has formula (I-IIa) or formula (I-IIab) [ka] or a pharma- ceutically acceptable salt thereof, Here, R 31 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, - OR A1 , -SR A1 , -N(R A1 ) 2 , -N(R A1 ), -OC(=O)R A1 , - OC(=O)OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -S C(=O)R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O) N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O )SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O ) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O) R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 Each of each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, Substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted substituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, Oxygen protecting group when bonded to oxygen atom, sulfur protecting group when bonded to sulfur atom, nitrogen atom or two R A1 The groups together are either substituted or forms an unsubstituted heterocyclic or heteroaryl ring; R A2 is substituted or unsubstituted Alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or is an unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl v is 0, 1, or 2; , d is 0, 1, 2, or 3.

[0338] In some embodiments, the compound has formula (I-IIb) or formula (I-IIbb): [ka] or a pharma- ceutically acceptable salt thereof, wherein the variable group is as defined by the formula (II) above. Ia) or as defined by formula (I-IIab).

[0339] In some embodiments, R 31 is a substituted or unsubstituted alkyl, substituted or unsubstituted a alkynyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted aryl, or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted hetero It is aryl.

[0340] In some embodiments, R 31 but, [ka] and Here, R 20 Each occurrence of is independently a halogen, -NO 2 , -CN, -OR GA , - N(R GA ) 2 , -C(=O)R GA , -C(=O)OR GA , -OC(=O)R GA , -OC(=O)OR GA , -C(=O)N(R GA ) 2 , -N(R GA )C(=O)R G A , -OC(=O)N(R GA ) 2 , -N(R GA )C(=O)OR GA , -S(=O) 2 R GA , -S(=O) 2 OR GA , -OS(=O) 2 R GA , -S(=O) 2 N(R G A ) 2 , or -N(R GA )S(=O) 2 R GA ;Substituted or unsubstituted C 1~6 Alki , substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~4 Carbocyclyl, substituted or unsubstituted 3- to 4-membered heterocycles Rill or two R's if necessary GA together with the intervening atom, forms an unsubstituted 3- to 4-membered carbocyclic or heterocyclic ring; Here, R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6Alkyl, Substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, when bonded to oxygen oxygen protecting group when bonded to nitrogen, nitrogen protecting group when bonded to nitrogen, or two R GA Motogasuke together with the remaining atoms form a substituted or unsubstituted carbocyclic or heterocyclic ring; where n is 0, 1, 2, 3, 4, or 5.

[0341] In some embodiments, R 31 but, [ka] and Here, R 20 Each occurrence of is independently a halogen, -NO 2 , -CN, -OR GA , - N(R GA ) 2 , -C(=O)R GA , -C(=O)OR GA , -OC(=O)R GA , -OC(=O)OR GA , -C(=O)N(R GA ) 2 , -N(R GA )C(=O)R G A , -OC(=O)N(R GA ) 2 , -N(R GA )C(=O)OR GA , -S(=O) 2 R GA , -S(=O) 2 OR GA , -OS(=O)2 R GA , -S(=O) 2 N(R G A ) 2 , or -N(R GA )S(=O) 2 R GA ;Substituted or unsubstituted C 1~6 Alki , substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~4 Carbocyclyl, substituted or unsubstituted 3- to 4-membered heterocycles Rill or two R's if necessary GA together with the intervening atom, forms an unsubstituted 3- to 4-membered carbocyclic or heterocyclic ring; Here, R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, Substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, when bonded to oxygen oxygen protecting group when bonded to nitrogen, nitrogen protecting group when bonded to nitrogen, or two R GA Motogasuke together with the remaining atoms form a substituted or unsubstituted carbocyclic or heterocyclic ring; e is It can be 0, 1, 2, 3, 4, or 5.

[0342] In some embodiments, the compound has formula (I-IId) or formula (I-IIdb): [ka] or a pharma- ceutically acceptable salt thereof, where v is 0, 1, 2, or 3; R 10 are independently halogen, alkyl , hydroxyl, or cyano.

[0343] In some embodiments, the compound has formula (I-IIe) or formula (I-IIeb): [ka] or a pharma- ceutically acceptable salt thereof, where n is 0, 1, 2, or 3; p is 0, 1, or 3; v is 0, 1, 2, or 3; R 5 each independently represents a halogen, an alkyl, a hydroxy It is either aryl or cyano.

[0344] In some embodiments, the compound has formula (I-IIf) or formula (I-IIfb): [ka] or a pharma- ceutically acceptable salt thereof, wherein v is 0, 1, 2, or 3. ;R 10 are independently hydrogen, halogen, substituted or unsubstituted alkyl, hydroxy It is either aryl or cyano.

[0345] In some embodiments, the compound has formula (I-IIg) or formula (I-IIgb): [ka] or a pharma- ceutically acceptable salt thereof, where v is 0, 1, 2, or 3; and each X is independently -C(R N )-, -C( R N )2 -, -O-, -S-, -N-, or N(R N )-where R N is independent Hydrogen, substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR GA , -C(=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N( R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do.

[0346] In some embodiments, the compound has formula (I-IIh) or formula (I-IIhb) [ka] or a pharma- ceutically acceptable salt thereof, where v is 0, 1, 2, or 3, and R 10 Each of the formulas is independently selected from halogen, a m is 0, 1, 2, or 3.

[0347] In some embodiments, the compound has formula (I-IIi) or formula (I-IIib) [ka] or a pharma- ceutically acceptable salt thereof, where v is 0, 1, 2, or 3; n is 0, 1, or 2; and each X is independently Then, -C(R N )-, -C(R N ) 2 -, -O-, -S-, -N-, or N(R N )-where R N are independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, C( =O)R GA , -C(=O)OR GA , -C(=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do.

[0348] In some embodiments, R 3 is methoxymethyl or ethoxymethyl.

[0349] In some embodiments, R 8 or R 13 -C(O)CH 3 If R 3 is replaced or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl aryl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted Preferably, the aryl is unsubstituted, or the heteroaryl is substituted or unsubstituted.

[0350] In some embodiments, the compound has the formula (I-IIj): [ka] or a pharma- ceutically acceptable salt thereof, where s is 0, 1, or 2; R 12 is -N(R ab ) 2 , -OR ab in where R ab each independently represents H, substituted or unsubstituted alkyl, -SO 2 (R 15 ), -C(O)R 15 where R 15 is a substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteraryl, cycloalkane, or a substituted or unsubstituted cycloalkane.

[0351] In some embodiments, R 8 or R 13 But -C(O)R A1 , -C(=O)N(RA 1 ) 2 where R A1 is a substituted alkyl.

[0352] In some embodiments, R 8 and R 13 together form an oxo (=O) group.

[0353] In some embodiments, the compound is selected from the group consisting of the compounds identified in Table I-1 below. Selected: [Table 1-1] [Table 1-2] [Table 1-3] [Table 1-4] [Table 1-5] [Table 1-6] [Table 1-7] [Table 1-8] [Table 1-9] [Table 1-10]

Table 1-11

Table 1-12

Table 1-13

Table 1-14

Table 2-1

Table 2-2

Table 2-3

Table 2-4

Table 2-5

Table 2-6

Table 3-1

Table 3-2

Table 3-3

Table 3-4

[0001] The formulas depicted herein refer to specific carbon atoms (C17, C3, C19, etc.). These references are well known and used in the industry, as set forth below: Based on the position of the carbon atoms according to steroid nomenclature: [ka] . For example, C17 refers to the 17th carbon, and C3 refers to the 3rd carbon. . It should be recognized that the stereochemistry of C17 can be depicted in any of the following equivalent ways: Is: [ka] .

[0002] In one aspect, the compound of formula (II-I) [ka] or a pharma- ceutically acceptable salt thereof, In formula (II-I), t is 1; n is 0, 1, or 2; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted C 2 ~C 6 Alki aryl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl; R 5 is hydrogen or methyl; R 6a and R 6beach independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted a is alkynyl or R 6a and R 6b together form an oxo (=O) group ; R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or Unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -SR A1 , -N(R A1 ) 2 , -N(R A1 ), -OC(=O)R A1 , -OC(=O ) OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC(=O) R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A 1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , - SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen protecting group when bonded to a sulfur atom; sulfur protecting group when bonded to a nitrogen atom In the case of nitrogen protecting group or two R A1 The groups taken together are substituted or unsubstituted. forming a heterocyclic or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl; Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl; R 1a , R 1b , R 2a , R 2b , R 2aa , R 2ab , R 3a , R 3b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , or R 12b Each of the following is independent: and hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or is unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted a Rucynyl, -OR D1, -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,or- NR D1 C(=O)R D1 where R D1 Each occurrence of may independently represent hydrogen, substitution, or or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl , substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or is unsubstituted aryl, or substituted or unsubstituted heteroaryl, when attached to an oxygen atom or a nitrogen protecting group when bonded to a nitrogen atom, or two R D1 The base taken together form a substituted or unsubstituted heterocyclic ring; or R 2a and R 2b , R 4a and R 4b , R 7a and R 7b , R 11a and R 11b , and R 12a and R 12b taken together to form an oxo (=O) group; Here, R 1a , R 1b , R 2a , R 2b , R 2aa , R 2ab , R 3a , R 3b , R 4 a , or R 4b at least one of is hydroxyl; R 15a , R 15b , R 16a , and R 16b Each of the groups is independently hydrogen, halo. aryl, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted aryl, is an unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl -OR A1 , -SR A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O )SR A1 , -OC(=O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O)O R A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S (=O) 2 OR A1 where R A1 Each occurrence of is independently hydrogen, substitution or Unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted substituted aryl, substituted or unsubstituted heteroaryl, oxygen protecting group when bonded to an oxygen atom , a sulfur protecting group when attached to a sulfur atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 or two R A1 The groups together are either substituted or forms an unsubstituted heterocyclic or heteroaryl ring; R A2 is substituted or unsubstituted Alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or is an unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl aryl, or substituted or unsubstituted heteroaryl; where n is 0, t is 1, and R 19 is methyl and R 5 is hydrogen and R 3a is hydroxyl, ring B has a double bond, and R 6a , R 6b , R 1a , R 1b , R 2a , R 2b , R 2aa , R 2ab , R 3b , R 4a , R 4b , R 7a , R 7b , R 1 1a , R 11b , R 12a , R 12b , R 15a , R 15b , R 16a , and R 16b When each is hydrogen, R 1 is not methyl; Where: [ka] represents a single bond or a double bond, and when a double bond is present in ring B, R 6a or R 6 b One of and R 5 does not exist.

[0003] In some embodiments, the formula (II-II) [ka] or a pharma- ceutically acceptable salt thereof, The variables are defined as described in formula (II-I); 1a , R 1b , R 2a , R 2b , R 3a , or R 3b At least one of is hydroxyl.

[0004] In some embodiments, n is 1. In other embodiments, n is 2. Formula (II-I) and Formula (II-II): Group R 3a and R 3b

[0005] In some cases, R 3a and R 3b are each independently hydrogen, halogen, cyano, nitro thiol, azido, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene nyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -O R D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2, or -NR D1 C(= O)R D1 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted aryl. substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyl, Unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; or R 3a and R 3b Together This forms an oxo (=O).

[0006] In some cases, R 3a and R 3b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl.

[0007] In some cases, R 3a and R 3b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. .

[0008] In some cases, R 3a and R 3b are both hydrogen.

[0009] In some embodiments, R 3a and R 3b each independently represents hydrogen or a substituted or It is an unsubstituted alkyl.

[0010] In some embodiments, R 3a and R 3b each independently represents hydrogen, C 1 ~C 6 Alki Lu, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, also is -OH.

[0011] In some embodiments, R 3a and R 3b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II-I) and Formula (II-II): Group R 2a and R 2b

[0012] In some cases, R 2a and R 2b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC( =O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and , where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted or unsubstituted heteroaryl.

[0013] In some cases, R 2a and R 2b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl.

[0014] In some cases, R 2a and R 2b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(RD1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. .

[0015] In some cases, R 2a and R 2b are both hydrogen.

[0016] In some embodiments, R 2a and R 2b each independently represents hydrogen or a substituted or is unsubstituted alkyl.

[0017] In some embodiments, R 2a and R 2b each independently represents hydrogen, C 1 ~C 6 Alki Lu, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, also is -OH.

[0018] In some embodiments, R 2a and R 2b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II-I): group R 2aa and R 2ab

[0019] In some cases, R2aa and R 2ab are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -O C(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 in where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0020] In some cases, R 2aa and R 2ab are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl.

[0021] In some cases, R 2aa and R 2ab each independently represents hydrogen, a substituted or unsubstituted Substituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; be.

[0022] In some cases, R 2aa and R 2ab are both hydrogen.

[0023] In some embodiments, R 2aa and R 2ab each independently represents hydrogen or an optionally substituted Preferably it is unsubstituted alkyl.

[0024] In some embodiments, R 2aa and R 2ab each independently represents hydrogen, C 1 ~C 6 a Rukill, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, Or -OH. In some embodiments, R 2aa and R 2ab But -CH 3 , -CH 2 CH 3 , -OH, -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II-I) and Formula (II-II): Group R 1a and R1b

[0025] In some cases, R 1a and R 1b are each independently hydrogen, halogen, cyano, nitro thiol, azido, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene nyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -O R D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(= O)R D1 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted aryl. substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyl, Unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

[0026] In some cases, R 1a and R 1b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl.

[0027] In some cases, R1a and R 1b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. .

[0028] In some cases, R 1a and R 1b are both hydrogen.

[0029] In some embodiments, R 1a and R 1b each independently represents hydrogen or a substituted or It is an unsubstituted alkyl.

[0030] In some embodiments, R 1a and R 1b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or -O It's H. In some embodiments, R 1a and R 1b But -CH 3 , -CH 2 CH 3 , -OH, -O CH 3 , or -CH(CH 3 ) 2It is. Formula (II-I): group R 4a and R 4b

[0031] In some cases, R 4a and R 4b are each independently hydrogen, halogen, cyano, nitro thiol, azido, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene nyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -O R D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(= O)R D1 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted aryl. substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyl, Unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

[0032] In some cases, R 4a and R 4b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl.

[0033] In some cases, R 4a and R 4b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. .

[0034] In some cases, R 4a and R 4b and R are both hydrogen. 16a and R 16b are each independently hydrogen or substituted or unsubstituted alkyl; .

[0035] In some cases, R 4a and R 4b each independently represents hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or - In some other aspects, R 4a and R 4b But -CH 3 , -CH 2 CH 3 , -OH, -OCH 3 , or -CH(CH 3 )2 It is. Formula (II-I) and Formula (II-II): Group R 11a and R 11b

[0036] In some embodiments, R 11a and R 11b are each independently hydrogen, halogen, silyl Ano, nitro, azido, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl le, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D 1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or Unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted substituted aryl, or substituted or unsubstituted heteroaryl.

[0037] In some further embodiments, R 11a and R 11b each independently represents hydrogen, halo aryl, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene Nil, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl aryl, or substituted or unsubstituted heteroaryl.

[0038] In some cases, R 11a and R 11b each independently represents hydrogen, a substituted or unsubstituted Substituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; In some cases, R 11a and R 11b are both hydrogen.

[0039] In some cases, R 11a and R 11b each independently represents hydrogen or a substituted or In some aspects, R 11a and R 11b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Arco It is -xyhalo, or -OH.

[0040] In some cases, R 11a and R 11b But -CH 3 , -CH 2 CH 3, -OH, - OCH 3 , or -CH(CH 3 ) 2 It is.

[0041] In some embodiments, R 11a and R 11b together to form oxo (=O) do. Formula (II-I) and Formula (II-II): Group R 15a and R 15b

[0042] In some cases, R 15a and R 15b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -O C(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 in where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0043] In some embodiments, R 15a and R 15b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(RD1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl.

[0044] In some embodiments, R 15a and R 15b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0045] In some further embodiments, R 15a and R 15b are both hydrogen.

[0046] In some cases, R 15a and R 15b each independently represents hydrogen or a substituted or In some aspects, R 15a and R 15b Each of these independently represents water. Basic, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 In some aspects, R 15a and R 15b but,- CH 3 , -CH 2 CH 3 , -OH, -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II-I) and Formula (II-II): Group R 16a and R 16b

[0047] In some cases, R 16a and R 16b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -O C(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 in where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0048] In some embodiments, R 16a and R 16b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2, or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl.

[0049] In some embodiments, R 16a and R 16b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0050] In some further embodiments, R 16a and R 16b are both hydrogen.

[0051] In some cases, R 16a and R 16b each independently represents hydrogen or a substituted or In some aspects, R 16a and R 16b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6Arco It is -xyhalo, or -OH.

[0052] In some cases, R 16a and R 16b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (II-I) and Formula (II-II): Group R 7a and R 7b

[0053] In some embodiments, R 7a and R 7b are each independently hydrogen, halogen, or cyano. , nitro, azido, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted aryl alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C (=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted. substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted a aryl, or substituted or unsubstituted heteroaryl, or R 7a and R 7b taken together to form an oxo (=O).

[0054] In some further embodiments, R 7a and R 7b are each independently hydrogen, halogen , cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl , -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 and here R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted Substituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

[0055] In some cases, R 7a and R 7b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. .

[0056] In some cases, R 7a and R 7b All of the is hydrogen.

[0057] In some cases, R 7a and R 7b each independently represents hydrogen or a substituted or unsubstituted In some aspects, R 7a and R 7b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo , or -OH.

[0058] In some cases, R 7a and R 7b But -CH 3 , -CH 2 CH 3 , -OH, -OC H 3 , or -CH(CH 3 ) 2 It is.

[0059] In some embodiments, R 7a and R 7b When either of these is combined, it forms an oxo (=O) Form. Formula (II-I) and Formula (II-II): Group R 5

[0060] In some cases, R 5 is a hydrogen cis to C19. , R 5 is a hydrogen trans to C19. 5 , C1 In some further embodiments, R 5 But C19th place In contrast, it is methyl in the trans position. Formula (II-I) and Formula (II-II): Group R 19

[0061] In some cases, R 19 is hydrogen.

[0062] In other embodiments, R 19 is a substituted alkyl.

[0063] In other embodiments, R 19 But substitution C2 ~C 6 In another embodiment, R 19 But non-substituted C 2 ~C 6 It is an alkyl.

[0064] In other embodiments, R 19 is substituted alkenyl. In other embodiments, R 19 but, It is an unsubstituted alkenyl.

[0065] In other embodiments, R 19 is substituted alkynyl. In other embodiments, R 19 but, It is an unsubstituted alkynyl.

[0066] In some embodiments, R 19 Deuterium substituted C 2 -C 6 Alkyl .

[0067] In some embodiments, R 19 is ethyl. Formula (II-I) and Formula (II-II): Group R 6a and R 6b

[0068] In some embodiments, R 6a and R 6b are independently hydrogen, halogen, substituted or Unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl It is.

[0069] In some cases, R 6a and R 6b are independently hydrogen or substituted or unsubstituted alkoxy. It's a kill.

[0070] In some cases, R 6a and R 6b are independently hydrogen or substituted alkyl. In some embodiments, R 6aand R 6b is independently hydrogen or unsubstituted alkyl.

[0071] In some cases, R 6a and R 6b are hydrogen. In some aspects, R 6a but , halo or alkyl; R 6b is hydrogen. In some embodiments, R 6a Oh BiR 6b Both are halos.

[0072] In some cases, R 6a and R 6b are both alkyl.

[0073] In some embodiments, R 6a and R 6b together form an oxo group. Formula (II-I) and Formula (II-II): Group R 12a and R 12b

[0074] In some embodiments, R 12a and R 12b are each independently hydrogen, halogen, silyl Ano, nitro, azido, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl le, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D 1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or Unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted substituted aryl, or substituted or unsubstituted heteroaryl.

[0075] In some cases, R 12a and R 12b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl.

[0076] In some embodiments, R 12a and R 12b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is.

[0077] In some embodiments, R 12a and R 12b are both hydrogen.

[0078] In some further embodiments, R 12a and R 12b are each independently hydrogen or It is a substituted or unsubstituted alkyl.

[0079] In some embodiments, R 12a and R 12b together form an oxo group (=O) do.

[0080] In some embodiments, ring A is [ka] is selected from the group consisting of Where: [ka] indicates that ring A is bonded to ring B.

[0081] In some embodiments, R 1 is a substituted or unsubstituted alkyl, aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heptyl. It is a teraryl.

[0082] In some embodiments, R 1 but, [ka] and Here, R 20 Each occurrence of is independently a halogen, -NO 2 , -CN, -OR GA , - N(R GA ) 2 , -C(=O)R GA , -C(=O)OR GA , -OC(=O)RGA , -OC(=O)OR GA , -C(=O)N(R GA ) 2 , -N(R GA )C(=O)R G A , -OC(=O)N(R GA ) 2 , -N(R GA )C(=O)OR GA , -S(=O) 2 R GA , -S(=O) 2 OR GA , -OS(=O) 2 R GA , -S(=O) 2 N(R G A ) 2 , or -N(R GA )S(=O) 2 R GA ;Substituted or unsubstituted C 1~6 Alki , substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~4 Carbocyclyl, substituted or unsubstituted 3- to 4-membered heterocycles Rill or two R's if necessary GA together with the intervening atom, forms an unsubstituted 3- to 4-membered carbocyclic or heterocyclic ring; Here, R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, Substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, when bonded to oxygen oxygen protecting group when bonded to nitrogen, nitrogen protecting group when bonded to nitrogen, or two R GA Motogasuke together with the remaining atoms form a substituted or unsubstituted carbocyclic or heterocyclic ring; e is n is 0, 1, 2, 3, 4, or 5.

[0083] In some embodiments, R 1 but, [ka] and Here, R 20 Each occurrence of is independently hydrogen, halogen, -NO 2 , -CN, -OR G A , -N(R GA ) 2 , -C(=O)R GA , -C(=O)OR GA , -OC(=O)R GA , -OC(=O)OR GA , -C(=O)N(R GA ) 2 , -N(R GA )C(=O )R GA , -OC(=O)N(R GA ) 2 , -N(R GA )C(=O)OR GA , -S( =O) 2 R GA , -S(=O) 2 OR GA , -OS(=O) 2 R GA , -S(=O) 2 N (R GA ) 2 , or -N(R GA )S(=O) 2 R GA ;Substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alki Nyl, substituted or unsubstituted C 3~4 Carbocyclyl, substituted or unsubstituted 3- or 4-membered heptane or optionally with two R GA together with the intervening atom, or forms an unsubstituted 3- to 4-membered carbocyclic or heterocyclic ring; Here, R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, Substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, when bonded to oxygen oxygen protecting group when bonded to nitrogen, nitrogen protecting group when bonded to nitrogen, or two R GA Motogasuke together with the remaining atoms form a substituted or unsubstituted carbocyclic or heterocyclic ring; e is n is 0, 1, 2, 3, 4, or 5.

[0084] In some embodiments, the compound has formula (II-Ia), (II-Iab) or (II- Iac) [ka] or a pharma- ceutically acceptable salt thereof.

[0085] In some embodiments, the compound has formula (II-Ib), (II-Ibb) or (II- Ibc) [ka] or a pharma- ceutically acceptable salt thereof.

[0086] In some embodiments, the compound has formula (II-Ic), (II-Icb), or (II- Icc) [ka] or a pharma- ceutically acceptable salt thereof.

[0087] In some embodiments, the compound has formula (II-Ie), (II-Ieb), or (II- Iec) [ka] or a pharma- ceutically acceptable salt thereof, where m is 0, 1, 2, or 3; p is 0, 1, or 3; R 32 Each of is independently halogen, alkyl, hydroxyl, or cyano.

[0088] In some embodiments, the compound has formula (II-Ig), (II-Igb), or (II- Igc) [ka] is a compound of where u is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -S-, -N-, or N(R N )-where R N are independently hydrogen, Substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR GA , -C (=O)N(RGA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with or a pharma- ceutically acceptable salt thereof.

[0089] In some embodiments, the compound has the formula (II-Ieg), (II-Iegb), or (II I-Iegc) [ka] is a compound of where u is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -S-, -N-, or N(R N )-where R N are independently hydrogen, Substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR GA , -C (=O)N(R GA) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with or a pharma- ceutically acceptable salt thereof.

[0090] In some embodiments, the compound has formula (II-Ih), (II-Ihb), or (II- IHC) [ka] or a pharma- ceutically acceptable salt thereof, wherein R 35 Each of the following is independently aryl, alkyl, hydroxyl, or cyano; r is 0, 1, 2, or 3. be.

[0091] In some embodiments, the compound has formula (II-Ii), (II-Iib) or (II- Iic) [ka] is a compound of where s is 0, 1, or 2; each X is independently -C(R N )-, -C(R N ) 2 -, -O-, -S-, -N-, or N(R N )-where R N is independent , hydrogen, substituted or unsubstituted C1-6 alkyl, C(=O)R GA , -C(=O)OR G A , -C(=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with or a pharma- ceutically acceptable salt thereof.

[0092] In some embodiments, the compound has formula (II-IIa) or (II-IIab) [ka] or a pharma- ceutically acceptable salt thereof.

[0093] In some embodiments, the compound has formula (II-IIb) or (II-IIbb) [ka] or a pharma- ceutically acceptable salt thereof.

[0094] In some embodiments, the compound has formula (II-IIc) or (II-IIcb) [ka] or a pharma- ceutically acceptable salt thereof.

[0095] In some embodiments, the compound has formula (II-IIe) or (II-IIeb) [ka] is a compound of where m is 0, 1, 2, or 3; p is 0, 1, or 3; R 32 each is independently halogen, alkyl, hydroxyl, or cyano; or a pharma- ceutically acceptable salt thereof.

[0096] In some embodiments, the compound has formula (II-IIg) or (II-IIgb): [ka] is a compound of where u is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -S-, -N-, or N(R N )-where R N are independently hydrogen, Substituted or unsubstituted C 1~6Alkyl, C(=O)R GA , -C(=O)OR GA , -C (=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with or a pharma- ceutically acceptable salt thereof.

[0097] In some embodiments, the compound has the formula (II-IIh) or (II-IIhb): [ka] or a pharma- ceutically acceptable salt thereof, Here, R 35 each independently represents a halogen, an alkyl, a hydroxyl, or a cyano. and r is 0, 1, 2, or 3.

[0098] In some embodiments, the compound has formula (II-IIi) or (II-IIib): [ka] is a compound of where v is 0, 1, 2, or 3; n is 0, 1, or 2; and each X is independently Then, -C(R N )-, -C(R N ) 2 -, -O-, -S-, -N-, or N(R N )-where R N are independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, C( =O)R GA , -C(=O)OR GA , -C(=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and;

[0099] R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with or a pharma- ceutically acceptable salt thereof. [000100] In some embodiments, the compound is selected from the group consisting of the compounds identified in Table II-1 below. Selected: [Table 4-1] [Table 4-2] [Table 4-3] [Table 4-4] [Table 4-5] [Table 4-6] [Table 4-7] [Table 4-8] [Table 4-9] [000101] In one aspect, the compound of formula (III-I) [ka] or a pharma- ceutically acceptable salt thereof, In formula (III-I), R 5 is hydrogen or a substituted or unsubstituted methyl (e.g., -CH 3 ) or [ka] If is a double bond, R 5 does not exist; R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; can be; R 19 is hydrogen, substituted or unsubstituted alkyl (e.g., substituted or unsubstituted C 1 -C 6 alkyl), substituted or unsubstituted alkenyl (e.g., substituted or unsubstituted C 2 -C 6 alkenyl), or substituted or unsubstituted alkynyl (e.g., substituted or unsubstituted C 2 -C 6 alkynyl); R 6a and R 6b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted a is alkynyl or R 6a and R 6b together form an oxo (=O) group ; R 1a , R 1b , R 12a , R 12b , R 2a , R 2b , R 4a , R 4b , R 11a , R 11b , R 18a , and R 18b Each of the groups is independently hydrogen, halogen, cyano, hydride. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1, -OC(= O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; In the case of nitrogen protecting group or two R D1 The groups taken together are substituted or unsubstituted form a monocyclic ring; or R 1a and R 1b , R 12a and R 12b , R 2a oh YobiR 2b , R 4a and R 4b , R 11a and R 11b , and R 18a and R 18b taken together to form an oxo (=O) group; R 7a , R 7b , R 7aa , and R 7bb Each of the groups is independently selected from hydrogen, halogen, and sialic acid. hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , - OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1C(=O)R D1 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or Substituted or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; Nitrogen protecting group for binding or two R D1 The groups taken together are substituted or forming an unsubstituted heterocyclic ring; or R 7a and R 7b And R 7aa and R 7bb taken together to form an oxo (=O) group; R 16a , R 16b , R 17a , and R 17b Each of the groups is independently hydrogen, halo. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted substituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -S R A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -OC(= O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O)ORA1 , -SC(=O) S.R. A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O) OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O ) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 Yes Here, R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aryl is an unsubstituted heteroaryl, an oxygen protecting group when bonded to an oxygen atom, or a sulfur protecting group when bonded to a sulfur atom. a sulfur protecting group when attached to a nitrogen atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 or two R A1 The groups taken together form a substituted or unsubstituted heterocyclic ring or or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl, substituted or Unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or is unsubstituted heteroaryl, or R 17a and R 17b Together, Oxo Forming a base; Where: [ka] represents a single or double bond, and when a double bond is present, R 5 and R 6a or R 6b One of them does not exist. [000102] In one aspect, the compound of formula (III-I) [ka] or a pharma- ceutically acceptable salt thereof, In formula (III-I), R 5 is hydrogen or a substituted or unsubstituted methyl (e.g., -CH 3 ) or [ka] If is a double bond, R 5 does not exist; R 3 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or Unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R 19 is a substituted or unsubstituted alkyl (e.g., substituted or unsubstituted C 1 -C 6 Al alkyl), substituted or unsubstituted alkenyl (e.g., substituted or unsubstituted C 2 -C 6 Arke yl), or substituted or unsubstituted alkynyl (e.g., substituted or unsubstituted C 2 -C 6 alkynyl); R 6a and R 6b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted a is alkynyl or R 6a and R 6b together form an oxo (=O) group ; R 1a , R 1b , R 12a , R 12b , R 2a , R 2b , R 4a , R 4b , R 11a , R 11b , R 18a , and R 18b Each of the groups is independently hydrogen, halogen, cyano, hydride. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(= O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; In the case of nitrogen protecting group or two R D1 The groups taken together are substituted or unsubstituted form a homocyclic ring; or R 1a and R 1b , R 12a and R 12b , R 2a oh YobiR 2b , R 4a and R 4b , R 11a and R 11b , and R 18a and R 18b taken together to form an oxo (=O) group; R 7a , R 7b , R 7aa , and R 7bb Each of the groups is independently selected from hydrogen, halogen, and sialic acid. hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , - OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or Substituted or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; Nitrogen protecting group for binding or two R D1 The groups taken together are substituted or forming an unsubstituted heterocyclic ring; or R 7a and R 7b And R 7aa and R 7bb taken together to form an oxo (=O) group; R 16a , R 16b , R 17a , and R 17b Each of the groups is independently hydrogen, halo. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted substituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -S R A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -OC(= O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O)OR A1 , -SC(=O) S.R. A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O) OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O ) 2 R A2, -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 Yes Here, R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aryl is an unsubstituted heteroaryl, an oxygen protecting group when bonded to an oxygen atom, or a sulfur protecting group when bonded to a sulfur atom. a sulfur protecting group when attached to a nitrogen atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 or two R A1 The groups taken together form a substituted or unsubstituted heterocyclic ring or or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl, substituted or Unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or is unsubstituted heteroaryl, or R 17a and R 17b Together, Oxo Forming a base; Where: [ka] represents a single or double bond, and when a double bond is present, R 5 and R6a or R 6b One of them does not exist. [000103] In one aspect, the compound of formula (III-II) [ka] or a pharma- ceutically acceptable salt thereof, In formula (III-II), R 5 is hydrogen or a substituted or unsubstituted methyl (e.g., -CH 3 ) or [ka] If is a double bond, R 5 does not exist; R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; can be; R 6a and R 6b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted a is alkynyl or R 6a and R 6b together form an oxo (=O) group ; R 1a , R 1b , R 12a , R 12b , R 2a , R 2b , R 4a , R 4b , R 11a , R11b , R 18a , and R 18b Each of the groups is independently hydrogen, halogen, cyano, hydride. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(= O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; In the case of nitrogen protecting group or two R D1 The groups taken together are substituted or unsubstituted form a homocyclic ring; or R 1a and R 1b , R 12a and R 12b , R 2a oh YobiR 2b , R 4a and R 4b , R 11a and R 11b , and R 18a and R 18b taken together to form an oxo (=O) group; R 7a , R 7b , R 7aa , and R 7bb Each of the groups is independently selected from hydrogen, halogen, and sialic acid. hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , - OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or Substituted or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; Nitrogen protecting group for binding or two R D1 The groups taken together are substituted or forming an unsubstituted heterocyclic ring; or R 7a and R 7b And R 7aa and R 7bb taken together to form an oxo (=O) group; R 16a , R 16b , R 17a , and R 17b Each of the groups is independently hydrogen, halo. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted substituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -S R A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(RA1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -OC(= O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O)OR A1 , -SC(=O) S.R. A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O) OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O ) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 Yes Here, R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aryl is an unsubstituted heteroaryl, an oxygen protecting group when bonded to an oxygen atom, or a sulfur protecting group when bonded to a sulfur atom. a sulfur protecting group when attached to a nitrogen atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 or two R A1 The groups taken together form a substituted or unsubstituted heterocyclic ring or or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl, substituted or Unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or is unsubstituted heteroaryl; Where: [ka] represents a single or double bond, and when a double bond is present, R 5 and R 6a or R 6b One of them does not exist. Formula (III-I) and Formula (III-II): Group R 1a and R 1b [000104] In some cases, R 1a and R 1b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC( =O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and , where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted or unsubstituted heteroaryl. [000105] In some cases, R 1a and R 1b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl. [000106] In some cases, R 1a and R 1b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. . [000107] In some cases, R 1a and R 1b are both hydrogen. [000108] In some embodiments, R 1a and R 1b each independently represents hydrogen or a substituted or It is an unsubstituted alkyl. [000109] In some embodiments, R 1a and R 1b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or -O It's H. [000110] In some embodiments, R 1a and R 1b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (III-I) and Formula (III-II): Group R 2a and R 2b [000111] In some cases, R 2a and R 2b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC( =O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and , where R D1Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted or unsubstituted heteroaryl. [000112] In some cases, R 2a and R 2b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl. [000113] In some cases, R 2a and R 2b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. . [000114] In some cases, R 2a and R 2b are both hydrogen. [000115] In some embodiments, R 2a and R 2b each independently represents hydrogen or a substituted or It is an unsubstituted alkyl. [000116] In some embodiments, R 2a and R 2b each independently represents hydrogen, C 1 ~C 6 Alki Lu, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, also is -OH. [000117] In some embodiments, R 2a and R 2b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (III-I) and Formula (III-II): Group R 4a and R 4b [000118] In some cases, R 4a and R 4b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC( =O)R D1 , -NH 2 , -N(R D1 )2 , or -NR D1 C(=O)R D1 and , where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted or unsubstituted heteroaryl. [000119] In some cases, R 4a and R 4b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl. [000120] In some cases, R 4a and R 4b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. . [000121] In some cases, R 4a and R 4b and R are both hydrogen. 4a and R 4b is each independently hydrogen or substituted or unsubstituted alkyl. [000122] In some cases, R 4a and R 4b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~ C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo or -OH In some other aspects, R 4a and R 4b But -CH 3 , -CH 2 CH 3 , -OH , -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (III-I) and Formula (III-II): Group R 11a and R 11b [000123] In some embodiments, R 11a and R 11b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)RD1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl. [000124] In some further embodiments, R 11a and R 11b each independently represents hydrogen, halo aryl, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene Nil, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl aryl, or substituted or unsubstituted heteroaryl. [000125] In some cases, R 11a and R 11b each independently represents hydrogen, a substituted or unsubstituted Substituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,or -NR D1 C(=O)R D1 where R D1Each occurrence of is independently hydrogen, substitution or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; In some cases, R 11a and R 11b are both hydrogen. [000126] In some cases, R 11a and R 11b each independently represents hydrogen or a substituted or In some aspects, R 11a and R 11b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Arco It is -xyhalo, or -OH. [000127] In some cases, R 11a and R 11b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. [000128] In some embodiments, R 11a and R 11b together to form oxo (=O) do. Formula (III-I) and Formula (III-II): Group R 16a and R 16b [000129] In some cases, R 16a and R 16b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -O C(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 in where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. [000130] In some embodiments, R 16a and R 16b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl. [000131] In some embodiments, R 16a and R 16b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1, -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is. [000132] In some further embodiments, R 16a and R 16b are both hydrogen. [000133] In some cases, R 16a and R 16b each independently represents hydrogen or a substituted or In some aspects, R 16a and R 16b Each of these independently represents water. Basic, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or -OH. [000134] In some cases, R 16a and R 16b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (III-I) and Formula (III-II): Group R 7a , R 7b , R 7aa , and R 7 bb [000135] In some embodiments, R 7a , R 7b , R 7aa , and R 7bb However, each independently, Hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted Substituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkyl Nil, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, a substitution or is unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted substituted aryl, or substituted or unsubstituted heteroaryl, or R 7a and R 7b , or R 7aa and R 7bb together form oxo (=O). [000136] In some further embodiments, R 7a , R 7b , R 7aa , and R 7bb However, each In particular, hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkyl, or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N( R D1 ) 2 where RD1 Each occurrence is independently hydrogen, substituted or unsubstituted aryl. alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted aryl, or substituted or unsubstituted heteroaryl. [000137] In some cases, R 7a , R 7b , R 7aa , and R 7bb are each independently hydrogen , substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N( R D1 ) 2 , or -NR D1 C(=O)R D1 where R D1 Each existence is unique. In particular, hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted substituted heteroaryl. [000138] In some cases, R 7a , R 7b , R 7aa , and R 7bb All of the is hydrogen. [000139] In some cases, R 7a , R 7b , R 7aa , and R 7bb are each independently hydrogen or substituted or unsubstituted alkyl. In some aspects, R 7a , R 7b , R 7aa , and R 7bb each independently represents hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6Hello Aruki Lu, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or -OH. [000140] In some cases, R 7a , R 7b , R 7aa , and R 7bb But -CH 3 , -CH 2 CH 3 , -OH, -OCH 3 , or -CH(CH 3 ) 2 It is. [000141] In some embodiments, R 7a and R 7b or R 7aa and R 7bb Either Together they form an oxo (=O). Formula (III-I) and Formula (III-II): Group R 5 [000142] In some cases, R 5 is a hydrogen atom at the cis position. In some other aspects, R 5 But, Tran In some embodiments, R 5 However, it is a methyl group at the cis position. In certain embodiments, R 5 is a methyl in the trans position. Formula (III-I) and Formula (III-II): Group R 3 [000143] In some embodiments, R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted substituted alkenyl, or substituted or unsubstituted alkynyl. [000144] In some embodiments, R 3 is a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is a rule. [000145] In some embodiments, R 3 is substituted or unsubstituted alkyl. [000146] In some embodiments, R 3 is hydrogen. In some embodiments, R 3 is a substituted alkyl In some embodiments, R 3 is unsubstituted alkyl. In some embodiments, R 3 is methyl. Formula (III-I): Group R 19 [000147] In some cases, R 19 is hydrogen. [000148] In some embodiments, R 19 is substituted alkyl. In some embodiments, R 19 but , unsubstituted alkyl. [000149] In some embodiments, R 19 is methyl. In some embodiments, R 19 But -O CH 3 In some cases, R 19 is ethyl. Formula (III-I) and Formula (III-II): Group R 6a and R 6b [000150] In some embodiments, R 6a and R 6b are independently hydrogen, halogen, substituted or Unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl It is. [000151] In some cases, R6a and R 6b are independently hydrogen or substituted or unsubstituted alkoxy. It's a kill. [000152] In some cases, R 6a and R 6b are independently hydrogen or substituted alkyl. In some embodiments, R 6a and R 6b is independently hydrogen or unsubstituted alkyl. [000153] In some cases, R 6a and R 6b are hydrogen. In some aspects, R 6a but , halo or alkyl; R 6b is hydrogen. In some embodiments, R 6a Oh BiR 6b Both are halos. [000154] In some cases, R 6a and R 6b are both alkyl. [000155] In some embodiments, R 6a and R 6b together form an oxo group. Formula (III-I) and Formula (III-II): Group R 12a and R 12b [000156] In some embodiments, R 12a and R 12b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NRD1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl. [000157] In some cases, R 12a and R 12b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl. [000158] In some embodiments, R 12a and R 12b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is. [000159] In some embodiments, R 12a and R 12b are both hydrogen. [000160] In some further embodiments, R 12a and R 12b are each independently hydrogen or is substituted or unsubstituted alkyl. [000161] In some embodiments, R 12a and R 12b together form an oxo group (=O) do. Formula (III-I) and Formula (III-II): Group R 17a and R 17b [000162] In some cases, R 17a and R 17b is a substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, -OR A1 , -SR A1 , -N (R A1 ) 2 , -N(R A1 ), -C(O)R A1 , -OC(=O)R A1 , -OC(= O)OR A1 , -C(=O)N(R A1 ) 2 , -OC(=O)SR A1 , or -OC( =O)N(R A1 ) 2 where R A1 Each occurrence of is independently hydrogen, a substitution or is unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted It is a substituted aryl, or a substituted or unsubstituted heteroaryl. [000163] In some embodiments, R 17a and R 17b is a substituted or unsubstituted alkyl, -C (O)R A1 , -OC(=O)R A1 , or -OC(=O)OR A1 where R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted Alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted substituted heteroaryl. [000164] In some cases, R 17a and R 17b But -C(O)R A1 where R A1 is a substituted alkyl. [000165] In some embodiments, the alkyl is substituted with a heteroaryl. [000166] In some further embodiments, the alkyl is substituted with a 5-membered heteroaryl. Formula (III-I) and Formula (III-II): Group R 18a and R 18b [000167] In some embodiments, R 18a and R 18b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -ORD1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl. [000168] In some cases, R 18a and R 18b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl. [000169] In some embodiments, R 18a and R 18b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)RD1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is. [000170] In some embodiments, R 18a and R 18b are both hydrogen. [000171] In some further embodiments, R 18a and R 18b are each independently hydrogen or It is a substituted or unsubstituted alkyl. [000172] In some embodiments, R 18a and R 18b together form an oxo group (=O) do. Formula (III-I) [000173] In some embodiments, the compound has formula (III-Ia): [ka] or a pharma- ceutically acceptable salt thereof. [000174] In some embodiments, the compound has formula (III-Ib): [ka] or a pharma- ceutically acceptable salt thereof. [000175] In some embodiments, the compound has formula (III-Ic): [ka] or a pharma- ceutically acceptable salt thereof. [000176] In some embodiments, the compound has formula (III-Id): [ka] or a pharma- ceutically acceptable salt thereof. [000177] In some embodiments, the compound has formula (III-Ie): [ka] or a pharma- ceutically acceptable salt thereof. [000178] In some embodiments, the compound has formula (III-If): [ka] or a pharma- ceutically acceptable salt thereof, R 1 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl le, -OR A1 , -SR A1 , -N(R A1 ) 2 , -OC(=O)R A1 , -OC(=O ) OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC(=O) R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)RA1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A 1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , - SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen protecting group when bonded to a sulfur atom; sulfur protecting group when bonded to a nitrogen atom In the case of nitrogen protecting group or two R A1 The groups taken together are substituted or unsubstituted. forming a heterocyclic or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl; Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is substituted or unsubstituted heteroaryl; and n is 0, 1, or 2. [000179] In some embodiments, the compound has formula (III-Ig): [ka] or a pharma- ceutically acceptable salt thereof, R 1 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl le, -OR A1 , -SR A1 , -N(R A1 ) 2 , -OC(=O)R A1 , -OC(=O ) OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC(=O) R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A 1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , - SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen protecting group when bonded to a sulfur atom; sulfur protecting group when bonded to a nitrogen atom In the case of nitrogen protecting group or two R A1 The groups taken together are substituted or unsubstituted. forming a heterocyclic or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl; Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is substituted or unsubstituted heteroaryl; and n is 0, 1, 2, or 3. [000180] In some embodiments, the compound has the formula (III-Ih): [ka] or a pharma- ceutically acceptable salt thereof, where u is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -S-, -N-, or N(R N )-where R N are independently hydrogen, Substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR GA , -C (=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O)2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do. [000181] In some embodiments, the compound has formula (III-Ii): [ka] or a pharma- ceutically acceptable salt thereof, where u is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -S-, -N-, or N(R N )-where R N are independently hydrogen, Substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR GA , -C (=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do. [000182] In some embodiments, the compound has formula (III-Ij): [ka] or a pharma- ceutically acceptable salt thereof, where m is 0, 1, 2, or 3; n is 0, 1, 2, or 3; R 21 is independently halogen, alkyl, hydroxyl, or cyano. [000183] In some embodiments, the compound has formula (III-Ik): [ka] or a pharma- ceutically acceptable salt thereof, where m is 0, 1, 2, or 3; n is 0, 1, or 2; R 21 Each of is independently halogen, alkyl, hydroxyl, or cyano. [000184] In some embodiments, R 21 In some embodiments, m is 1 and n is 1. [000185] In some embodiments, the compound has formula (III-IL): [ka] or a pharma- ceutically acceptable salt thereof. [000186] In some embodiments, the compound has the formula (III-Im): [ka] or a pharma- ceutically acceptable salt thereof. [000187] In some embodiments, the compound of formula (III-I) is of formula (III-In) or formula (I II-Io) [ka] or a pharma- ceutically acceptable salt thereof, where s is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -O-, -S-, -N-, or N(R N )-where R N is independent , hydrogen, substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR G A , -C(=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do. Formula (III-II) [000188] In some embodiments, the compound has the formula (III-IIa): [ka] or a pharma- ceutically acceptable salt thereof. [000189] In some embodiments, the compound has the formula (III-IIb): [ka] or a pharma- ceutically acceptable salt thereof. [000190] In some embodiments, the compound has the formula (III-IIc): [ka] or a pharma- ceutically acceptable salt thereof. [000191] In some embodiments, the compound has the formula (III-IId): [ka] or a pharma- ceutically acceptable salt thereof. [000192] In some embodiments, the compound has the formula (III-IIe): [ka] or a pharma- ceutically acceptable salt thereof. [000193] In some embodiments, the compound has the formula (III-IIf): [ka] or a pharma- ceutically acceptable salt thereof, Here, R 1 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted Alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heptane ROARYL, -OR A1 , -SR A1 , -N(R A1 ) 2 , -OC(=O)R A1 , -O C(=O)OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC (=O)R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N (R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O) S.R. A1 , -NHC(=O)N(RA1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 The existence of each each independently represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid Oxygen protecting group when bonded to oxygen atom, sulfur protecting group when bonded to sulfur atom, nitrogen protecting group when bonded to nitrogen atom Nitrogen protecting group for binding or two R A1 The groups taken together are substituted or forming an unsubstituted heterocyclic or heteroaryl ring; R A2 is a substituted or unsubstituted substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyl, Unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl n is 0, 1, 2, or 3. do. [000194] In some embodiments, the compound has the formula (III-IIg): [ka] or a pharma- ceutically acceptable salt thereof, R 1 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl le, -OR A1 , -SR A1 , -N(R A1 ) 2 , -OC(=O)R A1 , -OC(=O ) OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC(=O) R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A 1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , - SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen protecting group when bonded to a sulfur atom; sulfur protecting group when bonded to a nitrogen atom In the case of nitrogen protecting group or two R A1 The groups taken together are substituted or unsubstituted. forming a heterocyclic or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl; Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is substituted or unsubstituted heteroaryl; and n is 0, 1, 2, or 3. [000195] In some embodiments, the compound has the formula (III-IIh): [ka] or a pharma- ceutically acceptable salt thereof, where u is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -S-, -N-, or N(R N )-where R N are independently hydrogen, Substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR GA , -C (=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do. [000196] In some embodiments, the compound has the formula (III-IIi): [ka] or a pharma- ceutically acceptable salt thereof, where u is 0, 1, or 2, and each X is independently -C(R N )-, -C(R N ) 2 -, -S-, -N-, or N(R N )-where R N are independently hydrogen, Substituted or unsubstituted C 1~6 Alkyl, C(=O)R GA , -C(=O)OR GA , -C (=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GAEach occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do. [000197] In some embodiments, the compound has the formula (III-IIj): [ka] or a pharma- ceutically acceptable salt thereof, where m is 0, 1, 2, or 3; n is 0, 1, or 2; R 21 is independently halogen, alkyl, hydroxyl, or cyano. [000198] In some embodiments, the compound has the formula (III-IIk): [ka] or a pharma- ceutically acceptable salt thereof, where m is 0, 1, 2, or 3; n is 0, 1, 2, or 3; R 21 Each of is independently halogen, alkyl, hydroxyl, or cyano. [000199] In some embodiments, R 21 In some embodiments, m is 1 and n is 1. [000200] In some embodiments, the compound has the formula (III-IIL): [ka] or a pharma- ceutically acceptable salt thereof. [000201] In some embodiments, the compound has the formula (III-IIm): [ka] or a pharma- ceutically acceptable salt thereof. [000202] In some embodiments, the compound has formula (III-IIn) or formula (III-IIo): [ka] or a pharma- ceutically acceptable salt thereof, where s is 0, 1, or 2; each X is independently -C(R N )-, -C(R N ) 2 -, -O-, -S-, -N-, or N(R N )-where R N is independent , hydrogen, substituted or unsubstituted C1-6 alkyl, C(=O)R GA , -C(=O)OR G A , -C(=O)N(R GA ) 2 , -S(=O) 2 R GA , or -S(=O) 2 N(R GA ) 2 and; R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, substituted or is unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, acid when bonded to oxygen a nitrogen protecting group when bonded to nitrogen, or a nitrogen protecting group when bonded to nitrogen, or two R GA The group is an intervening atom together with do. [000203] In some embodiments, R 1 is a substituted or unsubstituted alkyl, aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic alkyl, It's a reel. [000204] In some embodiments, R 1 but, [ka] and Here, R 20 Each occurrence of is independently a halogen, -NO 2 , -CN, -OR GA , - N(R GA ) 2 , -C(=O)R GA , -C(=O)OR GA , -OC(=O)R GA , -OC(=O)OR GA , -C(=O)N(R GA ) 2 , -N(R GA )C(=O)R G A , -OC(=O)N(R GA ) 2 , -N(R GA )C(=O)OR GA , -S(=O) 2 R GA , -S(=O) 2 OR GA , -OS(=O) 2 R GA , -S(=O) 2 N(R G A ) 2 , or -N(R GA )S(=O) 2 R GA ;Substituted or unsubstituted C 1~6 Alki , substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~4 Carbocyclyl, substituted or unsubstituted 3- to 4-membered heterocycles Rill or two R's if necessary GA together with the intervening atom, forms an unsubstituted 3- to 4-membered carbocyclic or heterocyclic ring; Here, R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, Substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, when bonded to oxygen oxygen protecting group when bonded to nitrogen, nitrogen protecting group when bonded to nitrogen, or two R GA Motogasuke together with the remaining atoms form a substituted or unsubstituted carbocyclic or heterocyclic ring; e is It can be 0, 1, 2, 3, 4, or 5. [000205] In some embodiments, R 1 but, [ka] and Here, R 20 Each occurrence of is independently a halogen, -NO 2 , -CN, -OR GA , - N(R GA ) 2 , -C(=O)R GA , -C(=O)OR GA , -OC(=O)R GA , -OC(=O)OR GA , -C(=O)N(R GA ) 2 , -N(R GA )C(=O)R G A , -OC(=O)N(R GA ) 2 , -N(R GA )C(=O)OR GA , -S(=O) 2 R GA , -S(=O) 2 OR GA , -OS(=O) 2 R GA , -S(=O) 2 N(R G A ) 2 , or -N(R GA )S(=O) 2 R GA ;Substituted or unsubstituted C 1~6 Alki , substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~4 Carbocyclyl, substituted or unsubstituted 3- to 4-membered heterocycles Rill or two R's if necessary GA together with the intervening atom, forms an unsubstituted 3- to 4-membered carbocyclic or heterocyclic ring; Here, R GA Each occurrence of is independently hydrogen, substituted or unsubstituted C 1~6 Alkyl, Substituted or unsubstituted C 2~6 Alkenyl, substituted or unsubstituted C 2~6 Alkynyl, Substituted or unsubstituted C 3~6 Carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, when bonded to oxygen oxygen protecting group when bonded to nitrogen, nitrogen protecting group when bonded to nitrogen, or two R GA Motogasuke together with the remaining atoms form a substituted or unsubstituted carbocyclic or heterocyclic ring; where n is 0, 1, 2, 3, 4, or 5. [000206] In one aspect, the compound of formula (IV-I): [ka] or a pharma- ceutically acceptable salt thereof, In formula (IV-I), R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] If is a double bond, R 5 does not exist; R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; can be; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or is substituted or unsubstituted alkynyl; R 6a and R 6b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted a is alkynyl or R 6a and R 6b together form an oxo (=O) group ; R 1a , R 1b , R 12a , R 12b , R 2a , R 2b , R 4a , R 4b , R 11a , R 11b , R 18a , and R 18b Each of the groups is independently hydrogen, halogen, cyano, hydride. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(= O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; In the case of nitrogen protecting group or two R D1 The groups taken together are substituted or unsubstituted form a homocyclic ring; or R 1a and R 1b , R 12a and R 12b , R 2a oh YobiR 2b , R 4a and R 4b , R 11a and R 11b , and R 18a and R 18b taken together to form an oxo (=O) group; R 16a , R 16b , R 17a , and R 17b Each of the groups is independently hydrogen, halo. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted substituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -S R A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -OC(= O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O)OR A1, -SC(=O) S.R. A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O) OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O ) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 Yes Here, R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aryl is an unsubstituted heteroaryl, an oxygen protecting group when bonded to an oxygen atom, or a sulfur protecting group when bonded to a sulfur atom. a sulfur protecting group when attached to a nitrogen atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 or two R A1 The groups taken together form a substituted or unsubstituted heterocyclic ring or or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl, substituted or Unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or is unsubstituted heteroaryl; Where: [ka] represents a single or double bond, and when a double bond is present, R 5 and R 6a or R 6b One of them does not exist. [000207] In one aspect, the compound of formula (IV-I): [ka] or a pharma- ceutically acceptable salt thereof, In formula (IV-I), R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] If is a double bond, R 5 does not exist; R 3 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or Unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R 19 is a substituted or unsubstituted alkyl (e.g., substituted or unsubstituted C 1 -C 6 Al alkyl), substituted or unsubstituted alkenyl (e.g., substituted or unsubstituted C 2 -C 6 Arke nyl), or substituted or unsubstituted alkynyl; R 6a and R 6b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted a is alkynyl or R 6a and R 6b together form an oxo (=O) group ; R 1a , R 1b , R 12a , R 12b , R 2a , R 2b , R 4a , R 4b , R 11a , R 11b , R 18a , and R 18b Each of the groups is independently hydrogen, halogen, cyano, hydride. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(= O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; In the case of nitrogen protecting group or two R D1 The groups taken together are substituted or unsubstituted form a monocyclic ring; or R 1aand R 1b , R 12a and R 12b , R 2a oh YobiR 2b , R 4a and R 4b , R 11a and R 11b , and R 18a and R 18b taken together to form an oxo (=O) group; R 16a , R 16b , R 17a , and R 17b Each of the groups is independently hydrogen, halo. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted substituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -S R A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -OC(= O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O)OR A1 , -SC(=O) S.R. A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O) OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2, -OS(=O ) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 Yes Here, R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aryl is an unsubstituted heteroaryl, an oxygen protecting group when bonded to an oxygen atom, or a sulfur protecting group when bonded to a sulfur atom. a sulfur protecting group when attached to a nitrogen atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 or two R A1 The groups taken together form a substituted or unsubstituted heterocyclic ring or or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl, substituted or Unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or is unsubstituted heteroaryl; Where: [ka] represents a single or double bond, and when a double bond is present, R 5 and R 6a or R 6b One of them does not exist. [000208] In one aspect, the compound of formula (IV-II): [ka] or a pharma- ceutically acceptable salt thereof, In formula (IV-II), R 5 is hydrogen or a substituted or unsubstituted methyl (e.g., -CH 3 ) or [ka] If is a double bond, R 5 does not exist; R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; can be; R 6a and R 6b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted a is alkynyl or R 6a and R 6b together form an oxo (=O) group ; R 1a , R 1b , R 12a , R 12b , R 2a , R 2b , R 4a , R 4b , R 11a , R 11b , R 18a, and R 18b Each of the groups is independently hydrogen, halogen, cyano, hydride. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(= O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or or unsubstituted heteroaryl; oxygen protecting group when bonded to an oxygen atom; In the case of nitrogen protecting group or two R D1 The groups taken together are substituted or unsubstituted form a homocyclic ring; or R 1a and R 1b , R 12a and R 12b , R 2a oh YobiR 2b , R 4a and R 4b , R 11a and R 11b , and R 18a and R 18b taken together to form an oxo (=O) group; R 16a , R 16b , R 17a , and R 17b Each of the groups is independently hydrogen, halo. aryl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted substituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -S R A1 , -N(R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -OC(= O)N(R A1 ) 2 , -SC(=O)R A2 , -SC(=O)OR A1 , -SC(=O) S.R. A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O) OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O ) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 Yes Here, R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aryl is an unsubstituted heteroaryl, an oxygen protecting group when bonded to an oxygen atom, or a sulfur protecting group when bonded to a sulfur atom. a sulfur protecting group when attached to a nitrogen atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 or two R A1 The groups taken together form a substituted or unsubstituted heterocyclic ring or or heteroaryl ring; R A2 is a substituted or unsubstituted alkyl, substituted or Unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or is unsubstituted heteroaryl; Where: [ka] represents a single or double bond, and when a double bond is present, R 5 and R 6a or R 6b One of them does not exist. [000209] In one aspect, the compound of formula (IV-III) [ka] Provided herein is a compound of the formula: In formula (IV-III), R 1 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted C, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -OR A1 , -SR A1 , -N(R A1 ) 2 , -OC(=O )R A1 , -OC(=O)OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A 1 ) 2 , -SC(=O)R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , - SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , - NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , -SO 2 R A2 , or -S(=O) 2 OR A1 where R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted Alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heptane aryl, oxygen protecting group when bonded to an oxygen atom, sulfur protecting group when bonded to a sulfur atom group, a nitrogen protecting group when attached to a nitrogen atom, or two RA1 The foundation comes together R forms a substituted or unsubstituted heterocyclic or heteroaryl ring; A2 also substitute or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl , substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or is unsubstituted aryl, or substituted or unsubstituted heteroaryl; R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; can be; R 19 is hydrogen, substituted or unsubstituted alkyl (e.g., substituted or unsubstituted C 1 -C 6 alkyl), substituted or unsubstituted alkenyl (e.g., substituted or unsubstituted C 2 -C 6 alkenyl), or substituted or unsubstituted alkynyl (e.g., substituted or unsubstituted C 2 -C 6 alkynyl). Formula (IV-I) and Formula (IV-II): Group R 1a and R 1b [000210] In some cases, R 1a and R 1b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC( =O)R D1 , -NH2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and , where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted or unsubstituted heteroaryl. [000211] In some cases, R 1a and R 1b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl. [000212] In some cases, R 1a and R 1b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. . [000213] In some cases, R 1a and R 1b are both hydrogen. [000214] In some embodiments, R 1a and R 1b each independently represents hydrogen or a substituted or It is an unsubstituted alkyl. [000215] In some embodiments, R 1a and R 1b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or -O It's H. [000216] In some embodiments, R 1a and R 1b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (IV-I) and Formula (IV-II): Group R 2a and R 2b [000217] In some cases, R 2a and R 2b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC( =O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and , where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted or unsubstituted heteroaryl. [000218] In some cases, R 2a and R 2b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl. [000219] In some cases, R 2a and R 2b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N RD1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. . [000220] In some cases, R 2a and R 2b are both hydrogen. [000221] In some embodiments, R 2a and R 2b each independently represents hydrogen or a substituted or It is an unsubstituted alkyl. [000222] In some embodiments, R 2a and R 2b each independently represents hydrogen, C 1 ~C 6 Alki Lu, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, also is -OH. [000223] In some embodiments, R 2a and R 2b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (IV-I) and Formula (IV-II): Group R 4a and R 4b [000224] In some cases, R 4a and R 4bare each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC( =O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 and , where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carboxyl aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted or unsubstituted heteroaryl. [000225] In some cases, R 4a and R 4b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carboxyl, aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted Or it is an unsubstituted heteroaryl. [000226] In some cases, R 4a and R 4b each independently represents hydrogen, a substituted or unsubstituted alkyl group, Rukill, -OR D1, -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -N R D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substituted or or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. . [000227] In some cases, R 4a and R 4b and R are both hydrogen. 4a and R 4b is each independently hydrogen or substituted or unsubstituted alkyl. [000228] In some cases, R 4a and R 4b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~ C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo or -OH In some other aspects, R 4a and R 4b But -CH 3 , -CH 2 CH 3 , -OH , -OCH 3 , or -CH(CH 3 ) 2 It is. Formula (IV-I) and Formula (IV-II): Group R 11a and R 11b [000229] In some embodiments, R 11aand R 11b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl. [000230] In some further embodiments, R 11a and R 11b each independently represents hydrogen, halo aryl, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkene Nil, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 and Here, R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or is an unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl aryl, or substituted or unsubstituted heteroaryl. [000231] In some cases, R 11a and R 11b each independently represents hydrogen, a substituted or unsubstituted Substituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,or -NR D1 C(=O)R D1 where R D1 Each occurrence of is independently hydrogen, substitution or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heptane aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; In some cases, R 11a and R 11b are both hydrogen. [000232] In some cases, R 11a and R 11b each independently represents hydrogen or a substituted or In some aspects, R 11a and R 11b are independently hydrogen, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Arco It is -xyhalo, or -OH. [000233] In some cases, R 11a and R 11b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. [000234] In some embodiments, R 11a and R 11b together to form oxo (=O) do. Formula (IV-I) and Formula (IV-II): Group R 16a and R 16b [000235] In some cases, R 16a and R 16b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -O C(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D1 in where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbo cyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. [000236] In some embodiments, R 16a and R 16b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, - OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or or substituted or unsubstituted heteroaryl. [000237] In some embodiments, R 16a and R 16b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is. [000238] In some further embodiments, R 16a and R 16b are both hydrogen. [000239] In some cases, R 16a and R 16b each independently represents hydrogen or a substituted or In some aspects, R 16a and R 16b Each of these independently represents water. Basic, C 1 ~C 6 Alkyl, C 1 ~C 6 Haloalkyl, C 1 ~C 6 Alkoxy, C 1 ~C 6 Alkoxyhalo, or -OH. [000240] In some cases, R 16a and R 16b But -CH 3 , -CH 2 CH 3 , -OH, - OCH 3 , or -CH(CH 3 ) 2 It is. Formula (IV-I) and Formula (IV-II): Group R 5 [000241] In some cases, R 5 is a hydrogen atom at the cis position. In some other aspects, R 5 But, Tran In some embodiments, R 5 However, it is a methyl group at the cis position. In certain embodiments, R 5 is a methyl in the trans position. Formula (IV-I), Formula (IV-II) and Formula (IV-III): Group R 3 [000242] In some embodiments, R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted substituted alkenyl, or substituted or unsubstituted alkynyl. [000243] In some embodiments, R 3 is a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is a rule. [000244] In some embodiments, R 3 is substituted or unsubstituted alkyl. [000245] In some embodiments, R 3 is hydrogen. In some embodiments, R 3 is a substituted alkyl In some embodiments, R 3 is unsubstituted alkyl. In some embodiments, R 3 is methyl. Formula (IV-I) and Formula (IV-III): Group R 19 [000246] In some cases, R 19 is hydrogen. [000247] In some embodiments, R 19 is substituted alkyl. In some embodiments, R 19 but , unsubstituted alkyl. [000248] In some embodiments, R 19 is methyl. In some embodiments, R 19 But -O CH 3 In some cases, R 19 is ethyl. Formula (IV-I) and Formula (IV-II): Group R 6a and R 6b [000249] In some embodiments, R 6a and R 6b are independently hydrogen, halogen, substituted or Unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl It is. [000250] In some cases, R 6a and R 6b are independently hydrogen or substituted or unsubstituted alkoxy. It's a kill. [000251] In some cases, R 6a and R 6b are independently hydrogen or substituted alkyl. In some embodiments, R 6a and R 6b is independently hydrogen or unsubstituted alkyl. [000252] In some cases, R 6a and R 6b are hydrogen. In some aspects, R 6a but , halo or alkyl; R 6bis hydrogen. In some embodiments, R 6a Oh BiR 6b Both are halos. [000253] In some cases, R 6a and R 6b are both alkyl. [000254] In some embodiments, R 6a and R 6b together form an oxo group. Formula (IV-I) and Formula (IV-II): Group R 12a and R 12b [000255] In some embodiments, R 12a and R 12b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl. [000256] In some cases, R 12a and R 12b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl. [000257] In some embodiments, R 12a and R 12b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is. [000258] In some embodiments, R 12a and R 12b are both hydrogen. [000259] In some further embodiments, R 12a and R 12b are each independently hydrogen or is substituted or unsubstituted alkyl. [000260] In some embodiments, R 12a and R 12btogether form an oxo group (=O) do. Formula (IV-I) and Formula (IV-II): Group R 17a and R 17b [000261] In some cases, R 17a and R 17b is a substituted or unsubstituted alkyl, or unsubstituted alkenyl, substituted or unsubstituted alkynyl, -OR A1 , -SR A1 , -N (R A1 ) 2 , -N(R A1 ), -CN(R A1 ) 2 , -C(O)R A1 , -OC(=O )R A1 , -OC(=O)OR A1 , -C(=O)N(R A1 ) 2 , -OC(=O)SR A1 , or -OC(=O)N(R A1 ) 2 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or Unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl aryl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl. [000262] In some embodiments, R 17a and R 17b is a substituted or unsubstituted alkyl, -C (O)R A1 , -OC(=O)R A1 , or -OC(=O)OR A1 where R A1 Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted Alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted substituted heteroaryl. [000263] In some cases, R 17a and R 17b But -C(O)R A1 where R A1 is a substituted alkyl. [000264] In some embodiments, the alkyl is substituted with a heteroaryl. [000265] In some further embodiments, the alkyl is substituted with a 5-membered heteroaryl. Formula (IV-I) and Formula (IV-II): Group R 18a and R 18b [000266] In some embodiments, R 18a and R 18b are each independently hydrogen, halogen, silyl Ano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 , or -NR D1 C(=O)R D 1 where R D1 each occurrence is independently hydrogen, substituted or unsubstituted alkyl, Substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbazole ruthenium, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or is a substituted or unsubstituted heteroaryl. [000267] In some cases, R 18a and R 18b are each independently hydrogen, halogen, or cyano. , hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, -OR D1 , -OC(=O)R D1 , -NH 2 , or -N(R D1 ) 2 where R D1 Each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbazole, bocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or It is a substituted or unsubstituted heteroaryl. [000268] In some embodiments, R 18a and R 18b each independently represents hydrogen, a substituent or Unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH 2 , -N(R D1 ) 2 ,Ma or-NR D1 C(=O)R D1 where R D1 each occurrence independently represents hydrogen, Substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl It is. [000269] In some embodiments, R 18a and R 18b are both hydrogen. [000270] In some further embodiments, R 18a and R18b are each independently hydrogen or It is a substituted or unsubstituted alkyl. [000271] In some embodiments, R 18a and R 18b together form an oxo group (=O) do. Formula (IV-I) [000272] In some embodiments, the compound has formula (IV-Ia): [ka] or a pharma- ceutically acceptable salt thereof. [000273] In some embodiments, the compound has formula (IV-Ib): [ka] or a pharma- ceutically acceptable salt thereof. [000274] In some embodiments, the compound has formula (IV-Ic): [ka] or a pharma- ceutically acceptable salt thereof. [000275] In some embodiments, the compound has formula (IV-Id): [ka] or a pharma- ceutically acceptable salt thereof. [000276] In some embodiments, the compound has formula (IV-Ie): [ka] or a pharma- ceutically acceptable salt thereof. [000277] In some embodiments, the compound has formula (IV-If): [ka] or a pharma- ceutically acceptable salt thereof, R 1 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl aryl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted Unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl le, -OR A1 , -SR A1 , -N(R A1 ) 2 , -OC(=O)R A1 , -OC(=O ) OR A1 , -OC(=O)SR A1 , -OC(=O)N(R A1 ) 2 , -SC(=O) R A2 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 ) 2 , -NHC(=O)R A1 , -NHC(=O)OR A1 , -NHC(=O)SR A1 , -NHC(=O)N(R A1 ) 2 , -OS(=O) 2 R A2 , -OS(=O) 2 OR A 1 , -SS(=O) 2 R A2 , -SS(=O) 2 OR A1 , -S(=O)R A2 , - SO 2 RA2 , or -S(=O) 2 OR A1 where R A1 Each existence is independent and hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or is unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclic aryl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, oxygen protecting group when bonded to a ...

Claims

1. Formula (I-I): 【Chemistry 424】 or a pharma- ceutically acceptable salt thereof, In formula (II), t is 1; R ７ is hydrogen; R ３ is a substituted or unsubstituted C １～３ is alkyl; R ９ is hydrogen or unsubstituted C １～３ is alkyl; R ５ａ , R ５ｂ , R ６ａ , R ６ｂ , R １１ａ , R １１ｂ , R １５ａ , R １５ｂ , R １６ａ , R １６ｂ , R １７ａ , R １７ｂ , R １８ａ , R １８ｂ , R １９ａ , or R １９ｂ each is hydrogen; R ８ and R １３ each independently represents hydrogen, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -SR Ａ１ , -N(R Ａ１ ) ２ , -C(O)R Ａ１ , -C(=O)N(R Ａ１ ) ２ , -OC(=O)R Ａ１ , -OC(=O)OR Ａ１ , -OC(=O)SR Ａ１ , -OC(=O)N(R Ａ１ ) ２ , -SC(=O)R Ａ２ , -SC(=O)OR Ａ１ , -SC(=O)SR Ａ１ , -SC(=O)N(R Ａ１ ) ２ , -NHC(=O)R Ａ１ , -NHC(=O)OR Ａ１ , -NHC(=O)SR Ａ１ , -NHC(=O)N(R Ａ１ ) ２ , -OS(=O) ２ R Ａ２ , -OS(=O) ２ OR Ａ１ , -S-S(=O) ２ R Ａ２ , -S-S(=O) ２ OR Ａ１ , -S(=O)R Ａ２ , -SO ２ R Ａ２ Or -S(=O) ２ OR Ａ１ where R Ａ１ each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, a nitrogen protecting group when attached to a nitrogen atom, -SO ２ R Ａ２ , -C(O)R Ａ２ or two R Ａ１ groups taken together form a substituted or unsubstituted heterocyclic or heteroaryl ring; R Ａ２ is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Here, R ８ and R １３ At least one of is ethyl, substituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -SR Ａ１ , -N(R Ａ１ ) ２ , -C(O)R Ａ１ , -C(=O)N(R Ａ１ ) ２ , -OC(=O)R Ａ１ , -OC(=O)OR Ａ１ , -OC(=O)SR Ａ１ , -OC(=O)N(R Ａ１ ) ２ , -SC(=O)R Ａ２ , -SC(=O)OR Ａ１ , -SC(=O)SR Ａ１ , -SC(=O)N(R Ａ１ ) ２ , -NHC(=O)R Ａ１ , -NHC(=O)OR Ａ１ , -NHC(=O)SR Ａ１ , -NHC(=O)N(R Ａ１ ) ２ , -OS(=O) ２ R Ａ２ , -OS(=O) ２ OR Ａ１ , -S-S(=O) ２ R Ａ２ , -S-S(=O) ２ OR Ａ１ , -S(=O)R Ａ２ , -SO ２ R Ａ２ Or -S(=O) ２ OR Ａ１ Must be; or R ８ and R １３ together form an oxo (=O) group, Here, R ８ and R １３ and cannot both be methyl; and Where: 【Chemistry 426】 represents a single bond, a compound or a pharma- ceutically acceptable salt thereof.

2. R ７ But, R ９ 2. The compound or pharma- ceutically acceptable salt of claim 1, wherein:

3. R ７ But, R ９ 2. The compound or pharma- ceutically acceptable salt of claim 1, wherein:

4. R ３ is unsubstituted C １～３ Alkyl or unsubstituted C １～３ Alkoxy-C １～３ 4. The compound or a pharma- ceutically acceptable salt according to any one of claims 1 to 3, wherein: R is an alkyl group;

5. R ３ The compound or pharma- ceutically acceptable salt of any one of claims 1 to 4, wherein is methyl, ethyl, methoxymethyl, or ethoxymethyl.

6. R ３ 6. The compound or pharma- ceutically acceptable salt according to any one of claims 1 to 5, wherein is methyl or ethoxymethyl.

7. R ９ The compound or pharma- ceutically acceptable salt of any one of claims 1 to 6, wherein is hydrogen, methyl, or ethyl.

8. The compound or pharma- ceutically acceptable salt according to any one of claims 1 to 7, wherein R9 is hydrogen.

9. The compound or pharma- ceutically acceptable salt according to any one of claims 1 to 7, wherein R9 is methyl.

10. R ８ is hydrogen and R １３ is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, -SR Ａ１ , -N(R Ａ１ ) ２ , -C(O)R Ａ１ , -C(=O)N(R Ａ１ ) ２ , -OC(=O)R Ａ１ , -OC(=O)OR Ａ１ , -OC(=O)SR Ａ１ or -OC(=O)N(R Ａ１ ) ２ where R Ａ１ 10. The compound of any one of claims 1-9, or a pharma- ceutically acceptable salt thereof, wherein each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

11. R ８ Or R １３ is a substituted or unsubstituted alkyl, —C(O)R Ａ１ , -C(=O)N(R Ａ１ ) ２ , -OC(=O)R Ａ１ or -OC(=O)OR Ａ１ where R Ａ１ 10. The compound of any one of claims 1-9, or a pharma- ceutically acceptable salt thereof, wherein each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

12. R ８ Or R １３ But -C(O)R Ａ１ where R Ａ１ 12. The compound or pharma- ceutically acceptable salt of any one of claims 1 to 9 or 11, wherein is alkyl substituted with a substituted or unsubstituted heteroaryl.

13. The compound according to claim 1, wherein R 8 is hydrogen, R 13 is -C(O)R A1 , -C(=O)N(R A1 ) 2 , or -C(=O)NH(R A1 ), and each occurrence of R A1 is independently substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 , or two R A1 groups taken together form a substituted or unsubstituted heterocyclic or heteroaryl ring, wherein said heterocyclic or heteroaryl has at least one nitrogen atom; and R A2 or a pharma- ceutically acceptable salt thereof. The compound of any one of claims 1 to 9, wherein is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

14. The compound according to claim 14, wherein R 8 is hydrogen and R 13 is -N(R A1 ) 2 , where each occurrence of R A1 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, a nitrogen protecting group when attached to a nitrogen atom, -SO 2 R A2 , -C(O)R A2 , or two R A1 groups taken together form a substituted or unsubstituted heterocyclic or heteroaryl ring, wherein said heterocyclic or heteroaryl has at least one nitrogen atom; and R A2 or a pharma- ceutically acceptable salt thereof. The compound of any one of claims 1 to 9, wherein is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

15. The compound of formula (II) is represented by formula (I-Ia) 【Chemistry 610】 or a pharma- ceutically acceptable salt thereof, Here, R １ is a substituted or unsubstituted alkyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR Ａ１ , -SR Ａ１ , -N(R Ａ１ ) ２ , -N(R Ａ１ ), -OC(=O)R Ａ１ , -OC(=O)OR Ａ１ , -OC(=O)SR Ａ１ , -OC(=O)N(R Ａ１ ) ２ , -SC(=O)R Ａ２ , -SC(=O)OR Ａ１ , -SC(=O)SR Ａ１ , -SC(=O)N(R Ａ１ ) ２ , -NHC(=O)R Ａ１ , -NHC(=O)OR Ａ１ , -NHC(=O)SR Ａ１ , -NHC(=O)N(R Ａ１ ) ２ , -OS(=O) ２ R Ａ２ , -OS(=O) ２ OR Ａ１ , -S-S(=O) ２ R Ａ２ , -S-S(=O) ２ OR Ａ１ , -S(=O)R Ａ２ , -SO ２ R Ａ２ Or -S(=O) ２ OR Ａ１ where R Ａ１ Each occurrence of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or two R Ａ１ groups taken together form a substituted or unsubstituted heterocyclic or heteroaryl ring; R Ａ２ is substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; 2. The compound or pharma- ceutically acceptable salt of claim 1, wherein n is 0, 1, 2, or 3.

16. The compound of formula (I-Ia) is represented by formula (I-Ib) 【Chemistry 611】 16. The compound or pharma- ceutically acceptable salt of claim 15, which is the compound or a pharma- ceutically acceptable salt thereof:

17. R １ but, 【Chemistry 430】 and Here, R ２０ Each occurrence of is independently a halogen, —NO ２ , -CN, -OR ＧＡ , -N(R ＧＡ ) ２ , -C(=O)R ＧＡ , -C(=O)OR ＧＡ , -OC(=O)R ＧＡ , -OC(=O)OR ＧＡ , -C(=O)N(R ＧＡ ) ２ , -N(R ＧＡ ) C(=O)R ＧＡ , -OC(=O)N(R ＧＡ ) ２ , -N(R ＧＡ ) C(=O)OR ＧＡ , -S(=O) ２ R ＧＡ , -S(=O) ２ OR ＧＡ , -OS(=O) ２ R ＧＡ , -S(=O) ２ N (R ＧＡ ) ２ , or -N(R ＧＡ ) S(=O) ２ R ＧＡ ; substituted or unsubstituted C １～６ Alkyl, substituted or unsubstituted C ３～４ carbocyclyl, or a substituted or unsubstituted 3- to 4-membered heterocyclyl; Here, R ＧＡ Each occurrence is independently hydrogen, substituted or unsubstituted C １～６ Alkyl, substituted or unsubstituted C ３～６ carbocyclyl, substituted or unsubstituted 3- to 6-membered heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or two R ＧＡ the groups, together with the intervening atoms, form a substituted or unsubstituted carbocyclic or heterocyclic ring; 17. The compound or pharma- ceutically acceptable salt of claim 15 or claim 16, wherein each of n and e is independently 0, 1, 2, 3, 4, or 5.

18. The compound of formula (II) is represented by formula (I-Id): 【Chemistry 612】 or a pharma- ceutically acceptable salt thereof, Here, R １０ 2. The compound or pharma- ceutically acceptable salt of claim 1, wherein is independently hydrogen, halogen, substituted or unsubstituted alkyl, hydroxyl, or cyano.

19. The compound of formula (II) is represented by formula (I-Ie): 【Chemistry 613】 or a pharma- ceutically acceptable salt thereof, where e is 0, 1, 2, or 3; p is 0, 1, or 3; R ５ 2. The compound or pharma- ceutically acceptable salt of claim 1, wherein each of is independently halogen, alkyl, hydroxyl, or cyano.

20. The compound of formula (II) is represented by formula (I-If) 【Chemistry 614】 or a pharma- ceutically acceptable salt thereof, Here, R １０ 2. The compound of claim 1, or a pharma- ceutically acceptable salt thereof, wherein is hydrogen, halogen, substituted or unsubstituted alkyl, hydroxyl, or cyano.

21. 【Table 21-1】 【Table 21-2】 【Table 21-3】 【Table 21-4】 【Table 21-5】 【Table 21-6】 【Table 21-7】 【Table 21-8】 【Table 21-9】 【Table 21-10A】 【Table 21-11】 【Table 21-12】 or a pharma- ceutically acceptable salt thereof.

22. The compound, 【Chemistry 22-1】 【Chemistry 22-2】 【Chemistry 22-3】 【Chemistry 22-4】 【Chemistry 22-5】 【Chemistry 22-6】 【Chemistry 22-7】 or a pharma- ceutically acceptable salt thereof.

22. The compound of claim 21, wherein said compound is selected from:

23. The compound, 【Chemistry 23-1】 【Chemistry 23-2】 【Chemistry 23-3】 or a pharma- ceutically acceptable salt thereof.

22. The compound of claim 21, wherein said compound is selected from:

24. A pharmaceutical composition comprising a compound according to any one of claims 1 to 23 or a pharma- ceutically acceptable salt thereof, and a pharma- ceutically acceptable excipient.

25. 24. A composition for use in treating a CNS-related disorder in a subject in need thereof, comprising a compound according to any one of claims 1 to 23 or a pharma- ceutically acceptable salt thereof, wherein the CNS-related disorder is a sleep disorder, a mood disorder, a schizophrenia spectrum disorder, a seizure disorder, a disorder of memory and / or cognition, a movement disorder, a personality disorder, an autism spectrum disorder, pain, a traumatic brain injury, a vascular disease, a substance abuse disorder and / or withdrawal syndrome, tinnitus, or status epilepticus.

26. 26. The composition of claim 25, wherein the CNS-related disorder is depression.

27. 27. The composition of claim 26, wherein the depression is postpartum depression.

28. 26. The composition of claim 25, wherein the CNS-related disorder is major depressive disorder.

29. 29. The composition of claim 28, wherein the major depressive disorder is moderate major depressive disorder.

30. 29. The composition of claim 28, wherein the major depressive disorder is severe major depressive disorder.

31. 26. The composition of claim 25, wherein the CNS-related disorder is seizures.

32. 26. The composition of claim 25, wherein the CNS-related disorder is epilepsy or status epilepticus.

33. 26. The composition of claim 25, wherein the CNS-related disorder is tremor.

34. 34. The composition of claim 33, wherein the tremor is essential tremor.

35. 26. The composition of claim 25, wherein the composition is administered chronically or acutely.

36. 36. The composition of claim 35, wherein the composition is administered orally, intravenously, transdermally, intranasally, or subcutaneously.

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