Compositions and methods for treating CNS disorders

Abstract

As used herein, a compound of formula (1-I): JPEG2022538300000478.jpg47165, or a pharmaceutically acceptable salt thereof, wherein R 2a , R 2b , R 3 , R 4a , R 4b , R 5 , R 6a , R 6b , R 11a , R 11b , R 16a , R 16b , R 19 , R 18 , X, q, r, s, t, u, and n are defined herein. Also provided herein are pharmaceutical compositions comprising the compounds of formula (1-I), and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Description

[Technical Field]

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS This application claims the benefit of and priority to U.S. Provisional Application Nos. 62 / 867,646, filed June 27, 2019, 62 / 867,657, filed June 27, 2019, and 62 / 867,662, filed June 27, 2019, the contents of each of which are incorporated herein by reference in their entirety. [Background technology]

[0002] Brain excitability is defined as the level of excitement of an animal, a continuum ranging from coma to seizures, and is regulated by various neurotransmitters. Generally, neurotransmitters are responsible for regulating the conduction of ions across the neuronal membrane. At rest, the neuronal membrane has a potential (or membrane voltage) of approximately -70 mV, with the interior of the cell being negative relative to the exterior. The potential (voltage) is determined by the flow of ions (K) across the neuronal semipermeable membrane. + , Na + , Cl - Neurotransmitters are stored in presynaptic vesicles and are released under the influence of an action potential in the neuron. When released into the synaptic cleft, excitatory chemical transmitters such as acetylcholine cause membrane depolarization (a change in potential occurs between -70 mV and -50 mV). This effect is stimulated by acetylcholine and Na + It is mediated by postsynaptic nicotinic receptors, which increase membrane permeability to ions. The decrease in membrane potential stimulates neuronal excitability in the form of postsynaptic action potentials.

[0003] In the case of the GABA receptor complex (GRC), its influence on brain excitability is mediated by the neurotransmitter gamma-aminobutyric acid (GABA). GABA profoundly influences overall brain excitability, as up to 40% of neurons in the brain utilize GABA as a neurotransmitter. GABA regulates the excitability of individual neurons by modulating the conductance of chloride ions across the neuronal membrane. GABA interacts with its recognition sites on the GRC, promoting chloride ions flowing down the GRC's electrochemical gradient into the cell. Intracellular increases in the levels of this anion cause hyperpolarization of the transmembrane potential, making the neuron less susceptible to excitatory inputs, i.e., a decrease in neuronal excitability. In other words, the higher the concentration of chloride ions within neurons, the lower the brain's excitability and arousal levels.

[0004] It has been well documented that the GRC mediates anxiety, seizure activity, and sedation. Thus, GABA and drugs that act like GABA or potentiate the effects of GABA (e.g., therapeutically useful barbiturates and benzodiazepines (BZs), e.g., Valium®) exert their therapeutic effects by interacting with specific regulatory sites on the GRC. Accumulating evidence now indicates that, in addition to the binding sites for benzodiazepines and barbiturates, the GRC contains distinct sites for neuroactive steroids. See, e.g., Lan, NC et al., Neurochem. Res. (1991) 16:347-356.

[0005] Neuroactive steroids can occur endogenously. The most potent endogenous neuroactive steroids are 3α-hydroxy-5-reduced pregnan-20-one and 3α-21-dihydroxy-5-reduced pregnan-20-one, which are metabolites of the hormonal steroids progesterone and deoxycorticosterone, respectively. The ability of these steroid metabolites to alter brain excitability was recognized in 1986 (see Majewska, MD et al., Science 232:1004-1007 (1986); Harrison, NL et al., J Pharmacol. Exp. Ther. 241:346-353 (1987)). There is a need for new and improved compounds that function as modulators of brain excitability and as agents for the prevention and treatment of CNS-related disorders. The compounds, compositions, and methods described herein are directed toward this end. [Prior art documents] [Non-patent literature]

[0006] [Non-Patent Document 1] Lan, NC 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,NLet al.,J Pharmacol.Exp.Ther.241:346-353(1987) Summary of the Invention [Means for solving the problem]

[0007] For example, compounds designed to act as GABA modulators are provided herein. In some embodiments, such compounds are contemplated to be useful as therapeutic agents for treating CNS-related disorders.

[0008] In some embodiments, provided herein are compounds of formula (1-I): [ka] or a pharmaceutically acceptable salt thereof is provided.

[0009] In some embodiments, the compound of formula (1-I) is a compound of formula (1-II-a): [ka] or a pharmaceutically acceptable salt thereof.

[0010] In some embodiments, the compound of formula (1-I) is a compound of formula (1-II-b): [ka] or a pharmaceutically acceptable salt thereof.

[0011] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-II-c): [ka] or a pharmaceutically acceptable salt thereof.

[0012] In some embodiments, the compound of formula (1-I) is a compound of formula (1-II-d): [ka] or a pharmaceutically acceptable salt thereof.

[0013] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-III-a): [ka] or a pharmaceutically acceptable salt thereof.

[0014] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-III-b): [ka] or a pharmaceutically acceptable salt thereof.

[0015] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-III-c): [ka] or a pharmaceutically acceptable salt thereof.

[0016] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-III-d): [ka] or a pharmaceutically acceptable salt thereof.

[0017] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IV-a): [ka] or a pharmaceutically acceptable salt thereof.

[0018] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IV-b): [ka] or a pharmaceutically acceptable salt thereof.

[0019] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IV-c): [ka] or a pharmaceutically acceptable salt thereof.

[0020] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IV-d): [ka] or a pharmaceutically acceptable salt thereof.

[0021] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-Va): [ka] or a pharmaceutically acceptable salt thereof.

[0022] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-Vb): [ka] or a pharmaceutically acceptable salt thereof.

[0023] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VI-a): [ka] or a pharmaceutically acceptable salt thereof.

[0024] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VI-b): [ka] or a pharmaceutically acceptable salt thereof.

[0025] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VII-a): [ka] or a pharmaceutically acceptable salt thereof.

[0026] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VII-b): [ka]

[0027] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VIII-a): [ka] or a pharmaceutically acceptable salt thereof.

[0028] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VIII-b): [ka] or a pharmaceutically acceptable salt thereof.

[0029] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IX-a): [ka] or a pharmaceutically acceptable salt thereof.

[0030] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IX-b): [ka] or a pharmaceutically acceptable salt thereof.

[0031] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IX-c): [ka] or a pharmaceutically acceptable salt thereof.

[0032] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IX-d): [ka] or a pharmaceutically acceptable salt thereof.

[0033] In some embodiments, the compound of formula (1-I) is a compound of formula (1-Xa): [ka] or a pharmaceutically acceptable salt thereof.

[0034] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-Xb): [ka] or a pharmaceutically acceptable salt thereof.

[0035] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-Xc): [ka] or a pharmaceutically acceptable salt thereof.

[0036] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-Xd): [ka] or a pharmaceutically acceptable salt thereof.

[0037] In some embodiments, the compound of formula (1-I) is a compound of formula (1-XI-a): [ka] or a pharmaceutically acceptable salt thereof.

[0038] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XI-b): [ka] or a pharmaceutically acceptable salt thereof.

[0039] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XI-c): [ka] or a pharmaceutically acceptable salt thereof.

[0040] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XI-d): [ka] or a pharmaceutically acceptable salt thereof.

[0041] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XII-a): [ka] or a pharmaceutically acceptable salt thereof.

[0042] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XII-b): [ka] or a pharmaceutically acceptable salt thereof.

[0043] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XIII-a): [ka] or a pharmaceutically acceptable salt thereof.

[0044] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XIII-b): [ka] or a pharmaceutically acceptable salt thereof.

[0045] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XIV-a): [ka] or a pharmaceutically acceptable salt thereof.

[0046] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XIV-b): [ka] or a pharmaceutically acceptable salt thereof.

[0047] In some embodiments, provided herein are compounds of formula 2-I: [ka] or a pharmaceutically acceptable salt thereof is provided.

[0048] In some embodiments, the compound of formula 2-I is a compound of formula 2-Ia or formula 2-Ib: [ka] or a pharmaceutically acceptable salt thereof.

[0049] In some embodiments, the compound of formula 2-I is a compound of formula 2-Iaa or formula 2-Iab: [ka] or a pharmaceutically acceptable salt thereof.

[0050] In some embodiments, provided herein are compounds of formula 2-II: [ka] or a pharmaceutically acceptable salt thereof is provided.

[0051] In some embodiments, the compound of Formula 2-II is a compound of Formula 2-IIa: [ka] or a pharmaceutically acceptable salt thereof.

[0052] In some embodiments, provided herein are compounds of formula 2-III: [ka] or a pharmaceutically acceptable salt thereof is provided.

[0053] In some embodiments, the compound of Formula 2-III is a compound of Formula 2-IIIa: [ka] or a pharmaceutically acceptable salt thereof.

[0054] In certain embodiments, provided herein are compounds of formula 2-IVa or 2-IVb: [ka] or a pharmaceutically acceptable salt thereof is provided.

[0055] In some embodiments, the compound of formula 2-IV is a compound of formula 2-IVaa or formula 2-IVba: [ka] or a pharmaceutically acceptable salt thereof.

[0056] In embodiments, provided herein are compounds of formula 2-V: [ka] or a pharmaceutically acceptable salt thereof is provided.

[0057] In some embodiments, the compound of formula 2-V is a compound of formula 2-Va: [ka] or a pharmaceutically acceptable salt thereof.

[0058] In embodiments, provided herein are compounds of formula 2-VI: [ka] or a pharmaceutically acceptable salt thereof is provided.

[0059] In some embodiments, the compound of Formula 2-VI is a compound of Formula 2-VIa: [ka] or a pharmaceutically acceptable salt thereof.

[0060] In embodiments, provided herein are compounds of formula 2-VII: [ka] or a pharmaceutically acceptable salt thereof is provided.

[0061] In some embodiments, the compound of Formula 2-VII is a compound of Formula 2-VIIa: [ka] or a pharmaceutically acceptable salt thereof.

[0062] In some embodiments, provided herein are compounds of formula 3-I: [ka] or a pharmaceutically acceptable salt thereof is provided.

[0063] In some embodiments, the compound of formula 3-I is a compound of formula 3-IIa or formula 3-IIb: [ka] or a pharmaceutically acceptable salt thereof.

[0064] In some embodiments, the compound of formula 3-III: [ka] or a pharmaceutically acceptable salt thereof.

[0065] In some embodiments, the compound of formula 3-IV: [ka] or a pharmaceutically acceptable salt thereof.

[0066] In some embodiments, the compound of Formula Va or Formula 3-Vb: [ka] or a pharmaceutically acceptable salt thereof.

[0067] In some embodiments, the compound of formula 3-VI: [ka] or a pharmaceutically acceptable salt thereof.

[0068] In some embodiments, the compound of formula 3-VII: [ka] or a pharmaceutically acceptable salt thereof.

[0069] In some embodiments, the compound of formula 3-VIII: [ka] or a pharmaceutically acceptable salt thereof.

[0070] In some embodiments, the compound of formula 3-IX: [ka] or a pharmaceutically acceptable salt thereof.

[0071] In some embodiments, the compound of formula 3-Ia: [ka] or a pharmaceutically acceptable salt thereof.

[0072] In some embodiments, the compound of Formula 3-IIaa or Formula 3-IIba: [ka] or a pharmaceutically acceptable salt thereof.

[0073] In some embodiments, the compound of Formula 3-IIIa: [ka] or a pharmaceutically acceptable salt thereof.

[0074] In some embodiments, the compound of Formula 3-IVa: [ka] or a pharmaceutically acceptable salt thereof.

[0075] In some embodiments, a compound of formula 3-Vac or formula 3-Vacc: [ka] or a pharmaceutically acceptable salt thereof.

[0076] In some embodiments, the compound of formula 3-VIac: [ka] or a pharmaceutically acceptable salt thereof.

[0077] In some embodiments, the compound of formula 3-VIIac: [ka] or a pharmaceutically acceptable salt thereof.

[0078] In some embodiments, the compound of formula 3-VIIIac: [ka] or a pharmaceutically acceptable salt thereof.

[0079] In some embodiments, the compound of formula 3-IXac: [ka] or a pharmaceutically acceptable salt thereof.

[0080] In one aspect, provided herein is a pharmaceutical composition comprising a compound described herein (e.g., a compound of Formula (1-I)) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. 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.

[0081] In some embodiments, a method for treating a CNS-related disorder in a subject in need thereof comprises administering to the subject an effective amount of a compound described herein or a pharmaceutically acceptable salt thereof. In some embodiments, the CNS-related disorder is a sleep disorder, a mood disorder, a schizophrenia spectrum disorder, a seizure disorder, a memory and / or cognition disorder, 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. In some embodiments, the CNS-related disorder is depression. In some embodiments, the CNS-related disorder is postpartum depression. In some embodiments, the CNS-related disorder is major depressive disorder. In some embodiments, the major depressive disorder is moderate major depressive disorder. In some embodiments, the major depressive disorder is severe major depressive disorder.

[0082] In some embodiments, the compound is selected from the group consisting of the compounds identified in Tables 1-3 herein.

[0083] The compounds of the invention described herein, in certain embodiments, function as GABA modulators, e.g., GABA A GABA receptors act in either a positive or negative manner as a regulator of central nervous system (CNS) excitability. A Such compounds are expected to have CNS activity, as mediated by their ability to modulate receptors.

[0084] Therefore, in another aspect, a method for treating a CNS-related disorder in a subject in need thereof is provided, comprising administering to the subject an effective amount of a compound of the present invention. In certain embodiments, the CNS-related disorder is a sleep disorder, a mood disorder, a schizophrenia spectrum disorder, a seizure disorder, a memory and / or cognitive disorder, 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. In certain embodiments, the CNS-related disorder is depression. In certain embodiments, the CNS-related disorder is postpartum depression. In certain embodiments, the CNS-related disorder is major depressive disorder. In certain embodiments, the major depressive disorder is moderate major depressive disorder. In certain embodiments, the major depressive disorder is severe major depressive disorder. In certain embodiments, the compound is administered orally, subcutaneously, intravenously, or intramuscularly. In certain embodiments, the compound is administered orally. In certain embodiments, the compound is administered chronically. In certain embodiments, the compound is administered continuously, for example, by continuous intravenous infusion. DETAILED DESCRIPTION OF THE INVENTION

[0085] As generally described herein, the present invention provides compounds that are designed to function as GABA A receptor modulators.In certain embodiments, it is envisioned that such compounds are useful as therapeutic agents for treating CNS-related disorders (e.g., disorders described herein, such as depression, such as postpartum depression or major depressive disorder).

[0086] definition chemical definition Definitions of specific functional groups and chemical terms are described in more detail below. Chemical elements are identified according to the Periodic Table of the Elements, CAS Edition, Handbook of Chemistry and Physics, 75th Edition, inside pages, and specific functional groups are generally defined as described herein. Additionally, general principles of organic chemistry, as well as specific functional moieties and reactivities, are described in 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 of Organic Synthesis, 3rd Edition, Cambridge University Press, Cambridge, 1987.

[0087] Isomers, e.g., stereoisomers, can be isolated from mixtures by methods known to those skilled in the art, including chiral high-pressure liquid chromatography (HPLC) and chiral salt formation and crystallization, or preferred isomers can be prepared by asymmetric synthesis. See, for example, Jacques et al., Enantiomers, Racemates and Resolutions (Wiley Interscience, New York, 1981); Wilen et al., Tetrahedron 33:2725 (1977); Eliel, Stereochemistry of Carbon Compounds (McGraw-Hill, NY, 1962); and Wilen, Tables of Resolving Agents and Optical Resolutions p. 268 (EL Eliel, Ed., University of Notre Dame Press, Notre Dame, IN 1972). The present invention additionally encompasses the compounds described herein as individual isomers substantially free of other isomers, and alternatively, as mixtures of various isomers.

[0088] "Stereoisomers": It should also be understood that compounds that have identical molecular formulas but differ in the nature or sequence of bonding of their atoms or the arrangement of their atoms in space are referred to as "isomers." Isomers that differ in the arrangement of their atoms in space are referred to as "stereoisomers." Stereoisomers that are not mirror images of each other are referred to as "diastereomers," and stereoisomers that are non-superimposable mirror images of each other are referred to as "enantiomers." When a compound has an asymmetric center, for example, when a compound is bonded to four different groups, a pair of enantiomers is possible. An enantiomer can be characterized by the absolute configuration of its asymmetric center and described by the R- and S-sequencing rules of Cahn and Prelog, or by the way the molecule rotates the plane of polarized light and is designated as dextrorotatory or levorotatory (i.e., as (+) or (-)-isomers, respectively). Chiral compounds can exist as individual enantiomers or as mixtures thereof. A mixture containing equal proportions of enantiomers is referred to as a "racemic mixture."

[0089] As used herein, a pure enantiomer compound is substantially free of other enantiomers or stereoisomers of a compound (i.e., in enantiomeric excess). In other words, the "S" form of a compound is substantially free of the "R" form of the compound and is thus in enantiomeric excess of the "R" form. The terms "enantiomerically pure" or "pure enantiomer" mean that a compound contains more than 75%, more than 80%, more than 85%, more than 90%, more than 91%, more than 92%, more than 93%, more than 94%, more than 95%, more than 96%, more than 97%, more than 98%, more than 98.5%, more than 99%, more than 99.2%, more than 99.5%, more than 99.6%, more than 99.7%, more than 99.8%, or more than 99.9% by weight of an enantiomer. In certain embodiments, the weight is based on the total weight of all enantiomers or stereoisomers of the compound.

[0090] In the compositions provided herein, the enantiomerically pure compound may be present together with other active or inactive ingredients. For example, a pharmaceutical composition containing an enantiomerically pure R position / center / carbon compound may contain, for example, about 90% excipients and about 10% enantiomerically pure R compound. In certain embodiments, the enantiomerically pure R compound in such a composition may contain, for example, 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 containing an enantiomerically pure S compound may contain, for example, about 90% excipients and about 10% of the enantiomerically pure S compound. In certain embodiments, the enantiomerically pure S compound in such a composition may contain, 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 be formulated with little or no excipients or carriers.

[0091] The term "diastereomerically pure" means that a compound contains more than 75%, 80%, 85%, 90%, 91%, 92%, 93%, 94%, 95%, 96%, 97%, 98%, 98.5%, 99%, 99.2%, 99.5%, 99.6%, 99.7%, 99.8%, or more than 99.9% by weight of a single diastereomer. Methods for determining diastereomeric and enantiomeric purity are well known in the art. Diastereomeric purity can be determined by any analytical method capable of quantitatively distinguishing between a compound and its diastereomer, for example, high-performance liquid chromatography (HPLC).

[0092] The articles "a" and "an" may be used herein to refer to one or to more than one (i.e., to at least one) of the grammatical object of the article. By way of example, "an analog" means one analog or more than one analog.

[0093] 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" refers to C1, C2, C3, C4, C5, C6, 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 Alkyl is intended to be included.

[0094] The following terms are intended to have the meanings presented below and are useful in understanding the description and intended scope of the present invention.

[0095] "Alkyl" refers to the radical of a straight-chain or branched saturated hydrocarbon group having from 1 to 20 carbon atoms ("C 1~20 In some embodiments, an alkyl group has 1 to 12 carbon atoms ("C 1~12 In some embodiments, an alkyl group has 1 to 10 carbon atoms ("C 1~10 In some embodiments, an alkyl group has 1 to 9 carbon atoms ("C 1~9 In some embodiments, an alkyl group has 1 to 8 carbon atoms ("C 1~8 In some embodiments, an alkyl group has 1 to 7 carbon atoms ("C 1~7 In some embodiments, an alkyl group has 1 to 6 carbon atoms ("C 1~6 In some embodiments, an alkyl group has 1 to 5 carbon atoms ("C 1~5In some embodiments, an alkyl group has 1 to 4 carbon atoms ("C 1~4 In some embodiments, an alkyl group has 1 to 3 carbon atoms ("C 1~3 In some embodiments, an alkyl group has 1 to 2 carbon atoms ("C 1~2 In some embodiments, the alkyl group has 1 carbon atom ("C alkyl"). In some embodiments, the alkyl group has 2 to 6 carbon atoms ("C 2~6 alkyl). C 1~6 Examples of alkyl groups include methyl (C1), ethyl (C2), n-propyl (C3), isopropyl (C3), n-butyl (C4), tertiary butyl (C4), sec-butyl (C4), isobutyl (C4), n-pentyl (C5), 3-pentanyl (C5), amyl (C5), neopentyl (C5), 3-methyl-2-butanyl (C5), tertiary amyl (C5), and n-hexyl (C6). Additional examples of alkyl groups include n-heptyl (C7), n-octyl (C8), and the like. Unless otherwise specified, each example of an alkyl group is independently optionally substituted, i.e., unsubstituted ("unsubstituted alkyl") or substituted with one or more substituents, e.g., 1 to 5 substituents, 1 to 3 substituents, or 1 substituent ("substituted alkyl"). In certain embodiments, an alkyl group is an unsubstituted C 1~10 In certain embodiments, the alkyl group is a substituted C 1~10 Common abbreviations for alkyl include Me(-CH), Et(-CHCH), iPr(-CH(CH)), nPr(-CHCHCH), n-Bu(-CHCHCHCHCH), or i-Bu(-CHCH(CH)).

[0096] "Alkylene" refers to an alkyl group in which two hydrogens are removed to provide a divalent radical, which can be substituted or unsubstituted. Unsubstituted alkylene groups include, but are not limited to, methylene (-CH-), ethylene (-CHCH-), propylene (-CHCHCH-), butylene (-CHCHCHCHCH-), pentylene (-CHCHCHCHCHCH-), hexylene (-CHCHCHCHCHCHCH-), and the like. For example, exemplary substituted alkylene groups substituted with one or more alkyl (methyl) groups include, but are not limited to, substituted methylene (-CH(CH)-, (-C(CH)-), substituted ethylene (-CH(CH)CH-, -CHCH(CH)-, -C(CH)CH-, -CHC(CH)-), substituted propylene (-CH(CH)CHCH-, -CHCH(CH)CH-, -CHCHCH(CH)CH-, -CHCHCH(CH)-, -C(CH)CHCH-, -CHC(CH)CH-, -CHCHC(CH)-), and the like. When a range or number of carbons is provided for a particular alkylene group, it is understood that the range or number refers to the range or number of carbons in a linear divalent carbon chain. An alkylene group can be unsubstituted or substituted with one or more substituents described herein.

[0097] "Alkenyl" refers to the radical of a straight-chain or branched hydrocarbon group having 2 to 20 carbon atoms, one or more carbon-carbon double bonds (e.g., 1, 2, 3, or 4 carbon-carbon double bonds), and optionally one or more carbon-carbon triple bonds (e.g., 1, 2, 3, or 4 carbon-carbon triple bonds) ("C 2~20 In certain embodiments, the alkenyl does not contain any triple bonds. In some embodiments, the alkenyl group has 2 to 10 carbon atoms ("C 2~10 In some embodiments, an alkenyl group has 2 to 9 carbon atoms ("C 2~9 In some embodiments, an alkenyl group has 2 to 8 carbon atoms ("C 2~8In some embodiments, an alkenyl group has 2 to 7 carbon atoms ("C 2~7 In some embodiments, an alkenyl group has 2 to 6 carbon atoms ("C 2~6 In some embodiments, an alkenyl group has 2 to 5 carbon atoms ("C 2~5 In some embodiments, an alkenyl group has 2 to 4 carbon atoms ("C 2~4 In some embodiments, an alkenyl group has 2 to 3 carbon atoms ("C 2~3 In some embodiments, the alkenyl group has two carbon atoms ("C2 alkenyl"). The one or more carbon-carbon double bonds can be internal (such as in 2-butenyl) or terminal (such as in 1-butenyl). C 2~4 Examples of alkenyl groups include ethenyl (C2), 1-propenyl (C3), 2-propenyl (C3), 1-butenyl (C4), 2-butenyl (C4), butadienyl (C4), and the like. 2~6 Examples of alkenyl groups include the above-mentioned C 2~4 Alkenyl groups include pentenyl (C5), pentadienyl (C5), hexenyl (C6), and the like. Additional examples of alkenyl include heptenyl (C7), octenyl (C8), octatrienyl (C8), and the like. Unless otherwise specified, each instance of an alkenyl group is independently optionally substituted, i.e., unsubstituted ("unsubstituted alkenyl") or substituted with one or more substituents, e.g., 1 to 5 substituents, 1 to 3 substituents, or 1 substituent ("substituted alkenyl"). In certain embodiments, an alkenyl group is an unsubstituted C 2~10 In certain embodiments, the alkenyl group is a substituted C 2~10 It is alkenyl.

[0098] "Alkynyl" refers to the radical of a straight-chain or branched hydrocarbon 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 bonds) ("C 2~20 In certain embodiments, alkynyl does not contain any double bonds. In some embodiments, alkynyl groups have 2 to 10 carbon atoms ("C 2~10 In some embodiments, an alkynyl group has 2 to 9 carbon atoms ("C 2~9 In some embodiments, an alkynyl group has 2 to 8 carbon atoms ("C 2~8 In some embodiments, an alkynyl group has 2 to 7 carbon atoms ("C 2~7 In some embodiments, an alkynyl group has 2 to 6 carbon atoms ("C 2~6 In some embodiments, an alkynyl group has 2 to 5 carbon atoms ("C 2~5 In some embodiments, an alkynyl group has 2 to 4 carbon atoms ("C 2~4 In some embodiments, an alkynyl group has 2 to 3 carbon atoms ("C 2~3 In some embodiments, the alkynyl group has two carbon atoms ("C2 alkynyl"). The one or more carbon-carbon triple bonds can be internal (such as in 2-butynyl) or terminal (such as in 1-butynyl). C 2~4 Examples of alkynyl groups include, without limitation, ethynyl (C2), 1-propynyl (C3), 2-propynyl (C3), 1-butynyl (C4), 2-butynyl (C4), and the like. 2~6 Examples of alkenyl groups include the above-mentioned C 2~4Alkynyl groups include pentynyl (C5), hexynyl (C6), and the like. Additional examples of alkynyl include heptynyl (C7), octynyl (C8), and the like. Unless otherwise specified, each instance of an alkynyl group is independently optionally substituted, i.e., unsubstituted (an "unsubstituted alkenyl") or substituted with one or more substituents, e.g., 1 to 5 substituents, 1 to 3 substituents, or 1 substituent (a "substituted alkenyl"). In certain embodiments, an alkynyl group is an unsubstituted C 2~10 In certain embodiments, the alkynyl group is a substituted C 2~10 It is alkynyl.

[0099] As used herein, the term "heteroalkyl" refers to an alkyl group, as defined herein, further comprising one or more (e.g., 1, 2, 3, or 4) heteroatoms (e.g., oxygen, sulfur, nitrogen, boron, silicon, phosphorus) in the parent chain, wherein one or more heteroatoms are inserted between adjacent carbon atoms in the parent carbon chain and / or one or more heteroatoms are inserted between a carbon atom and the parent molecule, i.e., between the points of attachment. In certain embodiments, a heteroalkyl group refers to a saturated group having 1 to 10 carbon atoms and 1, 2, 3, or 4 heteroatoms ("heteroC 1~10 In some embodiments, a heteroalkyl group is a saturated group having 1 to 9 carbon atoms and 1, 2, 3, or 4 heteroatoms ("heteroC 1~9 In some embodiments, a heteroalkyl group is a saturated group having 1 to 8 carbon atoms and 1, 2, 3, or 4 heteroatoms ("heteroC 1~8 In some embodiments, a heteroalkyl group is a saturated group having 1 to 7 carbon atoms and 1, 2, 3, or 4 heteroatoms ("heteroC 1~7 In some embodiments, a heteroalkyl group is a group having 1 to 6 carbon atoms and 1, 2, or 3 heteroatoms ("heteroC 1~6In some embodiments, a heteroalkyl group is a saturated group having 1 to 5 carbon atoms and 1 or 2 heteroatoms ("heteroC 1~5 In some embodiments, a heteroalkyl group is a saturated group having 1 to 4 carbon atoms and 1 or 2 heteroatoms ("heteroC 1~4 In some embodiments, a heteroalkyl group is a saturated group having 1 to 3 carbon atoms and 1 heteroatom ("heteroC 1~3 In some embodiments, a heteroalkyl group is a saturated group having 1 to 2 carbon atoms and 1 heteroatom ("heteroC 1~2 In some embodiments, a heteroalkyl group is a saturated group having 1 carbon atom and 1 heteroatom ("heteroC1 alkyl"). In some embodiments, a heteroalkyl group is a saturated group having 2 to 6 carbon atoms and 1 or 2 heteroatoms ("heteroC 2~6 Unless otherwise specified, each instance of a heteroalkyl group is independently unsubstituted (an "unsubstituted heteroalkyl") or substituted (a "substituted heteroalkyl") with one or more substituents. In certain embodiments, a heteroalkyl group is an unsubstituted heteroC 1~10 In certain embodiments, the heteroalkyl group is a substituted heteroC 1~10 It is alkyl.

[0100] "Aryl" refers to a radical of a monocyclic or polycyclic (e.g., bicyclic or tricyclic) 4n+2 aromatic ring system (e.g., having 6, 10, or 14 π electrons shared in a cyclic arrangement) having 6 to 14 ring carbon atoms and 0 heteroatoms provided in the aromatic ring system ("C 6~14 In some embodiments, an aryl group has 6 ring carbon atoms ("C aryl"; e.g., phenyl). In some embodiments, an aryl group has 10 ring carbon atoms ("C 10Aryl"; e.g., naphthyl, such as 1-naphthyl and 2-naphthyl). In some embodiments, an aryl group has 14 ring carbon atoms ("C 14 "Aryl"; e.g., anthracyl). "Aryl" also includes ring systems in which an aryl ring, as defined above, is fused with one or more carbocyclyl or heterocyclyl groups, where the radical or point of attachment is on the aryl ring, and in such instances, the number of carbon atoms continues to designate the number of carbon atoms in the aryl ring system. Typical aryl groups include, but are not limited to, groups derived from aceanthrylene, acenaphthylene, acephenanthrylene, anthracene, azulene, benzene, chrysene, coronene, fluoranthene, fluorene, hexacene, hexaphene, hexalene, as-indacene, s-indacene, indane, indene, naphthalene, octacene, octaphene, octalene, ovalene, penta-2,4-diene, pentacene, pentalene, pentaphene, perylene, phenalene, phenanthrene, picene, pleiadene, pyrene, pyranthrene, rubicene, triphenylene, and trinaphthalene. In particular, aryl groups include phenyl, naphthyl, indenyl, and tetrahydronaphthyl. Unless otherwise specified, each instance of an aryl group is independently optionally substituted, i.e., unsubstituted ("unsubstituted aryl") or substituted with one or more substituents ("substituted aryl"). In certain embodiments, an aryl group is an unsubstituted C 6~14 In certain embodiments, the aryl group is a substituted C 6~14 It is aryl.

[0101] In certain embodiments, the aryl group is substituted with one or more groups selected from halo, C1-C8 alkyl, C1-C8 haloalkyl, cyano, hydroxy, C1-C8 alkoxy, and amino.

[0102] Representative examples of substituted aryl include: [ka] In the formula, R 56 and R 57 may be hydrogen, and one of R 56 and R 57 At least one of the following is independently selected from C1-C8 alkyl, C1-C8 haloalkyl, 4- to 10-membered heterocyclyl, alkanoyl, C1-C8 alkoxy, heteroaryloxy, alkylamino, arylamino, heteroarylamino, NR 58 COR 59 , N.R. 58 SOR 59 , N.R. 58 SO2R 59 , COO alkyl, COO aryl, CONR 58 R 59 ,CONR 58 OR 59 , N.R. 58 R 59 , SO2NR 58 R 59 , S-alkyl, SO alkyl, SO alkyl, S aryl, SO aryl, SO aryl, or R 56 and R 57 are joined to form a cyclic ring (saturated or unsaturated) of 5 to 8 atoms, optionally containing one or more heteroatoms selected from N, O, or S. R 60 and R 61 are independently hydrogen, C1-C8 alkyl, C1-C4 haloalkyl, C3-C 10 Cycloalkyl, 4-10 membered heterocyclyl, C6-C 10 Aryl, substituted C6-C 10 It is aryl, 5- to 10-membered heteroaryl, or substituted 5- to 10-membered heteroaryl.

[0103] "Fused aryl" refers to an aryl having two of its ring carbons common to a second aryl or heteroaryl ring, or a carbocyclic or heterocyclic ring.

[0104] "Heteroaryl" refers to the radical of a 5- to 10-membered monocyclic or bicyclic 4n+2 aromatic ring system (e.g., having 6 or 10 π electrons shared in a cyclic arrangement) having ring carbon atoms and 1 to 4 ring heteroatoms provided in the aromatic ring system, each heteroatom being independently selected from nitrogen, oxygen, and sulfur ("5- to 10-membered heteroaryl"). In heteroaryl groups containing one or more nitrogen atoms, the point of attachment may be at a carbon or nitrogen atom, valence permitting. Heteroaryl bicyclic ring systems may contain one or more heteroatoms in one or both rings. "Heteroaryl" includes ring systems in which a heteroaryl ring, as defined above, is fused with one or more carbocyclyl or heterocyclyl groups, the point of attachment being on the heteroaryl ring; in such instances, the number of ring members continues to designate the number of ring members in the heteroaryl ring system. "Heteroaryl" also includes ring systems in which a heteroaryl ring, as defined above, is fused to one or more aryl groups, and the point of attachment can be on either the aryl ring or the heteroaryl ring; in such instances, the number of ring members designates the number of ring members in the fused (aryl / heteroaryl) ring system. For bicyclic heteroaryl groups in which one ring does not contain a heteroatom (e.g., indolyl, quinolinyl, carbazolyl, etc.), the point of attachment can be on either ring, i.e., the ring with a heteroatom (e.g., 2-indolyl) or the ring without a heteroatom (e.g., 5-indolyl).

[0105] In some embodiments, a heteroaryl group is a 5- to 10-membered aromatic ring system having ring carbon atoms and 1 to 4 ring heteroatoms provided in the aromatic ring system, each heteroatom being independently selected from nitrogen, oxygen, and sulfur ("5- to 10-membered heteroaryl"). In some embodiments, a heteroaryl group is a 5- to 8-membered aromatic ring system having ring carbon atoms and 1 to 4 ring heteroatoms provided in the aromatic ring system, each heteroatom being independently selected from nitrogen, oxygen, and sulfur ("5- to 8-membered heteroaryl"). In some embodiments, a heteroaryl group is a 5- to 6-membered aromatic ring system having ring carbon atoms and 1 to 4 ring heteroatoms provided in the aromatic ring system, each heteroatom being independently selected from nitrogen, oxygen, and sulfur ("5- to 6-membered heteroaryl"). In some embodiments, a 5- to 6-membered heteroaryl has 1 to 3 ring heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, a 5- to 6-membered heteroaryl has 1 to 2 ring heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, the 5- to 6-membered heteroaryl has one ring heteroatom selected from nitrogen, oxygen, and sulfur. Unless otherwise specified, each instance of a heteroaryl group is independently optionally substituted, i.e., unsubstituted ("unsubstituted aryl") or substituted with one or more substituents ("substituted aryl"). In certain embodiments, the heteroaryl group is an unsubstituted 5- to 14-membered heteroaryl. In certain embodiments, the heteroaryl group is a substituted 5- to 14-membered heteroaryl.

[0106] Exemplary 5-membered heteroaryl groups containing one heteroatom include, without limitation, pyrrolyl, furanyl, and thiophenyl. Exemplary 5-membered heteroaryl groups containing two heteroatoms include, without limitation, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, and isothiazolyl. Exemplary 5-membered heteroaryl groups containing three heteroatoms include, without limitation, triazolyl, oxadiazolyl, and thiadiazolyl. Exemplary 5-membered heteroaryl groups containing four heteroatoms include, without limitation, tetrazolyl. Exemplary 6-membered heteroaryl groups containing one heteroatom include, without limitation, pyridinyl. Exemplary 6-membered heteroaryl groups containing two heteroatoms include, without limitation, pyridazinyl, pyrimidinyl, and pyrazinyl. Exemplary 6-membered heteroaryl groups containing three or four heteroatoms include, without limitation, triazinyl and tetrazinyl, respectively. Exemplary 7-membered heteroaryl groups containing one heteroatom include, without limitation, azepinyl, oxepinyl, and thiepinyl. Exemplary 5,6-bicyclic heteroaryl groups include, without limitation, indolyl, isoindolyl, indazolyl, benzotriazolyl, benzothiophenyl, isobenzothiophenyl, benzofuranyl, benzisofuranyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzoxadiazolyl, benzthiazolyl, benzthiadiazolyl, indolizinyl, and purinyl. Exemplary 6,6-bicyclic heteroaryl groups include, without limitation, naphthyridinyl, pteridinyl, quinolinyl, isoquinolinyl, cinnolinyl, quinoxalinyl, phthalazinyl, and quinazolinyl.

[0107] Representative examples of heteroaryl include: [ka] In the formula, each Z is a carbonyl, N, NR 65 , O, and S; R 65 are independently hydrogen, C1-C8 alkyl, C3-C10 Cycloalkyl, 4-10 membered heterocyclyl, C6-C 10 aryl, and 5- to 10-membered heteroaryl.

[0108] "Carbocyclyl" or "carbocyclic" refers to a ring system containing 3 to 10 ring carbon atoms ("C3-C 10 In some embodiments, a carbocyclyl group has 3 to 8 ring carbon atoms ("C 3~8 In some embodiments, a carbocyclyl group has 3 to 6 ring carbon atoms ("C 3~6 In some embodiments, a carbocyclyl group has 3 to 6 ring carbon atoms ("C 3~6 In some embodiments, a carbocyclyl group has 5 to 10 ring carbon atoms ("C 5~10 carbocyclyl). Exemplary C 3~6 Carbocyclyl groups include, without limitation, cyclopropyl (C), cyclopropenyl (C), cyclobutyl (C), cyclobutenyl (C), cyclopentyl (C), cyclopentenyl (C), cyclohexyl (C), cyclohexenyl (C), cyclohexadienyl (C), and the like. 3~8 The carbocyclyl group is not limited to the above-mentioned C 3~6 Carbocyclyl groups include cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (C8), cyclooctenyl (C8), bicyclo[2.2.1]heptanyl (C7), bicyclo[2.2.2]octanyl (C8), and the like. Exemplary C 3~10 The carbocyclyl group is not limited to the above-mentioned C 3~8 Carbocyclyl groups, as well as cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C 10 ), cyclodecenyl (C 10 ), octahydro-1H-indenyl (C9), decahydronaphthalenyl (C 10), spiro[4.5]decanyl (C 10 ) and the like. Where the foregoing examples illustrate, in certain embodiments, a carbocyclyl group is either monocyclic ("monocyclic carbocyclyl") or includes a fused, bridged, or spiro ring system, such as a bicyclic system ("bicyclic carbocyclyl"), and can be saturated or partially unsaturated. "Carbocyclyl" also includes ring systems in which a carbocyclyl ring, as defined above, is fused with one or more aryl or heteroaryl groups, the point of attachment being on the carbocyclyl ring; in such instances, the number of carbons continues to designate the number of carbons in the carbocyclic ring system. Unless otherwise specified, each instance of a carbocyclyl group is independently optionally substituted, i.e., unsubstituted ("unsubstituted carbocyclyl") or substituted with one or more substituents ("substituted carbocyclyl"). In certain embodiments, a carbocyclyl group is an unsubstituted C 3~10 In certain embodiments, the carbocyclyl group is a substituted C 3~10 It is a carbocyclyl.

[0109] In some embodiments, "carbocyclyl" is a monocyclic saturated carbocyclyl group having 3 to 10 ring carbon atoms ("C 3~10 In some embodiments, a cycloalkyl group has 3 to 8 ring carbon atoms ("C 3~8 In some embodiments, a cycloalkyl group has 3 to 6 ring carbon atoms ("C 3~6 In some embodiments, a cycloalkyl group has 5 to 6 ring carbon atoms ("C 5~6 In some embodiments, a cycloalkyl group has 5 to 10 ring carbon atoms ("C 5~10 Cycloalkyl). C 5~6 Examples of cycloalkyl groups include cyclopentyl (C5) and cyclohexyl (C5). 3~6 Examples of cycloalkyl groups include the aforementioned C 5~6Cycloalkyl groups include cyclopropyl (C3) and cyclobutyl (C4). 3~8 Examples of cycloalkyl groups include the aforementioned C 3~6 Cycloalkyl groups include cycloheptyl (C7) and cyclooctyl (C8). Unless otherwise specified, each example of a cycloalkyl group is independently unsubstituted ("unsubstituted cycloalkyl") or substituted with one or more substituents ("substituted cycloalkyl"). In certain embodiments, a cycloalkyl group is an unsubstituted C 3~10 In certain embodiments, the cycloalkyl group is a substituted C 3~10 It is cycloalkyl.

[0110] "Heterocyclyl" or "heterocyclic" refers to the radical of a 3- to 10-membered non-aromatic ring system having ring carbon atoms and 1 to 4 ring heteroatoms, each independently selected from nitrogen, oxygen, sulfur, boron, phosphorus, and silicon ("3- to 10-membered heterocyclyl"). In heteroaryl groups containing one or more nitrogen atoms, the point of attachment may be at a carbon or nitrogen atom, valence permitting. Heterocyclyl groups may be either monocyclic ("monocyclic heterocyclyl") or fused, bridged, or spiro ring systems, such as bicyclic systems ("bicyclic heterocyclyl"), and may be saturated or partially unsaturated. Heterocyclyl bicyclic ring systems may contain one or more heteroatoms in one or both rings. "Heterocyclyl" also includes ring systems in which a heterocyclyl ring as defined above is fused to one or more carbocyclyl groups (the point of attachment is on either the carbocyclyl or heterocyclyl ring), or to one or more aryl or heteroaryl groups (the point of attachment is on the heterocyclyl ring); in such instances, the number of ring members continues to designate the number of ring members in the heterocyclyl ring system. Unless otherwise specified, each instance of heterocyclyl is independently optionally substituted, i.e., unsubstituted ("unsubstituted heterocyclyl") or substituted with one or more substituents ("substituted heterocyclyl"). In certain embodiments, a heterocyclyl group is an unsubstituted 3- to 10-membered heterocyclyl. In certain embodiments, a heterocyclyl group is a substituted 3- to 10-membered heterocyclyl.

[0111] In some embodiments, a heterocyclyl group is a 5- to 10-membered non-aromatic ring system having ring carbon atoms and 1 to 4 ring heteroatoms, each independently selected from nitrogen, oxygen, sulfur, boron, phosphorus, and silicon (a "5- to 10-membered heterocyclyl"). In some embodiments, a heterocyclyl group is a 5- to 8-membered non-aromatic ring system having ring carbon atoms and 1 to 4 ring heteroatoms, each independently selected from nitrogen, oxygen, and sulfur (a "5- to 8-membered heterocyclyl"). In some embodiments, a heterocyclyl group is a 5- to 6-membered non-aromatic ring system having ring carbon atoms and 1 to 4 ring heteroatoms, each independently selected from nitrogen, oxygen, and sulfur (a "5- to 6-membered heterocyclyl"). In some embodiments, a 5- to 6-membered heterocyclyl has 1 to 3 ring heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, the 5- to 6-membered heterocyclyl has 1 to 2 ring heteroatoms selected from nitrogen, oxygen, and sulfur, In some embodiments, the 5- to 6-membered heterocyclyl has 1 ring heteroatom selected from nitrogen, oxygen, and sulfur.

[0112] Exemplary 3-membered heterocyclyl groups containing one heteroatom include, without limitation, aziridinyl, oxiranyl, and thiorenyl. Exemplary 4-membered heterocyclyl groups containing one heteroatom include, without limitation, azetidinyl, oxetanyl, and thietanyl. Exemplary 5-membered heterocyclyl groups containing one heteroatom include, without limitation, tetrahydrofuranyl, dihydrofuranyl, tetrahydrothiophenyl, dihydrothiophenyl, pyrrolidinyl, dihydropyrrolyl, and pyrrolyl-2,5-dione. Exemplary 5-membered heterocyclyl groups containing two heteroatoms include, without limitation, dioxolanyl, oxasulfuranyl, disulfuranyl, and oxazolidin-2-one. Exemplary 5-membered heterocyclyl groups containing three heteroatoms include, without limitation, triazolinyl, oxadiazolinyl, and thiadiazolinyl. Exemplary 6-membered heterocyclyl groups containing one heteroatom include, without limitation, piperidinyl, tetrahydropyranyl, dihydropyridinyl, and thianyl. Exemplary 6-membered heterocyclyl groups containing two heteroatoms include, without limitation, piperazinyl, morpholinyl, dithianyl, and dioxanyl. Exemplary 6-membered heterocyclyl groups containing two heteroatoms include, without limitation, triazinanyl. Exemplary 7-membered heterocyclyl groups containing one heteroatom include, without limitation, azepanyl, oxepanyl, and thiepanyl. Exemplary 8-membered heterocyclyl groups containing one heteroatom include, without limitation, azocanyl, oxecanyl, and thiocanyl. Exemplary 5-membered heterocyclyl groups fused to a C6 aryl ring (also referred to herein as a 5,6-bicyclic heterocyclic ring) include, without limitation, indolinyl, isoindolinyl, dihydrobenzofuranyl, dihydrobenzothienyl, benzoxazolinonyl, and the like. Exemplary 6-membered heterocyclyl groups fused to an aryl ring (also referred to herein as a 6,6-bicyclic heterocyclic ring) include, without limitation, tetrahydroquinolinyl, tetrahydroisoquinolinyl, and the like.

[0113] A "nitrogen-containing heterocyclyl" group refers to a 4- to 7-membered non-aromatic cyclic group containing at least one nitrogen atom, for example, 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-alkylpiperazines such as N-methylpiperazine. Specific examples include azetidine, piperidone, and piperazone.

[0114] "Hetero," when used to describe a compound or a group present on a compound, means that one or more carbon atoms in the compound or group have been replaced by a nitrogen, oxygen, or sulfur heteroatom. Hetero can apply to any of the above hydrocarbyl groups, such as alkyl, e.g., heteroalkyl; cycloalkyl, e.g., heterocyclyl; aryl, e.g., heteroaryl; cycloalkenyl, e.g., cycloheteroalkenyl, etc., having 1 to 5, especially 1 to 3, heteroatoms.

[0115] "Acyl" is the radical -C(O)R 20 refers to R 20 is 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, as defined herein. "Alkanoyl" is an acyl group, and R 20 is a group other than hydrogen. Representative acyl groups include formyl (-CHO), acetyl (-C(=O)CH3), cyclohexylcarbonyl, cyclohexylmethylcarbonyl, benzoyl (-C(=O)Ph), benzylcarbonyl (-C(=O)CH2Ph), -C(O)-C1 to C8 alkyl, -C(O)-(CH2) t (C6~C 10 aryl), -C(O)-(CH2) t(5-10 membered heteroaryl), -C(O)-(CH2) t (C3~C 10 cycloalkyl), and -C(O)-(CH2) t (4- to 10-membered heterocyclyl), where t is an integer from 0 to 4. In certain embodiments, R 21 is C1-C8 alkyl substituted with halo or hydroxy, or C3-C 10 Cycloalkyl, 4-10 membered heterocyclyl, C6-C 10 Aryl, arylalkyl, 5-10 membered heteroaryl or heteroarylalkyl, each of which is substituted with unsubstituted C1-C4 alkyl, halo, unsubstituted C1-C4 alkoxy, unsubstituted C1-C4 haloalkyl, unsubstituted C1-C4 hydroxyalkyl, or unsubstituted C1-C4 haloalkoxy or hydroxy.

[0116] "Alkoxy" is -OR 29 R refers to the group 29 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. Particular alkoxy groups are methoxy, 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 having 1 to 6 carbon atoms. More particular alkoxy groups have 1 to 4 carbon atoms.

[0117] In certain embodiments, R 29 is amino, substituted amino, C6-C 10 Aryl, aryloxy, carboxyl, cyano, C3-C 10A group having one or more substituents, for example, 1 to 5 substituents, and particularly 1 to 3 substituents, and particularly 1 substituent, selected from the group consisting of cycloalkyl, 4- to 10-membered heterocyclyl, halogen, 5- to 10-membered heteroaryl, hydroxyl, nitro, thioalkoxy, thioaryloxy, thiol, alkyl-S(O)-, aryl-S(O)-, alkyl-S(O)2-, and aryl-S(O)2-. Exemplary "substituted alkoxy" groups include -O-(CH2) t (C6~C 10 aryl), -O-(CH2) t (5-10 membered heteroaryl), -O-(CH2) t (C3~C 10 cycloalkyl), and -O-(CH2) t (4-10 membered heterocyclyl), where t is an integer from 0 to 4, and any aryl, heteroaryl, cycloalkyl, or heterocyclyl group present can itself be substituted by unsubstituted C1-C4 alkyl, halo, unsubstituted C1-C4 alkoxy, unsubstituted C1-C4 haloalkyl, unsubstituted C1-C4 hydroxyalkyl, or unsubstituted C1-C4 haloalkoxy or hydroxy. Certain exemplary "substituted alkoxy" groups are -OCF3, -OCH2CF3, -OCH2Ph, -OCH2-cyclopropyl, -OCH2CH2OH, and -OCH2CH2NMe2.

[0118] "Amino" refers to the radical -NH2.

[0119] An "oxo group" refers to -C(=O)-.

[0120] "Substituted amino" refers to a group of the formula -N(R 38 )2, where R 38 is 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, or an amino protecting group; R 38At least one of R is not hydrogen. 38 are independently hydrogen, C1-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, C6-C 10 Aryl, 5- to 10-membered heteroaryl, 4- to 10-membered heterocyclyl, or C3-C 10 cycloalkyl; or C1-C8 alkyl substituted with halo or hydroxy; C3-C8 alkenyl substituted with halo or hydroxy, C3-C8 alkynyl substituted with halo or hydroxy, or -(CH2) t (C6~C 10 aryl), -(CH2) t (5-10 membered heteroaryl), -(CH2) t (C3~C 10 cycloalkyl), or -(CH2) t (4-10 membered heterocyclyl), and t is an integer from 0 to 8, each of which is substituted by unsubstituted C1-C4 alkyl, halo, unsubstituted C1-C4 alkoxy, unsubstituted C1-C4 haloalkyl, unsubstituted C1-C4 hydroxyalkyl, or unsubstituted C1-C4 haloalkoxy or hydroxy, or both R 38 are joined to form an alkylene group.

[0121] Exemplary "substituted amino" groups include -NR 39 -C1-C8 alkyl, -NR 39 -(CH2) t (C6~C 10 aryl), -NR 39 -(CH2) t (5-10 membered heteroaryl), -NR 39 -(CH2) t (C3~C 10 cycloalkyl), and -NR 39 -(CH2) t (4-10 membered heterocyclyl), where t is an integer of 0 to 4, for example, 1 or 2, and each R 39independently represent H or C1-C8 alkyl, and any alkyl group present may itself be substituted by halo, substituted or unsubstituted amino, or hydroxy, and any aryl, heteroaryl, cycloalkyl, or heterocyclyl group present may itself be substituted by unsubstituted C1-C4 alkyl, halo, unsubstituted C1-C4 alkoxy, unsubstituted C1-C4 haloalkyl, unsubstituted C1-C4 hydroxyalkyl, or unsubstituted C1-C4 haloalkyl or hydroxy. For the avoidance of doubt, the term "substituted amino" includes alkylamino, substituted alkylamino, alkylarylamino, substituted alkylarylamino, arylamino, substituted arylamino, dialkylamino, and substituted dialkylamino groups as defined below. Substituted amino includes both mono- and di-substituted amino groups.

[0122] "Carboxy" refers to the radical --C(O)OH.

[0123] "Cyano" refers to the radical -CN.

[0124] "Halo" or "halogen" refers to fluoro (F), chloro (Cl), bromo (Br), and iodo (I). In certain embodiments, a halo group is either fluoro or chloro.

[0125] "Haloalkyl" refers to an alkyl radical in which the alkyl group is substituted with one or more halogens. Typical haloalkyl groups include, but are not limited to, trifluoromethyl, difluoromethyl, fluoromethyl, chloromethyl, dichloromethyl, dibromoethyl, tribromomethyl, tetrafluoroethyl, and the like.

[0126] "Hydroxy" refers to the radical --OH.

[0127] "Nitro" refers to the radical -NO2.

[0128] "Thioketo" refers to the =S group.

[0129] Alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl groups defined herein are optionally substituted (e.g., a "substituted" or "unsubstituted" alkyl, a "substituted" or "unsubstituted" alkenyl, a "substituted" or "unsubstituted" alkynyl, a "substituted" or "unsubstituted" carbocyclyl, a "substituted" or "unsubstituted" heterocyclyl, a "substituted" or "unsubstituted" aryl, or a "substituted" or "unsubstituted" heteroaryl group). In general, the term "substituted," whether preceded by the term "optionally," means that at least one hydrogen present on the group (e.g., a carbon or nitrogen atom) is replaced with a permissible substituent, e.g., a substituent that, upon substitution, gives rise to a stable compound, e.g., a compound that does not undergo spontaneous transformation, such as by rearrangement, cyclization, elimination, or other reaction. Unless otherwise specified, a "substituted" group has a substituent at one or more substitutable positions of the group, and when more than one position in any given structure is substituted, the substituents are either the same or different at each position. The term "substituted" is intended to include substitution with all permissible substituents of organic compounds, among the substituents described herein, that result in the formation of a stable compound. The present invention contemplates any and all such combinations in order to arrive at a stable compound. For purposes of this invention, heteroatoms such as nitrogen may have hydrogen substituents and / or any suitable substituents described herein that satisfy the valence of the heteroatom and result in the formation of a stable moiety.

[0130] Exemplary carbon atom substituents include halogen, -CN, -NO2, -N3, -SO2H, -SO3H, -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 、-CO2H、-CHO、-C(OR cc )2、-CO2R aa 、-OC(=O)R aa 、-OCO2R aa 、-C(=O)N(R bb )2、-OC(=O)N(R bb )2、-NR bb C(=O)R aa 、-NR bb CO2R 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 SO2R aa 、-NR bb SO2R aa 、-SO2N(R bb )2、-SO2R aa 、-SO2OR aa 、-OSO2R aa 、-S(=O)R aa 、-OS(=O)R aa 、-Si(R aa )3、-OSi(R aa )3-C(=S)N(R bb )2、-C(=O)SR aa 、-C(=S)SR aa 、-SC(=S)SR aa 、-SC(=O)SR aa 、-OC(=O)SR aa 、-SC(=O)OR aa 、-SC(=O)R aa 、-P(=O)2R aa, -OP(=O)2R aa , -P(=O)(R aa )2, -OP(=O)(R aa )2, -OP(=O)(OR cc )2, -P(=O)2N(R bb )2, -OP(=O)2N(R bb )2, -P(=O)(NR bb )2, -OP(=O)(NR bb )2, -NR bb P(=O)(OR cc )2, -NR bb P(=O)(NR bb )2, -P(R cc )2, -P(R cc )3, -OP(R cc )2, -OP(R cc )3, -B(R aa )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- to 14-membered heterocyclyl, C 6~14 and 5- to 14-membered heteroaryl, each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl independently having 0, 1, 2, 3, 4, or 5 R dd groups, or the two geminal hydrogens on the carbon atom are substituted with groups =O, =S, =NN(R bb )2, =NNR bb C(=O)R aa , =NNR bb C(=O)OR aa , =NNR bb S(=O)2R aa , =NR bb , or =NOR cc is replaced by R aa Each instance of is independently C 1~10 Alkyl, C 1~10 Haloalkyl, C2~10 Alkenyl, C 2~10 Alkynyl, C 3~10 Carbocyclyl, 3- to 14-membered heterocyclyl, C 6~14 aryl, and 5- to 14-membered heteroaryl, or two R aa groups joined to form a 3- to 14-membered heterocyclyl or 5- to 14-membered heteroaryl ring, and each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl independently contains 0, 1, 2, 3, 4, or 5 R dd is substituted with a group, R bb Each instance of is independently hydrogen, -OH, -OR aa , -N(R cc )2, -CN, -C(=O)R aa , -C(=O)N(R cc )2, -CO2R aa , -SO2R aa , -C(=NR cc ) OR aa , -C(=NR cc )N(R cc )2, -SO2N(R cc )2, -SO2R cc , -SO2OR cc , -SOR aa , -C(=S)N(R cc )2, -C(=O)SR cc , -C(=S)SR cc , -P(=O)2R aa , -P(=O)(R aa )2, -P(=O)2N(R cc )2, -P(=O)(=NR cc )2, C 1~10 Alkyl, C 1~10 Haloalkyl, C 2~10 Alkenyl, C 2~10 Alkynyl, C 3~10 Carbocyclyl, 3- to 14-membered heterocyclyl, C 6~14 aryl, and 5- to 14-membered heteroaryl, or two R bbgroups joined to form a 3- to 14-membered heterocyclyl or 5- to 14-membered heteroaryl ring, and each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl independently contains 0, 1, 2, 3, 4, or 5 R dd is substituted with a group, R cc Each instance 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- to 14-membered heterocyclyl, C 6~14 aryl, and 5- to 14-membered heteroaryl, or two R cc groups joined to form a 3- to 14-membered heterocyclyl or 5- to 14-membered heteroaryl ring, and each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl independently contains 0, 1, 2, 3, 4, or 5 R dd is substituted with a group, R dd Each example of is independently a halogen, -CN, -NO2, -N3, -SO2H, -SO3H, -OH, -OR ee , -ON(R ff )2, -N(R ff )2, -N(R ff )3 + X - , -N(OR ee )R ff , -SH, -SR ee , -SSR ee , -C(=O)R ee , -CO2H, -CO2R ee , -OC(=O)R ee , -OCO2R ee , -C(=O)N(R ff )2, -OC(=O)N(R ff )2, -NR ff C(=O)R ee , -NR ff CO2R 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(=NR ff )N(R ff )2, -OC(=NR ff )N(R ff )2, -NR ff C(=NR ff )N(R ff )2, -NR ff SO2R ee , -SO2N(R ff )2, -SO2R ee , -SO2OR ee , -OSO2R 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)2R ee , -P(=O)(R ee )2, -OP(=O)(R ee )2, -OP(=O)(OR ee )2, C 1~6 Alkyl, C 1~6 Haloalkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Carbocyclyl, 3-10 membered heterocyclyl, C 6~10 aryl, and 5- to 10-membered heteroaryl, each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl independently having 0, 1, 2, 3, 4, or 5 R gg substituted with a group or two geminal R dd the substituents can be joined to form =O or =S; R ee Each instance of is independently C 1~6 Alkyl, C 1~6Haloalkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Carbocyclyl, C 6~10 aryl, 3- to 10-membered heterocyclyl, and 3- to 10-membered heteroaryl, each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl independently having 0, 1, 2, 3, 4, or 5 R gg is substituted with a group, R ff Each instance 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 heterocyclyl, C 6~10 aryl, and 5- to 10-membered heteroaryl, or two R ff groups joined to form a 3- to 14-membered heterocyclyl or 5- to 14-membered heteroaryl ring, and each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl independently contains 0, 1, 2, 3, 4, or 5 R gg is substituted with a group, R gg Each example of is independently a halogen, -CN, -NO2, -N3, -SO2H, -SO3H, -OH, -OC 1~6 Alkyl, -ON(C 1~6 alkyl)2, -N(C 1~6 alkyl)2, -N(C 1~6 alkyl)3 + X - , -NH(C 1~6 alkyl)2 + X - , -NH2(C 1~6 alkyl) + X - , -NH3 + X - , -N(OC 1~6 Alkyl)(C 1~6 alkyl), -N(OH)(C 1~6 alkyl), -NH(OH), -SH, -SC1~6 Alkyl, -SS(C 1~6 alkyl), -C(=O)(C 1~6 alkyl), -CO2H, -CO2(C 1~6 alkyl), -OC(=O)(C 1~6 alkyl), -OCO2(C 1~6 alkyl), -C(=O)NH2, -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), -NHCO2(C 1~6 alkyl), -NHC(=O)N(C 1~6 alkyl)2, -NHC(=O)NH(C 1~6 alkyl), -NHC(=O)NH2, -C(=NH)O(C 1~6 alkyl), -OC(=NH)(C 1~6 alkyl), -OC(=NH)OC 1~6 Alkyl, -C(=NH)N(C 1~6 alkyl)2, -C(=NH)NH(C 1~6 alkyl), -C(=NH)NH2, -OC(=NH)N(C 1~6 alkyl)2, -OC(NH)NH(C 1~6 alkyl), -OC(NH)NH2, -NHC(NH)N(C 1~6 alkyl)2, -NHC(=NH)NH2, -NHSO2(C 1~6 alkyl), -SO2N(C 1~6 alkyl)2, -SO2NH(C 1~6 alkyl), -SO2NH2, -SO2C 1~6 Alkyl, -SO2OC 1~6 Alkyl, -OSO2C 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)NH2, -C(=O)S(C 1~6alkyl), -C(=S)SC 1~6 Alkyl, -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 Alkenyl, C 2~6 Alkynyl, C 3~10 Carbocyclyl, C 6~10 aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, or two geminal R gg The substituents can be joined to form =O or =S, and X - is the counter ion.

[0131] A "counterion" or "anionic counterion" is a negatively charged group associated with a cationic quaternary amino group to maintain electron neutrality. Exemplary counterions include halide ions (e.g., F - , Cl - , B - , I - ), NO3 - , ClO4 - , O.H. - , H2PO4 - , HSO4 - , sulfonate ions (e.g., methanesulfonate, trifluoromethanesulfonate, p-toluenesulfonate, benzenesulfonate, 10-camphorsulfonate, naphthalene-2-sulfonate, naphthalene-1-sulfonic acid-5-sulfonate, ethane-1-sulfonic acid-2-sulfonate, etc.), and carboxylate ions (e.g., acetate, ethanoate, propanoate, benzoate, glycerate, lactate, tartrate, glycolate, etc.).

[0132] These and other exemplary substituents are described in further detail in the detailed description and claims. The present invention is not intended to be limited in any way by the above recitation of exemplary substituents.

[0133] Other definitions As used herein, the term "modulation" refers to the A "Modulators" (e.g., modulatory compounds) refer to the inhibition or enhancement of receptor function, e.g., GABA receptors. A It can be an agonist, partial agonist, antagonist, or partial antagonist of the receptor.

[0134] "Pharmaceutically acceptable" means approved or approvable by a regulatory agency of a federal or state government or a corresponding agency in a country other than the United States, or listed in the United States Pharmacopoeia or other generally recognized pharmacopeia for use in animals, and more particularly in humans.

[0135] "Pharmaceutically acceptable salts" refers to salts of the compounds of the present invention that are pharmaceutically acceptable and possess the desired pharmacological activity of the parent compound. In particular, such salts are non-toxic and can be inorganic or organic acid addition salts and base addition salts. Specifically, such salts include: (1) acid addition salts formed with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like; or salts formed with acetic acid, propionic acid, hexanoic acid, cyclopentanepropionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, succinic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, 3-(4-hydroxybenzoic acid)benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic acid, 2-naphthalenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, 4- or (2) salts formed when an acidic proton present in the parent compound is replaced by a metal ion, e.g., an alkali metal ion, an alkaline earth ion, or an aluminum ion, or an equivalent organic base, such as ethanolamine, diethanolamine, triethanolamine, N-methylglucamine, etc. Salts include, by way of example only, salts of non-toxic organic or inorganic acids such as sodium, potassium, calcium, magnesium, ammonium, tetraalkylammonium, etc., and, if the compound contains a basic functional group, salts of non-toxic organic or inorganic acids such as hydrochloride, hydrobromide, tartrate, mesylate, acetate, maleate, oxalate, etc. The term "pharmaceutically acceptable cation" refers to an acceptable cationic counterion of an acidic functional group. Such cations are exemplified by sodium, potassium, calcium, magnesium, ammonium, tetraalkylammonium cations, etc. See, e.g., Berge, et al., J. Pharm. Sci. (1977) 66(1):1-79.

[0136] The term "prodrug" is intended to encompass therapeutically inactive compounds that are converted into the therapeutically active agents of the present invention under physiological conditions. One method for creating a prodrug is to design a selected moiety that is hydrolyzed or cleaved at the target in vivo site of action under physiological conditions, thereby revealing the desired molecule that then produces its therapeutic effect. In certain embodiments, the prodrug is converted by the enzyme activity of the target.

[0137] In an alternative embodiment, the present invention provides a prodrug of a compound of formula (1-I), (2-I) or (3-I), wherein the prodrug comprises a cleavable moiety on the C3 hydroxy as shown in formula (1-I), (2-I) or (3-I).

[0138] "Tautomers" refer to compounds that are interchangeable forms of a particular compound structure, altered by the displacement of hydrogen atoms and electrons. Thus, two structures can be in equilibrium through the shifting of π electrons and atoms (usually H). For example, enols and ketones are tautomers because they are rapidly interconverted by treatment with either acid or base. Another example of tautomerism is phenylnitromethane, whose acetyl and nitro forms are similarly formed by treatment with acid or base. Tautomeric forms can be relevant to achieving optimal chemical reactivity and biological activity of a desired compound.

[0139] "Subjects" to which administration is contemplated include, but are not limited to, humans (i.e., males or females of any age group, e.g., pediatric subjects (e.g., infants, children, adolescents) or adult subjects (e.g., young adults, middle-aged adults, or elderly adults)) and / or non-human animals, e.g., mammals such as primates (e.g., cynomolgus monkeys, rhesus monkeys), cows, pigs, horses, sheep, goats, rodents, cats, and / or dogs. In certain embodiments, the subject is a human ("human subject"). In certain embodiments, the subject is a non-human animal.

[0140] In certain embodiments, the substituent present on the oxygen atom is an oxygen protecting group (also referred to as a hydroxyl protecting group). Oxygen protecting groups include -R aa , -N(R bb )2, -C(=O)SR aa , -C(=O)R aa , -CO2R 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 , -SO2R aa , -Si(R aa )3, -P(R cc )2, -P(R cc )3, -P(=O)2R aa , -P(=O)(R aa )2, -P(=O)(OR cc )2, -P(=O)2N(R bb )2, and -P(=O)(NR bb ) 2, and R aa , R bb , and R cc is as defined herein. Oxygen protecting groups are well known in the art and include those described in detail in Protecting Groups in Organic Synthesis, T.W. Greene and P.G.M. Butts, 3rd edition, John Wiley & Sons, 1999, which is incorporated herein by reference.

[0141] Exemplary oxygen protecting groups include, but are not limited to, methyl, methoxylmethyl (MOM), 2-methoxyethoxymethyl (MEM), benzyl (Bn), triisopropylsilyl (TIPS), t-butyldimethylsilyl (TBDMS), t-butylmethoxyphenylsilyl (TBMPS), methanesulfonate (mesylate), and tosylate (Ts).

[0142] In certain embodiments, the substituent present on the sulfur atom is a sulfur protecting group (also referred to as a thiol protecting group). Sulfur protecting groups include -R aa , -N(R bb )2, -C(=O)SR aa , -C(=O)R aa , -CO2R 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 , -SO2R aa , -Si(R aa )3, -P(R cc )2, -P(R cc )3, -P(=O)2R aa , -P(=O)(R aa )2, -P(=O)(OR cc )2, -P(=O)2N(R bb )2, and -P(=O)(NR bb ) 2, and R aa , R bb , and R cc is as defined herein. Sulfur protecting groups are well known in the art and include those described in detail in Protecting Groups in Organic Synthesis, T.W. Greene and P.G.M. Butts, 3rd edition, John Wiley & Sons, 1999, which is incorporated herein by reference.

[0143] In certain embodiments, the substituent present on the nitrogen atom is an amino protecting group (also referred to herein as a 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)2R aa , -C(=NRcc )R aa , -C(=NR cc ) OR aa , -C(=NR cc )N(R cc )2, -SO2N(R cc )2, -SO2R cc , -SO2OR 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- to 14-membered heterocyclyl, C 6~14 and 5- to 14-membered heteroaryl groups, each alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl independently having 0, 1, 2, 3, 4, or 5 R dd substituted with R aa , R bb , R cc and R dd is as defined herein. Amino protecting groups are well known in the art and include those described in detail in Protecting Groups in Organic Synthesis, T.W. Greene and P.G.M. Butts, 3rd edition, John Wiley & Sons, 1999, which is incorporated herein by reference.

[0144] Exemplary amino-protecting groups include, but are not limited to, amide groups (e.g., —C(═O)R aa ; carbamate groups (e.g., —S(═O)R ), including, but not limited to, 9-fluorenylmethyl carbamate (Fmoc), t-butyl carbamate (BOC), and benzyl carbamate (Cbz); aasulfonamide groups (e.g., —S(═O)R ), including, but not limited to, p-toluenesulfonamide (Ts), methanesulfonamide (Ms), and N-[2-(trimethylsilyl)ethoxy]methylamine (SEM); aa ), but are not limited to these.

[0145] Disease, disorder, and condition are used interchangeably herein.

[0146] As used herein, unless otherwise specified, the terms "treat," "treating," and "treatment" contemplate the action of reducing the severity of the disease, disorder, or condition or delaying or slowing the progression of the disease, disorder, or condition (also, "therapeutic treatment"), occurring while a subject is afflicted with the specified disease, disorder, or condition.

[0147] "Prophylactic treatment" contemplates an effect that occurs before a subject begins to suffer from the named disease, disorder, or condition.

[0148] Generally, the "effective amount" of a compound refers to an amount sufficient to induce a desired biological response, for example, to treat a CNS-related disorder, and is sufficient to induce anesthesia or sedation.As will be understood by those skilled in the art, the effective amount of the compound of the present invention can vary depending on factors such as the desired biological endpoint, the pharmacokinetics of the compound, the disease being treated, the mode of administration, and the age, weight, health and condition of the subject.

[0149] As used herein, and unless otherwise specified, a "therapeutically effective amount" of a compound is an amount sufficient to provide a therapeutic benefit in the treatment of a disease, disorder, or condition, or to delay or minimize one or more symptoms associated with the disease, disorder, or condition. A therapeutically effective amount of a compound refers to an amount of a therapeutic agent that, alone or in combination with other therapies, provides a therapeutic benefit in the treatment of a disease, disorder, or condition. The term "therapeutically effective amount" can encompass an amount that improves overall therapy, reduces or avoids the symptoms or causes of a disease or condition, or enhances the therapeutic efficacy of another therapeutic agent.

[0150] In an alternative embodiment, the present invention contemplates administering a compound of the present invention, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable composition thereof, as a preventative agent before a subject begins to suffer from a particular disease, disorder, or condition. As used herein, and unless otherwise specified, a "prophylactically effective amount" of a compound is an amount sufficient to prevent a disease, disorder, or condition, or one or more symptoms associated with a disease, disorder, or condition, or to prevent its recurrence. A prophylactically effective amount of a compound refers to the amount of a therapeutic agent that, alone or in combination with other agents, provides a prophylactic benefit in the prevention of a disease, disorder, or condition. The term "prophylactically effective amount" can encompass an amount that improves overall prevention or enhances the prophylactic efficacy of another prophylactic agent.

[0151] compound It is understood that the formulas set forth herein may refer to specific carbon atoms, such as C17, C3, C19, etc. These references are based on the position of the carbon atoms according to steroid nomenclature known and used in the industry, as shown below. [ka] For example, C17 refers to the 17th carbon, and C3 refers to the 3rd carbon.

[0152] In one aspect, provided herein is a compound of formula (1-I): [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, q is independently 0, 1, 2, or 3; r is independently 0, 1, or 2; s is independently 0, 1, or 2; t is independently 0, 1, 2, or 3; n is independently 1 or 2; u is independently 1 or 2; X 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 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 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)2R A2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1Each instance 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 heteroaryl, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or a nitrogen protecting group when attached to a nitrogen atom; A2 each instance of 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, or substituted or unsubstituted heteroaryl; R 5 is hydrogen or methyl, or [ka] is a double bond, R 5 and R 6a Or R 6b One of them does not exist, R 19 is hydrogen or substituted or unsubstituted alkyl; R 18 is a substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 3 is 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; R 6a and R 6b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 2a, R 2b , R 4a , R 4b , R 11a , R 11b , R 16a , or R 16b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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 heteroaryl, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 2a and R 2b , or R 4a and R 4b , or R 11a and R 11b , or R 16a and R 16b is bonded to form an oxo (=O) group, however, The condition is that q, s, r, u, and t are not all 1 at the same time.

[0153] In some embodiments of the compound of Formula (1-I), when t is 0, 2, or 3, q, u, s, and r are not simultaneously 1. In some embodiments of the compound of Formula (1-I), when q is 0 or 2 and u is 1, t, s, and r are not simultaneously 1. In some embodiments of the compound of Formula (1-I), when u is 2 and q is 1, t, s, and r are not simultaneously 1. In some embodiments of the compound of Formula (1-I), when r is 0 or 2, q, u, s, and t are not simultaneously 1. In some embodiments of the compound of Formula (1-I), when s is 0 or 2, q, u, r, and t are not simultaneously 1.

[0154] In one embodiment, provided herein is a compound of formula (1-Va) or formula (1-Vb): [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, n is 1 or 2, X 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 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 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)2RA2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1 Each instance 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 heteroaryl, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or a nitrogen protecting group when attached to a nitrogen atom; A2 each instance of 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, or substituted or unsubstituted heteroaryl; R 5 is hydrogen or methyl, or [ka] is a double bond, R 5 does not exist, R 19 is hydrogen or substituted or unsubstituted alkyl; R 18 is a substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 3 is 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; R 6a and R 6beach is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, and R 2a , R 2b , R 4a , R 4b , R 11a , R 11b , R 16a , or R 16b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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 heteroaryl, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 2a and R 2b , or R 4a and R 4b , or R 11a and R 11b , or R 16a and R 16b Any one of the following is joined to form an oxo (=O) group.

[0155] In some embodiments, [ka] is a single bond. [ka] is a double bond.

[0156] In some embodiments, R 2a , R 2b , R 4a , R 4b , R 6a , R 6b , R 11a , R 11b , R 16a , or R 16b each independently represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, —OH, or —OR D1 or R 2a and R 2b , or R 4a and R 4b , or R 11a and R 11b , or R 16a and R 16b are joined to form an oxo (=O) group, and each alkyl is selected from halo, -OH, or -OR D1 and each R is optionally substituted with a substituent selected from D1 is independently hydrogen, haloalkyl, or unsubstituted alkyl.

[0157] In some embodiments, R 2a , R 2b , R 4a , R 4b , R 6a , R 6b , R 11a , R 11b , R 16a , or R 16b is hydrogen.

[0158] In some embodiments, provided herein are compounds of formula 2-I: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 5 and R 6a or R 6b provided that one of R 3 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 unsubstituted heteroaryl; R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 15a , and R 15b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -ORD1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 1a and R 1b , R 2a and R 2b , R 4a and R 4b , R 11a and R 11b , R 12a and R 12b , and R 15a and R 15b is joined to form an oxo (=O) group, R 16a and R 16b each independently represents 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 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)OR A1 , -SC(=O)SRA1 , -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)2R A2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1 Each instance 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 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, -SOR A2 , -C(O)R A2 or two R A1 groups are joined to form a substituted or unsubstituted heterocyclic 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 unsubstituted heteroaryl; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 28 is 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, -OR A1 , -N(R A1 )2, -SRA1 、-C(=O)R A1 、-C(=O)OR A1 、-C(=O)SR A1 、-C(=O)N(R A1 )2、-OC(=O)R A1 、-OC(=O)OR A1 、-OC(=O)N(R A1 )2、-OC(=O)SR A1 、-OS(=O)2R A1 、-OS(=O)2OR A1 、-OS(=O)2N(R A1 )2、-N(R A1 )C(=O)R A1 、-N(R A1 )C(=NR A1 )R A1 、-N(R A1 )C(=O)OR A1 、-N(R A1 )C(=O)N(R A1 )2、-N(R A1 )C(=NR A1 )N(R A1 )2、-N(R A1 )S(=O)2R A1 、-N(R A1 )S(=O)2OR A1 、-N(R A1 )S(=O)2N(R A1 )2、-SC(=O)R A1 、-SC(=O)OR A1 、-SC(=O)SR A1 、-SC(=O)N(R A1 )2、-S(=O)2R A1 、-S(=O)2OR A1 、または-S(=O)2N(R A1 )2であり、R A1each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; n is 1, 2, or 3, However, the compound is [ka] The condition is that it is not.

[0159] In another aspect, provided herein is a method of treating a CNS-related disorder in a subject in need thereof, comprising administering to the subject a compound of formula 2-I: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 5 and R 6a or R 6b provided that one of R 3 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 unsubstituted heteroaryl; R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 15a , and R 15b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 1a and R 1b , R 2a and R 2b , R 4a and R 4b , R11a and R 11b , R 12a and R 12b , and R 15a and R 15b is joined to form an oxo (=O) group, R 16a and R 16b each independently represents 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 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)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)2R A2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1Each instance 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 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, -SOR A2 , -C(O)R A2 or two R A1 groups are joined to form a substituted or unsubstituted heterocyclic 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 unsubstituted heteroaryl; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 28 is 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, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(RA1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; n is 1, 2, or 3.

[0160] In some embodiments, the compound of formula 2-I is a compound of formula 2-Ia or formula 2-Ib: [ka] or a pharmaceutically acceptable salt thereof.

[0161] In some embodiments, the compound of formula 2-I is a compound of formula 2-Iaa or formula 2-Iab: [ka] or a pharmaceutically acceptable salt thereof.

[0162] In some embodiments, provided herein are compounds of formula 2-II: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, t is 1 or 2, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 5 and R 6a or R 6b provided that one of R 3 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 unsubstituted heteroaryl; R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 1a, R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 30a , and R 30b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 1a and R 1b , R 2a and R 2b , R 4a and R 4b , R 11a and R 11b , R 12a and R 12b , and R 30a and R 30b is joined to form an oxo (=O) group, R 29a and R 29beach independently represents 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 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)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)2R A2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1 Each instance 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 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, -SOR A2 , -C(O)R A2 or two R A1 groups are joined to form a substituted or unsubstituted heterocyclic or heteroaryl ring, RA2 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 unsubstituted heteroaryl; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 28 is 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, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(RA1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; n is 1, 2, or 3.

[0163] In some embodiments, the compound of Formula 2-II is a compound of Formula 2-IIa: [ka] or a pharmaceutically acceptable salt thereof.

[0164] In some embodiments, provided herein are compounds of formula 2-III: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 5 and R 6a or R 6b provided that one of R 3is 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 unsubstituted heteroaryl; R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , and R 12b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1Each instance 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, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 1a and R 1b , R 2a and R 2b , R 4a and R 4b , R 11a and R 11b , R 12a and R 12b is joined to form an oxo (=O) group, R 31a and R 31b each independently represents 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 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)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)2RA2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1 Each instance 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 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, -SOR A2 , -C(O)R A2 or two R A1 groups are joined to form a substituted or unsubstituted heterocyclic 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 unsubstituted heteroaryl; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 28 is 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, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1, -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; n is 1, 2, or 3.

[0165] In some embodiments, the compound of Formula 2-III is a compound of Formula 2-IIIa: [ka] or a pharmaceutically acceptable salt thereof.

[0166] In some embodiments, provided herein are compounds of formula 2-IVa or 2-IVb: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 5 and R 6a or R 6b provided that one of R 3 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 unsubstituted heteroaryl; R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 1a , R 1b , R2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 15a , and R 15b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 1a and R 1b , R 2a and R 2b , R 4a and R 4b , R 11a and R 11b , R 12a and R 12b , and R 15a and R 15b is joined to form an oxo (=O) group, R 16a and R 16beach independently represents 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 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)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)2R A2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1 Each instance 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 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, -SOR A2 , -C(O)R A2 or two R A1 groups are joined to form a substituted or unsubstituted heterocyclic or heteroaryl ring, RA2 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 unsubstituted heteroaryl; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 28 is 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, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(RA1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; n is 1, 2, or 3; m is 2 or 3.

[0167] In some embodiments, the compound of formula 2-IV is a compound of formula 2-IVaa or formula 2-IVba: [ka] or a pharmaceutically acceptable salt thereof.

[0168] In some embodiments, provided herein are compounds of formula 2-V: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 5 and R 6a or R 6bprovided that one of R 3 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 unsubstituted heteroaryl; R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 15a , and R 15b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1Each instance 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, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 1a and R 1b , R 2a and R 2b , R 4a and R 4b , R 11a and R 11b , R 12a and R 12b , and R 15a and R 15b is joined to form an oxo (=O) group, R 16a and R 16b each independently represents 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 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)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)2R A2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1 Each instance 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 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, -SOR A2 , -C(O)R A2 or two R A1 groups are joined to form a substituted or unsubstituted heterocyclic 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 unsubstituted heteroaryl; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 28 is 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, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)RA1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; n is 1, 2, or 3.

[0169] In some embodiments, the compound of formula 2-V is a compound of formula 2-Va: [ka] or a pharmaceutically acceptable salt thereof.

[0170] In some embodiments, provided herein are compounds of formula 2-VI: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 5 and R 36a or R 36b provided that one of R 3 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 unsubstituted heteroaryl; R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] is a double bond, R 5 does not exist, R 36a and R 36b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 36a and R 36b is joined to form an oxo (=O) group, R 1a , R 1b , R2a , R 2b , R 4a , R 4b , R 11a , R 11b , R 12a , R 12b , R 15a , R 15b , R 34a , R 34b , R 35a , and R 35b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 1a and R 1b , R 2a and R 2b , R 4a and R 4b , R 11a and R 11b , R 12a and R 12b , and R 15a and R 15b is joined to form an oxo (=O) group, R 16a and R 16beach independently represents 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 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)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)2R A2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1 Each instance 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 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, -SOR A2 , -C(O)R A2 or two R A1 groups are joined to form a substituted or unsubstituted heterocyclic or heteroaryl ring, RA2 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 unsubstituted heteroaryl; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 28 is 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, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(RA1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; n is 1, 2, or 3.

[0171] In some embodiments, the compound of Formula 2-VI is a compound of Formula 2-VIa: [ka] or a pharmaceutically acceptable salt thereof.

[0172] In some embodiments, provided herein are compounds of formula 2-VII: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 5 and R 36a or R 36b provided that one of R 3is 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 unsubstituted heteroaryl; R 5 is hydrogen or substituted or unsubstituted methyl, or [ka] is a double bond, R 5 does not exist, R 37a and R 37b each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 37a and R 37b is joined to form an oxo (=O) group, R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 11a , R 11b , R 12a , R 12b , R 15a , and R 15b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1Each instance 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, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R D1 groups are joined to form a substituted or unsubstituted heterocyclic ring, or R 1a and R 1b , R 2a and R 2b , R 4a and R 4b , R 11a and R 11b , R 12a and R 12b , and R 15a and R 15b is joined to form an oxo (=O) group, R 16a and R 16b each independently represents 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 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)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)2R A2 , -OS(=O)2OR A1 , -SS(=O)2R A2 , -SS(=O)2OR A1 , -S(=O)R A2 , -SO2R A2 , or -S(=O)2OR A1 and R A1 Each instance 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 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, -SOR A2 , -C(O)R A2 or two R A1 groups are joined to form a substituted or unsubstituted heterocyclic 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 unsubstituted heteroaryl; R 19 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R 28 is 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, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)RA1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; n is 1, 2, or 3.

[0173] In some embodiments, the compound of Formula 2-VII is a compound of Formula 2-VIIa: [ka] or a pharmaceutically acceptable salt thereof.

[0174] In one aspect, provided herein are compounds of formula 3-I: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(RA1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17beach independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3, -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 18 is a substituted or unsubstituted alkyl; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2.

[0175] In some embodiments, provided herein are compounds of formula 3-Ix: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1)C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17beach independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3, -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 18 is a substituted or unsubstituted alkyl; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2.

[0176] In some embodiments, the compound of formula I is a compound of formula 3-IIa or formula IIb. [ka]

[0177] In another embodiment, the compound is a compound of formula 3-III: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1)2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1, or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(RC3 )2、-SR C3 、-C(=O)R C3 、-C(=O)OR C3 、-C(=O)SR C3 、-C(=O)N(R C3 )2、-OC(=O)R C3 、-OC(=O)OR C3 、-OC(=O)N(R C3 )2、-OC(=O)SR C3 、-OS(=O)2R C3 、-OS(=O)2OR C3 、-OS(=O)2N(R C3 )2、-N(R C3 )C(=O)R C3 、-N(R C3 )C(=NR C3 )R C3 、-N(R C3 )C(=O)OR C3 、-N(R C3 )C(=O)N(R C3 )2、-N(R C3 )C(=NR C3 )N(R C3 )2、-N(R C3 )S(=O)2R C3 、-N(R C3 )S(=O)2OR C3 、-N(R C3 )S(=O)2N(R C3 )2、-SC(=O)R C3 、-SC(=O)OR C3 、-SC(=O)SR C3 、-SC(=O)N(R C3 )2、-S(=O)2R C3 、-S(=O)2OR C3 、または-S(=O)2N(R C3 )2であり、R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2; t is 2 or 3.

[0178] In another embodiment, the compound is a compound of formula 3-IIIx: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)ORA1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a, R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2RA1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16beach independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2; t is 2 or 3.

[0179] In some further embodiments, the compound is a compound of formula 3-IV: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1, -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1)2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a and R 15b each independently represents hydrogen, halogen, —CN, —NO, 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 C3、-N(R C3 )2、-SR C3 、-C(=O)R C3 、-C(=O)OR C3 、-C(=O)SR C3 、-C(=O)N(R C3 )2、-OC(=O)R C3 、-OC(=O)OR C3 、-OC(=O)N(R C3 )2、-OC(=O)SR C3 、-OS(=O)2R C3 、-OS(=O)2OR C3 、-OS(=O)2N(R C3 )2、-N(R C3 )C(=O)R C3 、-N(R C3 )C(=NR C3 )R C3 、-N(R C3 )C(=O)OR C3 、-N(R C3 )C(=O)N(R C3 )2、-N(R C3 )C(=NR C3 )N(R C3 )2、-N(R C3 )S(=O)2R C3 、-N(R C3 )S(=O)2OR C3 、-N(R C3 )S(=O)2N(R C3 )2、-SC(=O)R C3 、-SC(=O)OR C3 、-SC(=O)SR C3 、-SC(=O)N(R C3 )2、-S(=O)2R C3 、-S(=O)2OR C3 、または-S(=O)2N(R C3 )2であり、R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2.

[0180] In other embodiments, the compound is a compound of formula 3-Va or formula 3-Vb: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1, -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1, -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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, —ORC3 、-N(R C3 )2、-SR C3 、-C(=O)R C3 、-C(=O)OR C3 、-C(=O)SR C3 、-C(=O)N(R C3 )2、-OC(=O)R C3 、-OC(=O)OR C3 、-OC(=O)N(R C3 )2、-OC(=O)SR C3 、-OS(=O)2R C3 、-OS(=O)2OR C3 、-OS(=O)2N(R C3 )2、-N(R C3 )C(=O)R C3 、-N(R C3 )C(=NR C3 )R C3 、-N(R C3 )C(=O)OR C3 、-N(R C3 )C(=O)N(R C3 )2、-N(R C3 )C(=NR C3 )N(R C3 )2、-N(R C3 )S(=O)2R C3 、-N(R C3 )S(=O)2OR C3 、-N(R C3 )S(=O)2N(R C3 )2、-SC(=O)R C3 、-SC(=O)OR C3 、-SC(=O)SR C3 、-SC(=O)N(R C3 )2、-S(=O)2R C3 、-S(=O)2OR C3 、または-S(=O)2N(R C3 )2であり、R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2; r is 2 or 3.

[0181] In other embodiments, the compound is a compound of formula 3-Vax or formula 3-Vbx: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1, -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1)2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16beach independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2; r is 2 or 3.

[0182] In other embodiments, the compound is a compound of formula 3-VI: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)ORA1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 7a , R 7b , R 11a, R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1, or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(RC3 )2、-SR C3 、-C(=O)R C3 、-C(=O)OR C3 、-C(=O)SR C3 、-C(=O)N(R C3 )2、-OC(=O)R C3 、-OC(=O)OR C3 、-OC(=O)N(R C3 )2、-OC(=O)SR C3 、-OS(=O)2R C3 、-OS(=O)2OR C3 、-OS(=O)2N(R C3 )2、-N(R C3 )C(=O)R C3 、-N(R C3 )C(=NR C3 )R C3 、-N(R C3 )C(=O)OR C3 、-N(R C3 )C(=O)N(R C3 )2、-N(R C3 )C(=NR C3 )N(R C3 )2、-N(R C3 )S(=O)2R C3 、-N(R C3 )S(=O)2OR C3 、-N(R C3 )S(=O)2N(R C3 )2、-SC(=O)R C3 、-SC(=O)OR C3 、-SC(=O)SR C3 、-SC(=O)N(R C3 )2、-S(=O)2R C3 、-S(=O)2OR C3 、または-S(=O)2N(R C3 )2であり、R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2.

[0183] In some embodiments, the compound is a compound of formula 3-VII: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1, -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1, -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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, —ORC3 、-N(R C3 )2、-SR C3 、-C(=O)R C3 、-C(=O)OR C3 、-C(=O)SR C3 、-C(=O)N(R C3 )2、-OC(=O)R C3 、-OC(=O)OR C3 、-OC(=O)N(R C3 )2、-OC(=O)SR C3 、-OS(=O)2R C3 、-OS(=O)2OR C3 、-OS(=O)2N(R C3 )2、-N(R C3 )C(=O)R C3 、-N(R C3 )C(=NR C3 )R C3 、-N(R C3 )C(=O)OR C3 、-N(R C3 )C(=O)N(R C3 )2、-N(R C3 )C(=NR C3 )N(R C3 )2、-N(R C3 )S(=O)2R C3 、-N(R C3 )S(=O)2OR C3 、-N(R C3 )S(=O)2N(R C3 )2、-SC(=O)R C3 、-SC(=O)OR C3 、-SC(=O)SR C3 、-SC(=O)N(R C3 )2、-S(=O)2R C3 、-S(=O)2OR C3 、または-S(=O)2N(R C3 )2であり、R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2; s is 2.

[0184] In some embodiments, the compound is a compound of formula 3-VIII: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)ORA1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a, R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2RA1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3, -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2.

[0185] In other embodiments, the compound is a compound of formula 3-IX: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1)N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SRA1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)RC3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted C3-C6 carbocyclyl or a substituted or unsubstituted aryl; n is 0, 1, or 2; q is 2.

[0186] In some embodiments, the compound is a compound of formula 3-Ia: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1)2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2RA1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3)2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 18 is a substituted or unsubstituted alkyl; R 19 is a substituted or unsubstituted heterocyclyl or a substituted or unsubstituted heteroaryl; n is 0, 1, or 2.

[0187] In some embodiments, the compound is a compound of formula 3-IIaa or formula 3-IIba. [ka]

[0188] In some embodiments, the compound is a compound of formula 3-IIIa: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1)S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SRA1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3ais 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3, -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted heterocyclyl or a substituted or unsubstituted heteroaryl; n is 0, 1, or 2; t is 2 or 3.

[0189] In some embodiments, the compound is a compound of formula 3-IVa: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)RA1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1, -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a and R 15b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NRC3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted heterocyclyl or a substituted or unsubstituted heteroaryl; n is 0, 1, or 2.

[0190] In some embodiments, the compound is a compound of formula 3-Vac or formula 3-Vacc: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6bprovided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1, -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6beach is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(RC3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted heterocyclyl or a substituted or unsubstituted heteroaryl; n is 0, 1, or 2; r is 2 or 3.

[0191] In some embodiments, the compound is a compound of formula 3-VIac: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(RA1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6beach is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(RC3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted heterocyclyl or a substituted or unsubstituted heteroaryl; n is 0, 1, or 2.

[0192] In some embodiments, the compound is a compound of formula 3-VIIac: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1, -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6beach is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(RC3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3 Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted heterocyclyl or a substituted or unsubstituted heteroaryl; n is 0, 1, or 2; s is 2.

[0193] In some embodiments, the compound is a compound of formula 3-VIIIac: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1, -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 15a , R 15b , R 16a and R16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3 , -N(R C3 )2, -SR C3 , -C(=O)R C3 , -C(=O)OR C3 , -C(=O)SR C3 , -C(=O)N(R C3 )2, -OC(=O)R C3 , -OC(=O)OR C3 , -OC(=O)N(R C3 )2, -OC(=O)SR C3 , -OS(=O)2R C3 , -OS(=O)2OR C3 , -OS(=O)2N(R C3 )2, -N(R C3 )C(=O)R C3 , -N(R C3 )C(=NR C3 )R C3 , -N(R C3 )C(=O)OR C3 , -N(R C3 )C(=O)N(R C3 )2, -N(R C3 )C(=NR C3 )N(R C3 )2, -N(R C3 )S(=O)2R C3 , -N(R C3 )S(=O)2OR C3 , -N(R C3 )S(=O)2N(R C3 )2, -SC(=O)R C3 , -SC(=O)OR C3 , -SC(=O)SR C3 , -SC(=O)N(R C3 )2, -S(=O)2R C3 , -S(=O)2OR C3 , or -S(=O)2N(R C3 )2 and R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted heterocyclyl or a substituted or unsubstituted heteroaryl; n is 0, 1, or 2.

[0194] In some embodiments, the compound is a compound of formula 3-IXac: [ka] or a pharmaceutically acceptable salt thereof, During the ceremony, [ka] represents a single bond or a double bond, provided that if a double bond is present, R 6a or R 6b provided that one of R 1 is a substituted or unsubstituted alkyl, a substituted or unsubstituted alkenyl, a substituted or unsubstituted alkynyl, a substituted or unsubstituted carbocyclyl, a substituted or unsubstituted heterocyclyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, -OR A1 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(RA1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2OR A1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 2a , R 2b , R 4a , R 4b , R 7a , R 7b , R11a , R 11b , R 12a , R 12b , or R 17b each independently represents hydrogen, halogen, —CN, —NO, 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 , -N(R A1 )2, -SR A1 , -C(=O)R A1 , -C(=O)OR A1 , -C(=O)SR A1 , -C(=O)N(R A1 )2, -OC(=O)R A1 , -OC(=O)OR A1 , -OC(=O)N(R A1 )2, -OC(=O)SR A1 , -OS(=O)2R A1 , -OS(=O)2OR A1 , -OS(=O)2N(R A1 )2, -N(R A1 )C(=O)R A1 , -N(R A1 )C(=NR A1 )R A1 , -N(R A1 )C(=O)OR A1 , -N(R A1 )C(=O)N(R A1 )2, -N(R A1 )C(=NR A1 )N(R A1 )2, -N(R A1 )S(=O)2R A1 , -N(R A1 )S(=O)2OR A1 , -N(R A1 )S(=O)2N(R A1 )2, -SC(=O)R A1 , -SC(=O)OR A1 , -SC(=O)SR A1 , -SC(=O)N(R A1 )2, -S(=O)2R A1 , -S(=O)2ORA1 , or -S(=O)2N(R A1 )2 and R A1 each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R A1 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 3a is 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; R 5 is hydrogen or methyl, [ka] is a double bond, R 5 does not exist, R 6a and R 6b each is hydrogen, halogen, —CN, —NO, —OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R 6a and R 6b is joined to form an oxo (=O) group, R 15a , R 15b , R 16a and R 16b each independently represents hydrogen, halogen, —CN, —NO, 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 C3、-N(R C3 )2、-SR C3 、-C(=O)R C3 、-C(=O)OR C3 、-C(=O)SR C3 、-C(=O)N(R C3 )2、-OC(=O)R C3 、-OC(=O)OR C3 、-OC(=O)N(R C3 )2、-OC(=O)SR C3 、-OS(=O)2R C3 、-OS(=O)2OR C3 、-OS(=O)2N(R C3 )2、-N(R C3 )C(=O)R C3 、-N(R C3 )C(=NR C3 )R C3 、-N(R C3 )C(=O)OR C3 、-N(R C3 )C(=O)N(R C3 )2、-N(R C3 )C(=NR C3 )N(R C3 )2、-N(R C3 )S(=O)2R C3 、-N(R C3 )S(=O)2OR C3 、-N(R C3 )S(=O)2N(R C3 )2、-SC(=O)R C3 、-SC(=O)OR C3 、-SC(=O)SR C3 、-SC(=O)N(R C3 )2、-S(=O)2R C3 、-S(=O)2OR C3 、または-S(=O)2N(R C3 )2であり、R C3Each instance of is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or a sulfur protecting group if attached to sulfur, or two R C3 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; R 19 is a substituted or unsubstituted heterocyclyl or a substituted or unsubstituted heteroaryl; n is 0, 1, or 2; q is 2.

[0195] In some embodiments, R 19 teeth, [ka] isn't it.

[0196] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-II), Formula (1-III), Formula (1-IV), Formula (1-V-), Formula (1-VI), Formula (1-VII), Formula (1-VIII), Formula (1-IX), Formula (1-X), Formula (1-XI), Formula (1-XII), Formula (1-XIII), or Formula (1-XIV).

[0197] R 2a and R 2b basis In some embodiments, R a and R 2b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)RD1 and R D1 Each instance 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.

[0198] For example, R 2a and R 2b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , or -OC(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0199] In another embodiment, R 2a and R 2b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR D1 and R D1 Each instance of is independently hydrogen or substituted or unsubstituted alkyl.

[0200] In another embodiment, R 2a and R 2b are each independently hydrogen.

[0201] In one embodiment, R 2a and R 2b are both hydrogen.

[0202] R 4a and R 4b basis In some embodiments, R 4a and R 4beach independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0203] In another embodiment, R 4a and R 4b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , or -OC(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0204] In some embodiments, R 4a and R 4b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR D1 and R D1 Each instance of is independently hydrogen or substituted or unsubstituted alkyl.

[0205] In some embodiments, R 4a and R 4b are each independently hydrogen.

[0206] In one embodiment, R 4a and R4b are both hydrogen.

[0207] In embodiments, R 2a and R 2b Each of is independently hydrogen or substituted or unsubstituted alkyl.

[0208] In certain embodiments, R 2a and R 2b each is independently hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 alkoxyhalo, or —OH.

[0209] In some embodiments, R 2a and R 2b is independently —CH 3 , —CH 2 CH 3 , —OH, —OCH 3 , or —CH(CH 3 ) 2 .

[0210] In some embodiments, R 2a and R 2b are both hydrogen.

[0211] In some embodiments, rR 2a and R 2b are each independently hydrogen.

[0212] R 6a and R 6b basis In some embodiments, R 6a and R 6b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1Each instance 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.

[0213] In one embodiment, R 6a and R 6b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , or -OC(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0214] In some embodiments, R 6a and R 6b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR D1 and R D1 Each instance of is independently hydrogen or substituted or unsubstituted alkyl.

[0215] In some embodiments, R 6a and R 6b are each independently hydrogen.

[0216] In one embodiment, R 6a and R 6b are both hydrogen.

[0217] In embodiments, R 6a and R 6b Each of is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.

[0218] In embodiments, R 6a and R 6b are both halogens.

[0219] In some embodiments, R 6a and R 6b are both alkyl.

[0220] In some embodiments, R 6a and R 6b is conjugated to form an oxo group.

[0221] In embodiments, R 6a and R 6b Each of is independently hydrogen or substituted or unsubstituted alkyl.

[0222] In embodiments, R 6a and R 6b Each of is independently hydrogen or substituted alkyl.

[0223] In some embodiments, R 6a and R 6b Each of is independently hydrogen or unsubstituted alkyl.

[0224] In certain embodiments, R 6a is halogen or alkyl, and R 6b is hydrogen.

[0225] In certain embodiments, R 6a and R 6b are both hydrogen.

[0226] In some embodiments, R 6a and R 6b Each of is independently hydrogen.

[0227] R 7a and R 7b basis In some embodiments, R 7a and R7b are each independently 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0228] In another embodiment, R 7a and R 7b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH2, or -N(R D1 )2 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0229] In embodiments, R 7a and R 7b each independently represents hydrogen, substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0230] In embodiments, R 7a and R 7b each is independently hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 alkoxyhalo, or —OH.

[0231] In some embodiments, R 7a and R 7b is independently —CH 3 , —CH 2 CH 3 , —OH, —OCH 3 , or —CH(CH 3 ) 2 .

[0232] In some embodiments, R 7a and R 7b Each of is independently hydrogen or substituted or unsubstituted alkyl.

[0233] In embodiments, R 7a or R 7b are both hydrogen.

[0234] R 11a and R 11b basis In some embodiments, R 11a and R 11b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0235] In some embodiments, R 11a and R 11b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , or -OC(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0236] In some embodiments, R 11a and R 11b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR D1 and R D1 Each instance of is independently hydrogen or substituted or unsubstituted alkyl.

[0237] In some embodiments, R 11a and R 11b are each independently hydrogen.

[0238] In one embodiment, R 11a and R 11b are both hydrogen.

[0239] R 12a and R 12b basis In some embodiments, R 12a and R 12b are each independently 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1Each instance 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.

[0240] In some embodiments, R 12a and R 12b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH2, or -N(R D1 )2 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0241] In embodiments, R 12a and R 12b each independently represents hydrogen, substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0242] In embodiments, R 12a and R 12b Each of is independently hydrogen or substituted or unsubstituted alkyl.

[0243] In certain embodiments, R 12a and R 12b are both hydrogen.

[0244] In certain embodiments, R 12a and R 12b are independently hydrogen.

[0245] R 15a and R 15b basis In some embodiments, R 15a and R 15b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0246] In some embodiments, R 15a and R 15b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH2, or -N(R D1 )2 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0247] In certain embodiments, R 15a and R 15b each independently represents hydrogen, substituted or unsubstituted alkyl, -OR D1, -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0248] In certain embodiments, R 15a and R 15b Each of is independently hydrogen or substituted or unsubstituted alkyl.

[0249] In embodiments, R 15a and R 15b are both hydrogen.

[0250] In embodiments, R 15a and R 15b are each independently hydrogen.

[0251] R 16a and R 16b basis In some embodiments, R 16a and R 16b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkynyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0252] In some embodiments, R 16a and R 16b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , or -OC(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0253] R 16a and R 16b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR D1 and R D1 Each instance of is independently hydrogen or substituted or unsubstituted alkyl.

[0254] In one embodiment, R 16a and R 16b are each independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR D1 and R D1 Each instance of is independently hydrogen or substituted or unsubstituted alkyl.

[0255] In some embodiments, R 16a and R 16b are each independently hydrogen.

[0256] In one embodiment, R 16a and R 16b are both hydrogen.

[0257] R 37a and R 37b basis In some embodiments, R 37a and R 37bEach of is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.

[0258] In some embodiments, R 37a and R 37b Each of is independently hydrogen.

[0259] In some embodiments, R 37a and R 37b Each of is hydrogen.

[0260] R 36a and R 36b basis In some embodiments, R 36a and R 36b Each of is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.

[0261] R 35a and R 35b basis In some embodiments, R 35a and R 35b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0262] R 34a and R34b basis In some embodiments, R 34a and R 34b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0263] R 33a and R 33b basis In some embodiments, R 33a and R 33b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0264] R 32a and R 32b basis In certain embodiments, R 32aand R 32b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0265] R 31a and R 31b basis In embodiments, R 31a and R 31b each independently represents 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 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 and R A1 Each instance 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.

[0266] R 30a and R 30b basis In some embodiments, R 30a and R 30b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH2, or -N(R D1 )2 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0267] R 29a and R 29b basis In certain embodiments, R 29a and R 29b are 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 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 and R A1 Each instance 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.

[0268] R 5 basis In some embodiments, R 5 is a hydrogen atom in the cis position.

[0269] In another embodiment, R 5 is a hydrogen in the trans position.

[0270] In yet another embodiment, R 5 is a methyl in the cis position.

[0271] In one embodiment, R 5 is a methyl in the trans position.

[0272] R 1a and R 1b basis In certain embodiments, R 1a and R 1b 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 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance 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.

[0273] In certain embodiments, R 1a and R 1b each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH2, or -N(R D1 )2 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0274] In embodiments, R 1a and R 1b each independently represents hydrogen, substituted or unsubstituted alkyl, -OR D1 , -OC(=O)R D1 , -NH2, -N(R D1 )2, or -NR D1 C(=O)R D1 and R D1 Each instance of is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0275] In embodiments, R 1a and R 1b Each of is independently hydrogen or substituted or unsubstituted alkyl.

[0276] In some embodiments, R 1a and R 1b each is independently hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 alkoxyhalo, or —OH.

[0277] In some embodiments, R 1a and R 1b is independently —CH 3 , —CH 2 CH 3 , —OH, —OCH 3 , or —CH(CH 3 ) 2 .

[0278] In embodiments, R 1a and R 1b are both hydrogen.

[0279] In embodiments, R 1a and R 1b are each independently hydrogen.

[0280] Integers n, q, r, s, t, and u In some embodiments, n is 1 or 2. In some embodiments, n is 1. In other embodiments, n is 2.

[0281] In some embodiments, u is 1 or 2. In some embodiments, u is 1. In other embodiments, u is 2.

[0282] In some embodiments, q is 0, 1, 2, or 3. In some examples, q is 0, 2, or 3. In some embodiments, q is 0 or 2, and in some embodiments, q is 2 or 3. In some embodiments, q is 1, 2, or 3. In some embodiments, q is 0, 1, or 2. In some embodiments, q is 0. In some embodiments, q is 1. In some embodiments, q is 2. In some embodiments, q is 3.

[0283] In some embodiments, r is 0, 1, or 2. In some examples, r is 0 or 2. In some embodiments, r is 1 or 2. In some embodiments, r is 0 or 1. In some embodiments, r is 0. In some embodiments, r is 1. In some embodiments, r is 2.

[0284] In some embodiments, s is 0, 1, or 2. In some examples, s is 0 or 2. In some embodiments, s is 1 or 2. In some embodiments, s is 0 or 1. In some embodiments, s is 0. In some embodiments, s is 1. In some embodiments, s is 2.

[0285] In some embodiments, t is 0, 1, 2, or 3. In some examples, t is 0, 2, or 3. In some embodiments, t is 0 or 2, and in some embodiments, t is 2 or 3. In some embodiments, t is 1, 2, or 3. In some embodiments, t is 0, 1, or 2. In some embodiments, t is 0. In some embodiments, t is 1. In some embodiments, t is 2. In some embodiments, t is 3.

[0286] In some embodiments, r is 1 and s is 1.

[0287] In some embodiments, q is 0, 2, or 3, and t is 0, 2, or 3. In other embodiments, q is 2, t is 2, and u is 1.

[0288] In some embodiments, q is 0, 2, or 3, and u is 1. In other embodiments, q is 0, 2, or 3, t is 0, 2, or 3, and u is 1.

[0289] In another embodiment, q is 1, t is 0, 2, or 3, and u is 2.

[0290] In some embodiments, q, u, r, s, and t are not all 1 at the same time. In some embodiments, when t is 0, 2, or 3, q, u, s, and r are not all 1 at the same time. In some embodiments, when q is 0 or 2 and u is 1, t, s, and r are not all 1 at the same time. In some embodiments, when u is 2 and q is 1, t, s, and r are not all 1 at the same time. In some embodiments, when r is 0 or 2, q, u, s, and t are not all 1 at the same time. In some embodiments, when s is 0 or 2, q, u, r, and t are not all 1 at the same time.

[0291] R 3 basis In some embodiments, R 3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0292] In some embodiments, R 3 is substituted or unsubstituted alkyl. In some embodiments, alkyl is optionally substituted with halo or OR D1 is replaced by .

[0293] In certain embodiments, R 3 is a substituted or unsubstituted alkyl.

[0294] In some embodiments, R 3 is a substituted alkyl.

[0295] In some embodiments, R 3 is an unsubstituted alkyl.

[0296] In some embodiments, R 3 is methyl.

[0297] In some embodiments, R 3 is -OCH3.

[0298] In some embodiments, R 3 is -CH2OCH3 or -CH2OCH2CH3.

[0299] R 3a basis In some embodiments, R 3a is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0300] In some embodiments, R 3a is substituted or unsubstituted alkyl. In some embodiments, alkyl is optionally substituted with halo or OR D1 is replaced by .

[0301] In certain embodiments, R 3a is a substituted or unsubstituted alkyl.

[0302] In some embodiments, R 3a is a substituted alkyl.

[0303] In some embodiments, R 3a is an unsubstituted alkyl.

[0304] In some embodiments, R 3a is methyl.

[0305] In some embodiments, R 3a is -OCH3.

[0306] In some embodiments, R 3a is -CH2OCH3 or -CH2OCH2CH3.

[0307] R D1 basis In one embodiment, R D1 is hydrogen, or substituted or unsubstituted alkyl.

[0308] R 19 basis In some embodiments, R 19 is a substituted alkyl.

[0309] In some embodiments, R 19 is an unsubstituted alkyl.

[0310] In another embodiment, R 19 is methyl or hydrogen.19 is methyl, ethyl, or hydrogen.

[0311] In some embodiments, R 19 is hydrogen.

[0312] In some embodiments, R 19 is methyl.

[0313] In some embodiments, R 19 is a substituted alkyl.

[0314] In some embodiments, R 19 is an unsubstituted alkyl.

[0315] In certain embodiments, R 19 is methyl.

[0316] In embodiments, R 19 is -CH2OCH3.

[0317] In embodiments, R 19 is -OCH3.

[0318] In certain embodiments, R 19 is ethyl.

[0319] In embodiments, R 19 is hydrogen.

[0320] X group In some embodiments, X is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heteroaryl.

[0321] In some embodiments, X is hydrogen, substituted or unsubstituted heteroaryl, or substituted or unsubstituted alkyl.

[0322] In another embodiment, X is substituted or unsubstituted heteroaryl.

[0323] In one embodiment, X is a substituted or unsubstituted 5-10 membered heteroaryl.

[0324] In one embodiment, X is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or -OR A1 and R A1 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0325] In some embodiments, X is hydrogen or substituted or unsubstituted heteroaryl.

[0326] For example, in some instances, X is a substituted or unsubstituted N-linked heteroaryl.

[0327] In one embodiment, the N-linked heteroaryl is a 5-6 membered N-linked heteroaryl.

[0328] In some embodiments, X is [ka] and R 20 Each example of is independently a halogen, -NO2, -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)2R GA , -S(=O)2OR GA , -OS(=O)2R GA , -S(=O)2N(R GA )2, or -N(R GA )S(=O)2R GA ;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 3~4 carbosilyl, or a substituted or unsubstituted 3- to 4-membered heterosilyl; R GA Each instance 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 carbosilyl, substituted or unsubstituted 3- to 6-membered heterosilyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, or two R GA the groups, together with the intervening atoms, form a substituted or unsubstituted carbocyclic ring or a substituted or unsubstituted heterocyclic ring; e is 0, 1, 2, 3, 4, or 5.

[0329] In some embodiments, X is [ka] and R 20 Each example of is independently a halogen, -NO2, -CN, -OR GA , -N(R GA )2, -C(=O)R GA , -C(=O)OR GA , -C(=O)N(R GA )2, -N(RGA )C(=O)R GA , -OC(=O)N(R GA )2, substituted or unsubstituted C 1~6 alkyl, substituted or unsubstituted 3- to 4-membered carbosilyl, substituted or unsubstituted 3- to 4-membered heterocyclyl; R GA Each instance of is independently hydrogen, substituted or unsubstituted C 1~6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or two R GA the groups, together with the intervening atoms, form a substituted or unsubstituted carbocyclic or heterocyclic ring; e is 0, 1, 2, or 3.

[0330] In some embodiments, X is [ka] and R 20 Each example of is independently a halogen, -NO2, -CN, -OR GA , -N(R GA )2, -C(=O)R GA , -C(=O)OR GA , -C(=O)N(R GA )2, -N(R GA )C(=O)R GA , -OC(=O)N(R GA )2, substituted or unsubstituted C 1~6 alkyl, substituted or unsubstituted 3- to 4-membered carbosilyl, substituted or unsubstituted 3- to 4-membered heterocyclyl; R GA Each instance of is independently hydrogen, substituted or unsubstituted C 1~6 alkyl, 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; e is 0, 1, 2, or 3.

[0331] R 28 basis In some embodiments, R 28 is 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.

[0332] In some embodiments, R 28 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroaryl.

[0333] In some embodiments, R 28 is hydrogen.

[0334] In some embodiments, R 28 is methyl.

[0335] In some embodiments, R 28 teeth, [ka] is selected from the group consisting of During the ceremony, R a Each example of is independently hydrogen, halogen, -NO2, -CN, -OR D4 , -N(R D4 )2, -C(=O)R D4 , -C(=O)OR D4 , -C(=O)N(R D4 )2, -OC(=O)R D4 , -OC(=O)OR D4 , -N(R D4 )C(=O)R D4 , -OC(=O)N(R D4 )2, -N(R D4 )C(=O)OR D4 , -S(=O)2R D4 , -S(=O)2OR D4 , -OS(=O)2R D4 , -S(=O)2N(R D4)2, or -N(R D4 )S(=O)2R D4 , 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 Carbosilyl, substituted or unsubstituted 3- to 6-membered heterosilyl, substituted or unsubstituted C 5~10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl; R D4 Each instance 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 Carbosilyl, substituted or unsubstituted 3- to 6-membered heterosilyl, substituted or unsubstituted C 5~10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, an oxygen protecting group if attached to oxygen, a nitrogen protecting group if attached to nitrogen, or two R D4 the groups, together with the intervening atoms, form a substituted or unsubstituted heterocyclic ring; p is an integer selected from 0 to 11.

[0336] In some embodiments, R 28 teeth, [ka] is selected from the group consisting of In the formula, R a and p is as defined herein.

[0337] In certain embodiments, R 28 teeth, [ka] and In the formula, R a and p is as defined herein.

[0338] In certain embodiments, R 28 teeth, [ka] is.

[0339] R 20 basis In some embodiments, R 20 is -CN.

[0340] In some embodiments, R 20 is an unsubstituted alkyl.

[0341] In another embodiment, R 20 is the unsubstituted C 1~6 It is alkyl.

[0342] In one embodiment, R 20 is methyl.

[0343] R 55 basis In some embodiments, R 55 is hydrogen, halogen, cyano, or substituted or unsubstituted alkyl.

[0344] In some embodiments, R 55 is cyano. In another embodiment, R 55 is methyl. In one embodiment, R 55 is hydrogen. 55 is a halogen.

[0345] R 18 basis In some embodiments, R 18 is an unsubstituted alkyl.

[0346] In another embodiment, R 18 is a substituted alkyl.

[0347] In one embodiment, R 18 is a substituted or unsubstituted C 1~4 It is alkyl.

[0348] In some embodiments, R 18 is the unsubstituted C 1~4 It is alkyl.

[0349] In some embodiments, R 18 is methyl.

[0350] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-II-a), Formula (1-II-b), Formula (1-II-c), or Formula (1-II-d): [ka] or a pharmaceutically acceptable salt thereof.

[0351] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-III-a), Formula (1-III-b), Formula (1-III-c), or Formula (1-III-d): [ka] or a pharmaceutically acceptable salt thereof.

[0352] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IV-a), Formula (1-IV-b), Formula (1-IV-c), or Formula (1-IV-d): [ka] or a pharmaceutically acceptable salt thereof.

[0353] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VI-a): [ka] or a pharmaceutically acceptable salt thereof.

[0354] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VI-b): [ka] or a pharmaceutically acceptable salt thereof.

[0355] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VII-a): [ka] or a pharmaceutically acceptable salt thereof.

[0356] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VII-b): [ka] or a pharmaceutically acceptable salt thereof.

[0357] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-VIII-a) or Formula (1-VIII-b): [ka] or a pharmaceutically acceptable salt thereof.

[0358] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-IX-a), Formula (1-IX-b), Formula (1-IX-c), or Formula (1-IX-d): [ka] or a pharmaceutically acceptable salt thereof.

[0359] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-Xa), Formula (1-Xb), Formula (1-Xc), or Formula (1-Xd): [ka] or a pharmaceutically acceptable salt thereof.

[0360] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XI-a), Formula (1-XI-b), Formula (1-XI-c), or Formula (1-XI-d): [ka] or a pharmaceutically acceptable salt thereof.

[0361] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XII-a) or Formula (1-XII-b): [ka] or a pharmaceutically acceptable salt thereof.

[0362] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XIII-a) or Formula (1-XIII-b): [ka] or a pharmaceutically acceptable salt thereof, R 55 is hydrogen, halogen, cyano, or substituted or unsubstituted alkyl.

[0363] In some embodiments, the compound of Formula (1-I) is a compound of Formula (1-XIV-a): [ka] or a pharmaceutically acceptable salt thereof, R 55 is hydrogen, halogen, cyano, or substituted or unsubstituted alkyl.

[0364] In some embodiments, the compound of formula 2-I is a compound of formula 2-Ic: [ka] or a pharmaceutically acceptable salt thereof.

[0365] In some embodiments, the compound has formula 2-Id: [ka] or a pharmaceutically acceptable salt thereof.

[0366] In some embodiments, the compound of formula 2-I is a compound of formula 2-Ie: [ka] or a pharmaceutically acceptable salt thereof.

[0367] In some embodiments, the compound of formula 2-I may be a compound of formula 2-If: [ka] or a pharmaceutically acceptable salt thereof.

[0368] In certain embodiments, the compound of Formula 2-I is a compound of Formula 2-Ig, Formula 2-Ig-II, or Formula 2-Ih: [ka] or a pharmaceutically acceptable salt thereof.

[0369] In some embodiments, the compound of formula 2-I is a compound of formula 2-Iga or formula 2-Iha: [ka] or a pharmaceutically acceptable salt thereof.

[0370] In some embodiments, the compound of formula 2-I is a compound of formula 2-Igb or formula 2-Ihb: [ka] or a pharmaceutically acceptable salt thereof.

[0371] In some embodiments, the compound of formula 2-I is a compound of formula 2-Igc: [ka] or a pharmaceutically acceptable salt thereof.

[0372] In some embodiments, the compound of formula 2-I is a compound of formula 2-Igd: [ka] or a pharmaceutically acceptable salt thereof.

[0373] It is understood that the stereochemistry at C17 can be either of the following but can be depicted in an equivalent manner: [ka]

[0374] In some embodiments, the compound of formula 3-III is a compound of formula 3-III-ad: [ka] or a pharmaceutically acceptable salt thereof.

[0375] In some embodiments, the compound of formula 3-III is a compound of formula 3-III-bd: [ka] or a pharmaceutically acceptable salt thereof. In some embodiments, R 55 is hydrogen, halogen, cyano, or substituted or unsubstituted alkyl. In some embodiments, R 55 is hydrogen. In some embodiments, R55 is halogen. In some embodiments, R 55 is cyano. In some embodiments, R 55 is unsubstituted alkyl. In some embodiments, R 55 is a substituted alkyl.

[0376] In some embodiments, the pharmaceutical composition comprises a compound described herein or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

[0377] In some embodiments, a method for treating a CNS-related disorder in a subject in need thereof comprises administering to the subject an effective amount of a compound described herein or a pharmaceutically acceptable salt thereof. In some embodiments, the CNS-related disorder is a sleep disorder, a mood disorder, a schizophrenia spectrum disorder, a seizure disorder, a memory and / or cognition disorder, 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. In some embodiments, the CNS-related disorder is depression. In some embodiments, the CNS-related disorder is postpartum depression. In some embodiments, the CNS-related disorder is major depressive disorder. In some embodiments, the major depressive disorder is moderate major depressive disorder. In some embodiments, the major depressive disorder is severe major depressive disorder.

[0378] In some embodiments, the compound is selected from the group consisting of the compounds identified in Table 1 below. [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 1-15]

[0379] In some embodiments, the compound is selected from the group consisting of the compounds identified in Table 2 below. [Table 2-1] [Table 2-2] [Table 2-3] [Table 2-4] [Table 2-5]

[0380] In some embodiments, the compound is selected from the group consisting of the compounds identified in Table 3 below. [Table 3-1] [Table 3-2] [Table 3-3]

[0381] In one aspect, provided herein are pharmaceutically acceptable salts of the compounds described herein (e.g., compounds of formula (1-I), (2-I), or (3-I)).

[0382] In one aspect, provided herein is a pharmaceutical composition comprising a compound described herein (e.g., a compound of Formula (1-I), (2-I), or (3-I)) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. In certain embodiments, the compound of the invention is provided in the pharmaceutical composition in an effective amount. In certain embodiments, the compound of the invention is provided in a therapeutically effective amount.

[0383] The compounds of the invention described herein may, in certain embodiments, A It acts as a regulator, e.g., GABA A GABA receptors act in either a positive or negative manner as a regulator of central nervous system (CNS) excitability. A Such compounds are expected to have CNS activity, as mediated by their ability to modulate receptors.

[0384] Therefore, in another aspect, a method for treating a CNS-related disorder in a subject in need thereof is provided, comprising administering to the subject an effective amount of a compound of the present invention. In certain embodiments, the CNS-related disorder is a sleep disorder, a mood disorder, a schizophrenia spectrum disorder, a seizure disorder, a memory and / or cognitive disorder, 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. In certain embodiments, the CNS-related disorder is depression. In certain embodiments, the CNS-related disorder is postpartum depression. In certain embodiments, the CNS-related disorder is major depressive disorder. In certain embodiments, the major depressive disorder is moderate major depressive disorder. In certain embodiments, the major depressive disorder is severe major depressive disorder. In certain embodiments, the compound is administered orally, subcutaneously, intravenously, or intramuscularly. In certain embodiments, the compound is administered orally. In certain embodiments, the compound is administered chronically. In certain embodiments, the compound is administered continuously, for example, by continuous intravenous infusion.

[0385] Exemplary compounds of the present invention can be synthesized from the following known starting materials using methods known to those skilled in the art or certain references: In one aspect, provided herein are pharmaceutically acceptable salts of the compounds described herein (e.g., compounds of formula (1-I), (2-I), or (3-I)).

[0386] Alternative Embodiments In alternative embodiments, the compounds described herein may also contain one or more isotopic substitutions. For example, hydrogen may be replaced by 2 H (D or deuterium) or 3 H (T or tritium), and carbon can be, for example, 13 C or 14 C, and oxygen may be, for example, 18 O, and the nitrogen may be, for example, 15In other embodiments, specific isotopes (e.g., 3 H, 13 C. 14 C. 18 O, or 15 N) can represent at least 1%, at least 5%, at least 10%, at least 15%, at least 20%, at least 25%, at least 30%, at least 35%, at least 40%, at least 45%, at least 50%, at least 60%, at least 65%, at least 70%, at least 75%, at least 80%, at least 85%, at least 90%, at least 95%, at least 99%, or at least 99.9% of the total isotopic abundance of the element occupying a particular site in the compound.

[0387] Pharmaceutical Compositions In one aspect, provided herein is a pharmaceutical composition comprising a compound described herein (e.g., a compound of Formula (1-I), (2-I), or (3-I)) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. In certain embodiments, the compound of the invention is provided in the pharmaceutical composition in an effective amount. In certain embodiments, the compound of the invention is provided in a therapeutically effective amount.

[0388] In certain embodiments, the pharmaceutical composition comprises an effective amount of the active ingredient. In certain embodiments, the pharmaceutical composition comprises a therapeutically effective amount of the active ingredient.

[0389] The pharmaceutical compositions provided herein can be administered by a variety of routes, including, but not limited to, oral (enteral), parenteral (by injection), rectal, transdermal, intradermal, intrathecal, subcutaneous (SC), intravenous (IV), intramuscular (IM), and intranasal administration.

[0390] Generally, the compounds provided herein are administered in an effective amount. The amount of compound actually administered is typically determined by a physician taking into account the relevant circumstances, including the condition being treated, the selected route of administration, the compound actually administered, the age, weight, and response of the individual patient, the severity of the patient's symptoms, etc.

[0391] When used to prevent the onset of CNS disorders, the compounds provided herein are typically administered at the dosage levels described above to subjects at risk of developing the condition under the advice and supervision of a physician. Subjects at risk of developing a particular condition generally include subjects with a family history of the condition, or subjects identified by genetic testing or screening as being particularly susceptible to developing the condition.

[0392] The pharmaceutical compositions provided herein can also be administered chronically ("chronic administration"). Chronic administration refers to administering a compound or a pharmaceutical composition thereof for an extended period of time, such as 3 months, 6 months, 1 year, 2 years, 3 years, 5 years, or can continue indefinitely, for example, for the life of the subject. In certain embodiments, chronic administration is intended to provide a constant level of the compound in the blood, for example, within the therapeutic window, for an extended period of time.

[0393] The pharmaceutical composition of the present invention can be further delivered using various administration methods.For example, in certain embodiments, the pharmaceutical composition can be given as a bolus, for example, to raise the concentration of the compound in the blood to an effective level.The placement of the bolus dose depends on the systemic level of the active ingredient desired throughout the body; for example, an intramuscular or subcutaneous bolus dose allows for a slow release of the active ingredient, while a bolus delivered directly into a vein (e.g., through infusion) allows for a much faster delivery, which quickly raises the concentration of the active ingredient in the blood to an effective level.In other embodiments, the pharmaceutical composition can be administered as a continuous infusion, for example, by infusion, to provide maintenance of the steady-state concentration of the active ingredient in the subject's body.In addition, in still other embodiments, the pharmaceutical composition can be initially administered as a bolus dose, followed by continuous infusion.

[0394] Compositions for oral administration can take the form of bulk liquid solutions or suspensions, or bulk powders. However, more commonly, compositions are presented in unit dosage forms to facilitate accurate dosing. The term "unit dosage form" refers to physically discrete units suitable as single dosages for human subjects and other mammals, each containing a predetermined amount of active agent calculated to produce a desired therapeutic effect in association with a suitable pharmaceutical excipient. Typical unit dosage forms include pre-filled, pre-measured ampoules or syringes of liquid compositions or pills, tablets, capsules, etc., in the case of solid compositions. In such compositions, the compound is typically a minor component (about 0.1 to about 50% by weight, preferably about 1 to about 40% by weight), with the remainder being various vehicles or excipients and processing aids that serve to form the desired dosage form.

[0395] A typical oral administration regimen is 1 to 5 times, particularly 2 to 4 times, typically 3 times per day. Using these administration patterns, each dose provides about 0.01 to about 20 mg / kg of the compound provided by the present invention, with preferred doses being about 0.1 to about 10 mg / kg, particularly about 1 to about 5 mg / kg.

[0396] The transdermal dose is generally selected to provide similar or lower blood levels than those achieved using an injection dose, and is generally an amount ranging from about 0.01 to about 20% by weight, preferably from about 0.1 to about 20% by weight, preferably from about 0.1 to about 10% by weight, and more preferably from about 0.5 to about 15% by weight.

[0397] Injection dose levels range from about 0.1 mg / kg / hour to at least 20 mg / kg / hour, all for about 1 to about 120 hours, particularly 24 to 96 hours. Preloading boluses of about 0.1 mg / kg to about 10 mg / kg or more may also be administered to achieve adequate steady-state levels. The maximum total dose is not expected to exceed about 5 g / day for a 40-80 kg human patient.

[0398] Liquid forms suitable for oral administration may include a suitable aqueous or nonaqueous vehicle with buffers, suspending and dispensing agents, colorants, flavors, etc. Solid forms may include, for example, any of the following ingredients, or compounds of a similar nature: a binder such as microcrystalline cellulose, gum tragacanth, or gelatin; an excipient such as starch or lactose; a disintegrating agent such as alginic acid, Primogel, or corn starch; a lubricant such as magnesium stearate; a glidant such as colloidal silicon dioxide; a sweetening agent such as sucrose or saccharin; or a flavoring agent such as peppermint, methyl salicylate, or orange flavoring.

[0399] Injectable compositions are typically based on injectable sterile saline or phosphate-buffered saline, or other injectable vehicles known in the art. As noted above, the active compound in such compositions is typically about 0.05-10% by weight, with the remainder being injectable excipients and the like.

[0400] Transdermal compositions are typically formulated as topical ointments or creams containing active ingredient(s). When formulated as an ointment, the active ingredient is typically combined with either a paraffinic or water-miscible ointment base. Alternatively, the active ingredient may be formulated in a cream, for example, with an oil-in-water cream base. Such transdermal formulations are well known in the art and generally contain additional ingredients to enhance the skin penetration of the active ingredient or the stability of the formulation. All such known transdermal formulations and ingredients are included within the scope provided herein.

[0401] The compounds provided herein can also be administered by a transdermal device. Accordingly, transdermal administration can be accomplished using a patch either of the reservoir or porous membrane type, or of a solid matrix variety.

[0402] The above-described components of the orally administrable, injectable, or topically administrable compositions are merely representative. Other materials, as well as processing techniques, etc., are described in Part 8 of Remington's Pharmaceutical Sciences, 17th edition, 1985, Mack Publishing Company, Easton, Pennsylvania, which is incorporated herein by reference.

[0403] The compounds of this invention can also be administered in sustained release forms or from sustained release drug delivery systems. A description of representative sustained release materials can be found in Remington's Pharmaceutical Sciences.

[0404] The present invention also relates to pharmaceutically acceptable acid addition salts of the compounds of the present invention. Acids that can be used to prepare pharmaceutically acceptable salts are those that form non-toxic acid addition salts, i.e., salts containing pharmacologically acceptable anions, such as hydrochloride, hydroiodide, hydrobromide, nitrate, sulfate, bisulfate, phosphate, acetate, lactate, citrate, tartrate, succinate, maleate, fumarate, benzoate, paratoluenesulfonate, etc.

[0405] In another aspect, the present invention provides pharmaceutical compositions comprising a compound of the present invention and a pharmaceutically acceptable excipient, eg, a composition suitable for injection, such as intravenous (IV) administration.

[0406] Pharmaceutically acceptable excipients include any diluents or other liquid vehicles, dispersing or suspending aids, surfactants, isotonicity agents, preservatives, lubricants, etc., that are suitable for the particular dosage form desired, e.g., injection. General considerations in the formulation and / or manufacture of pharmaceutical compositions can be found, for example, in Remington's Pharmaceutical Sciences, Sixteenth Edition, E.W. Martin (Mack Publishing Co., Easton, Pa., 1980), and Remington: The Science and Practice of Pharmacy, 21 st Edition (Lippincott Williams & Wilkins, 2005).

[0407] For example, injectable preparations, such as sterile injectable aqueous suspensions, can be formulated according to known techniques using suitable dispersing or wetting agents and suspending agents. Exemplary excipients that can be used include, but are not limited to, water, sterile saline or phosphate-buffered saline, or Ringer's solution.

[0408] In certain embodiments, the pharmaceutical composition further comprises a cyclodextrin derivative. The most common cyclodextrins are α-, β-, and γ-cyclodextrins, consisting of 6, 7, and 8 α-1,4-linked glucose units, respectively, optionally containing one or more substituents on the linked sugar moieties, including, but not limited to, substituted or unsubstituted methylation, hydroxyalkylation, acylation, and sulfoalkyl ether substitution. In certain embodiments, the cyclodextrin is a sulfoalkyl ether β-cyclodextrin, such as sulfobutyl ether β-cyclodextrin, also known as CAPTISOL®. See, e.g., U.S. Patent No. 5,376,645. In certain embodiments, the composition comprises hexapropyl-β-cyclodextrin. In more specific embodiments, the composition comprises hexapropyl-β-cyclodextrin (10-50% in water).

[0409] Injectable compositions can be sterilized, for example, by filtration through a bacterial-retaining filter, or by incorporating sterilizing agents in the form of sterile solid compositions which can be dissolved or dispersed in sterile water or other sterile injectable medium before use.

[0410] Generally, the compounds provided herein are administered in an effective amount. The amount of the compound actually administered is typically determined by a physician taking into account relevant circumstances, including the condition to be treated, the selected route of administration, the compound actually administered, the age, weight, response, and severity of the patient's symptoms of the individual patient.

[0411] The compositions are presented in unit dosage forms to facilitate accurate administration. The term "unit dosage form" refers to physically discrete units suitable as single dosages for human subjects and other mammals, each unit containing a predetermined amount of active agent calculated to produce a desired therapeutic effect in association with a suitable pharmaceutical excipient. Typical unit dosage forms include prefilled, premeasured ampoules or syringes of liquid compositions. In such compositions, the compound is usually a minor component (about 0.1 to about 50% by weight, preferably about 1 to about 40% by weight), with the remainder being various vehicles or excipients and processing aids that serve to form the desired dosage form.

[0412] The compounds provided herein can be administered as the sole active agent or in combination with other active agents. In one aspect, the present invention provides a combination of a compound of the present invention with another pharmacologically active agent. Co-administration can proceed by any technique apparent to those skilled in the art, including, for example, separate, sequential, simultaneous, and alternating administration.

[0413] Although the description of pharmaceutical compositions provided herein is primarily directed to pharmaceutical compositions suitable for administration to humans, it will be understood by those skilled in the art that such compositions are generally suitable for administration to animals of all kinds. Modifications of pharmaceutical compositions suitable for administration to humans to make compositions suitable for administration to a variety of animals are well understood, and those skilled in the art can design and / or perform such modifications with routine experimentation. General considerations in the formulation and / or manufacture of pharmaceutical compositions can be found, for example, in Remington: The Science and Practice of Pharmacy, 21 st ed., Lippincott Williams & Wilkins, 2005.

[0414] In one embodiment, a kit is provided that includes a composition (e.g., a solid composition) that includes a compound of formula (1-I), (2-I), or (3-I).

[0415] Combination therapy The compounds or compositions described herein (e.g., a compound of Formula (I-1), (I-2), (I-3), or (I-4), or a pharmaceutical salt thereof, or a composition comprising a compound of Formula (I-1), (I-2), (I-3), or (I-4), or a pharmaceutically acceptable salt thereof) can be administered in combination with an additional agent or therapy. The subject to whom the compounds disclosed herein are administered can have a disease, disorder, or condition, or a symptom thereof, that would benefit from treatment with another agent or therapy. Combination therapy can be achieved by administering two or more agents, each of which can be formulated and administered separately, or by administering two or more agents in a single formulation. In some embodiments, two or more agents in the combination therapy can be administered simultaneously. In other embodiments, two or more agents in the combination therapy are administered separately. For example, administration of a first agent (or combination of agents) can occur minutes, hours, days, or weeks before administration of a second agent (or combination of agents). Thus, two or more drugs can be administered within minutes of each other, or within 1, 2, 3, 6, 9, 12, 15, 18 or 24 hours of each other, or within 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 14 days of each other, or within 2, 3, 4, 5, 6, 7, 8, 9 or weeks of each other.In some cases, even longer intervals are possible.Although it is often desirable that two or more drugs used in combination therapy are present in patient's body at the same time, this does not have to be the case.

[0416] Combination therapy can also inc...

Claims

1. A compound of formula (1-V-a), (1-V-b), (1-VIIa), or (1-VII-b): 【Chemistry 416】 or a pharmaceutically acceptable salt thereof, During the ceremony, 【Chemical 390】 represents a single bond or a double bond, provided that when a double bond is present, R ５ and R ６ａ Or R ６ｂ One of them does not exist, n is independently 1 or 2; X 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 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 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 and R Ａ１ each instance 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 heteroaryl, an oxygen protecting group when attached to an oxygen atom, a sulfur protecting group when attached to a sulfur atom, or a nitrogen protecting group when attached to a nitrogen atom; Ａ２ each instance of 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, or substituted or unsubstituted heteroaryl; R ５ is hydrogen or methyl, R １９ is hydrogen, or substituted or unsubstituted alkyl; R １８ is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R ３ is substituted or unsubstituted alkyl; R ６ａ and R ６ｂ each is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, or R ６ａ and R ６ｂ is joined to form an oxo (=O) group, R ２ａ , R ２ｂ , R ４ａ , R ４ｂ , R １１ａ , R １１ｂ , R １６ａ , or R １６ｂ each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkynyl, -OR Ｄ１ , -OC(=O)R Ｄ１ , -NH ２ , -N(R Ｄ１ ) ２ , or -NR Ｄ１ C(=O)R Ｄ１ and R Ｄ１ each instance 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 heteroaryl, an oxygen protecting group if attached to an oxygen atom, a nitrogen protecting group if attached to a nitrogen atom, or two R Ｄ１ groups are joined to form a substituted or unsubstituted heterocyclic ring, or R ２ａ and R ２ｂ , or R ４ａ and R ４ｂ , or R １１ａ and R １１ｂ , or R １６ａ and R １６ｂ is joined to form an oxo (=O) group, or a pharmaceutically acceptable salt thereof.

2. The compound of formula (1-V-a), (1-V-b), (1-VIIa), or (1-VII-b) is a compound of formula (1-V-a): 【Chemistry 417】 2. The compound of claim 1, which is: or a pharmaceutically acceptable salt thereof.

3. The compound of formula (1-V-a), (1-V-b), (1-VIIa), or (1-VII-b) is a compound of formula (1-V-b): 【Chemistry 418】 2. The compound of claim 1, which is: or a pharmaceutically acceptable salt thereof.

4. The compound of formula (1-V-a), (1-V-b), (1-VIIa), or (1-VII-b) is a compound of formula (1-VIIa): 【Chemistry 419】 2. The compound of claim 1, which is: or a pharmaceutically acceptable salt thereof.

5. The compound of formula (1-V-a), (1-V-b), (1-VIIa), or (1-VII-b) is a compound of formula (1-VII-b): 【Chemistry 420】 2. The compound of claim 1, which is: or a pharmaceutically acceptable salt thereof.

6. R ２ａ and R ２ｂ each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR Ｄ１ and R Ｄ１ 5. The compound or pharmaceutically acceptable salt of any one of claims 1, 2, or 4, wherein is hydrogen or substituted or unsubstituted alkyl.

7. R ２ａ and R ２ｂ 7. The compound or pharmaceutically acceptable salt of claim 1, wherein:

8. R ４ａ and R ４ｂ each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR Ｄ１ and R Ｄ１ The compound or pharmaceutically acceptable salt of any one of claims 1 to 7, wherein is hydrogen, or substituted or unsubstituted alkyl.

9. R ４ａ and R ４ｂ The compound or pharmaceutically acceptable salt according to any one of claims 1 to 8, wherein both are hydrogen.

10. R ６ａ and R ６ｂ 10. The compound or pharmaceutically acceptable salt of any one of claims 1 to 9, wherein each of is independently hydrogen, halogen, cyano, hydroxyl, or substituted or unsubstituted alkyl.

11. R ６ａ and R ６ｂ The compound or pharmaceutically acceptable salt according to any one of claims 1 to 10, wherein both are hydrogen.

12. R １１ａ and R １１ｂ each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR Ｄ１ and R Ｄ１ 12. The compound or pharmaceutically acceptable salt of any one of claims 1 to 11, wherein is hydrogen, or substituted or unsubstituted alkyl.

13. R １１ａ and R １１ｂ The compound or pharmaceutically acceptable salt of any one of claims 1 to 12, wherein: are both hydrogen.

14. R １６ａ and R １６ｂ each independently represents hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, or -OR Ｄ１ and R Ｄ１ 14. The compound or pharmaceutically acceptable salt of any one of claims 1 to 13, wherein is independently hydrogen, or substituted or unsubstituted alkyl.

15. R １６ａ and R １６ｂ The compound or pharmaceutically acceptable salt of any one of claims 1 to 14, wherein: are both hydrogen.

16. R ５ But, R １９ The compound or pharmaceutically acceptable salt according to any one of claims 1 to 15, wherein R is hydrogen or methyl in the cis position relative to

17. R ５ But, R １９ The compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 15, wherein R is hydrogen or methyl in the trans position relative to R.

18. [Catalogue 432] is a double bond, and R ５ and R ６ａ Or R ６ｂ 18. The compound or pharmaceutically acceptable salt according to any one of claims 1 to 17, wherein one of: is absent.

19. 【Catalogue 433】 The compound or pharmaceutically acceptable salt according to any one of claims 1 to 17, wherein is a single bond.

20. R １９ 20. The compound or pharmaceutically acceptable salt of any one of claims 1 to 19, wherein is methyl, ethyl, or hydrogen.

21. R ３ is a substituted or unsubstituted C １－６ Alkyl or substituted or unsubstituted C １－６ 21. The compound or pharmaceutically acceptable salt of any one of claims 1 to 20, which is alkoxy.

22. R ３ But C １－３ C optionally substituted with alkoxy １－３ 22. The compound or pharmaceutically acceptable salt of any one of claims 1 to 21, wherein:

23. R １８ is a substituted or unsubstituted C １－４ 23. The compound or pharmaceutically acceptable salt of any one of claims 1 to 22, wherein:

24. R １８ is unsubstituted C １－４ 24. The compound or pharmaceutically acceptable salt of any one of claims 1 to 23, wherein: R is alkyl.

25. 25. The compound or pharmaceutically acceptable salt of any one of claims 1 to 24, wherein X is hydrogen, substituted or unsubstituted heteroaryl, or substituted or unsubstituted alkyl.

26. 25. The compound of any one of claims 1 to 24, or a pharmaceutically acceptable salt thereof, wherein X is a substituted or unsubstituted 5-10 membered heteroaryl.

27. X is, 【Chemistry 421】 and R ２０ Each instance 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 ２～６ Alkenyl, substituted or unsubstituted C ２～６ Alkynyl, substituted or unsubstituted C ３～４ carbosilyl, or substituted or unsubstituted 3- to 4-membered heterosilyl; R ＧＡ Each instance 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 carbosilyl, substituted or unsubstituted 3- to 6-membered heterosilyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to oxygen, a nitrogen protecting group when attached to nitrogen, or two R ＧＡ the groups, together with the intervening atoms, form a substituted or unsubstituted carbocyclic ring or a substituted or unsubstituted heterocyclic ring; e is 0, 1, 2, 3, 4, or 5; 25. The compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 24.

28. The compound of formula (1-V-a) is a compound of formula (1-XIII-a) or (1-XIV-a): 【Chemistry 506】 or a pharmaceutically acceptable salt thereof; R ５５ is hydrogen, halogen, cyano, or substituted or unsubstituted alkyl; 3. A compound or a pharmaceutically acceptable salt thereof according to claim 1 or claim 2.

29. The compound of formula (1-V-b) is a compound of formula (1-XIII-b) or (1-XIV-b): 【Chemistry 507】 or a pharmaceutically acceptable salt thereof; R ５５ is hydrogen, halogen, cyano, or substituted or unsubstituted alkyl; 4. A compound or a pharmaceutically acceptable salt thereof according to claim 1 or claim 3.

30. A compound or a pharmaceutically acceptable salt thereof selected from the group consisting of: 【Chemistry 422】 【Chemical Formula 423】 【Chemical 424】 【Chemistry 425】 【Chemical 426】 【Chemical 427】 【Chemistry 428】 【Chemical 429】 【Chemistry 430】 【Chemistry 431】 。

31. A pharmaceutical composition comprising a compound according to any one of claims 1 to 30, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

32. In the subject, GABA Ａ A composition comprising a compound according to any one of claims 1 to 30 or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition according to claim 31, for modulating a receptor.

33. A composition comprising a compound according to any one of claims 1 to 30 or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition according to claim 31, for treating a CNS-related disorder in a subject.

34. 34. The composition for use according to claim 33, wherein the CNS-related disorder is depression.

35. 35. The composition for use according to claim 34, wherein the depression is postpartum depression.

36. 34. The composition for use according to claim 33, wherein the CNS-related disorder is tremor.

37. 37. The composition for use according to claim 36, wherein the tremor is essential tremor.

38. 34. The composition for use according to claim 33, wherein the CNS-related disorder is stroke.

39. 34. The composition for use according to claim 33, wherein the CNS-related disorder is epilepsy or status epilepticus.

40. 40. The composition for use of claim 39, wherein the status epilepticus is convulsive status epilepticus or non-convulsive status epilepticus.

41. 40. The composition for use of claim 39, wherein the status epilepticus is convulsive status epilepticus, and the convulsive status epilepticus is early status epilepticus, established status epilepticus, refractory status epilepticus, or very refractory status epilepticus.

42. 40. The composition for use of claim 39, wherein the status epilepticus is non-convulsive status epilepticus, and the non-convulsive status epilepticus is generalized status epilepticus or complex partial status epilepticus.

43. A composition comprising a compound or a pharmaceutically acceptable salt of any one of claims 1 to 30, or a pharmaceutical composition of claim 31, for inducing sedation and / or anesthesia in a subject.

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