Biologically Active Compounds and Methods Thereof

Abstract

In particular, the present disclosure provides techniques such as compounds, compositions, methods, uses, etc. for preventing or treating various conditions, disorders or diseases. In some embodiments, the condition, disorder or disease is cancer.

Description

Technical Field

[0001] In particular, the present disclosure provides, for example, technologies useful for treating various conditions, disorders or diseases, such as compounds, compositions, methods, etc.

Background Art

[0002] Compounds have been reported to be useful in many applications, including for treating various conditions, disorders or diseases such as cancer. In some embodiments, ferroptosis dysfunction has been reported in many types of cancer.

Summary of the Invention

[0003] In particular, the present disclosure provides various compounds containing an isourea or isothiourea moiety. In some embodiments, the provided compounds contain -T-C(-N=)[-N(-)-], where T is O or S. In some embodiments, the isourea moiety is -O-C(=NR w1 )N(R w2 )(R w3 ) or has the structure of its salt form, where each variable is as described herein. In some embodiments, the isothiourea moiety is -S-C(=NR w1 )N(R w2 )(R w3 ) or has the structure of its salt form, where each variable is as described herein.

[0004] In some embodiments, the present disclosure provides R w is -T-C(=NR w1 )N(R w2 )(R w3 ) or its salt, where T is O or S, R w1 , R w2 and R w3 are each independently -L-R' or a detectable label, where Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms 1-10 aliphatic group or heteroaliphatic group, and here, one or more methylene units are optionally and independently -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-substituted, Each -Cy- is independently an optionally substituted 3- to 20-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms, Each R’ is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R)2, -S(O)R, or -S(O)OR, and Each R is independently -H or a C 1~20 aliphatic group of, a C having 1 to 10 heteroatoms 1~20 heteroaliphatic group of, a C 6~20 aryl group of, a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and an optionally substituted group selected from the group consisting of combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or, Two R groups are optionally and independently bonded to each other covalently, or, Two or more R groups on the same atom are optionally and independently combined with the atom to form an optionally substituted 3- to 20-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the atom, or, Two or more R groups on two or more atoms are optionally and independently combined with their intervening atoms to form an optionally substituted 3- to 30-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the intervening atoms, characterized by, R wTo provide a compound containing

[0005] In some embodiments, the present disclosure L w is a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms 1-6 aliphatic group or heteroaliphatic group, and wherein one or more methylene units are optionally and independently -C(R')2-, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R')-, -C(O)S-, or -C(O)O-substituted, and each other variable is as described herein independently, characterized by -L w -R w To provide a compound containing or its salt form.

[0006] For example, in some embodiments, the present disclosure provides a compound having the structure of formula A or a salt thereof:

[0007]

Chemical formula

[0008]

Chemical formula

[0009] In some embodiments, the present disclosure provides a compound having the structure of formula A', or a salt thereof:

[0010]

Chemical formula

[0011] In some embodiments, the present disclosure provides a compound having the structure of formula A-I, or a salt thereof:

[0012]

Chemical formula

[0013] In some embodiments, the present disclosure provides a compound having the structure of formula A-II, or a salt thereof:

[0014]

Chemical formula

[0015] In some embodiments, the present disclosure provides a compound having the structure of formula A-III, or a salt thereof:

[0016]

Chemical formula

[0017] In some embodiments, the present disclosure provides: Provided is a compound having the structure of Formula B, or a salt thereof:

[0018] [ka] During the ceremony, L R teeth,

[0019] [ka] , L, -C≡C-, optionally substituted -CH=CH-, -C(O)-, -C(S)-, or -C(NR'')-; L b is L, R b is R″, Ring L is an optionally substituted 3-20 membered monocyclic, bicyclic or polycyclic ring having 0-10 heteroatoms. R 4 is or contains an isourea or isothiourea moiety, or -L w -R w and L w is a covalent bond or an optionally substituted divalent C 1-6 an aliphatic or heteroaliphatic group, wherein one or more methylene units are optionally and independently replaced by -C(R')2-, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R')-, -C(O)S-, or -C(O)O-; R w is -TC(=NR w1 )N(R w2 )(R w3 ) and R w1 , R w2 , and Rw3 are each independently, -L-R’, or a detectable moiety, T is O, or S, each R s is independently an optionally substituted group selected from R'', halogen, -CN, oxo, -NO2, or an acyl group, acylamino group, hydroxy group, amino acid group, amine group, amide group, carbamate group, ester group, ether group, carboxylic acid group, thio group, thioalkyl group, thioester group, thioether group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, alkylsulfonyl group, and arylsulfonyl group, q is from 0 to 10, each R” is independently hydrogen, halogen, -L-R’, -L-OR’, -L-SR’, -L-C(O)OR’, -L-C(O)SR’, -L-C(O)N(R’)2, -L-OC(O)N(R’)2, -L-C(O)R’, -L-N(R’)2, -CN, -OC(R’)2COOH, -SC(R’)2COOH, -N(R’)C(R’)2COOH, or an optionally substituted group selected from an alkylsulfonyl group, arylsulfonyl group, carboxylic acid ester group, ester group, ether group, amide group, carbohydrate group, amino acid group, acyl group, acyl group substituted with an alkoxy, alditol group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, thioalkyl group, thioester group, and thioether group, each R’ is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R)2, -S(O)R, or -S(O)OR, each L is independently a covalent bond, or an optionally substituted divalent C having 1 to 6 heteroatoms 1-10an aliphatic group or a heteroaliphatic group, wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O- each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms; each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C 1~20 and a heteroaliphatic group of C having 1 to 10 heteroatoms, an aryl group of C 1~20 a heteroaryl group of 5 to 20 members having 1 to 10 heteroatoms, a heterocyclyl of 3 to 20 members having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or 6~20 two R groups are optionally and independently covalently bonded to each other, or two or more R groups on the same atom are optionally and independently combined with the atom to form an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms in addition to the atom, or two or more R groups on two or more atoms are optionally and independently combined with their intervening atoms to form an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 30 members having 0 to 10 heteroatoms in addition to the intervening atoms. In some embodiments, the present disclosure provides a compound having the structure of Formula B-1, or a salt thereof:

[0020] In some embodiments, the present disclosure provides a compound having the structure of Formula B-1, or a salt thereof:

[0021]

Chemical formula

[0022] In some embodiments, L b is -Cy- as described herein. In some embodiments, L b is an optionally substituted phenyl ring. In some embodiments, L b is an optionally substituted 5- to 6-membered heteroaryl ring having 1 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur. In some embodiments, L b is an optionally substituted bicyclic 9- to 10-membered heteroaryl ring having 1 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

[0023] In some embodiments, the present disclosure provides a compound having the structure of B-1a, B-1b, B-1c, or B-1d, or a salt thereof:

[0024]

Chemical formula

[0025] In some embodiments, the present disclosure provides a compound having the structure of B-2a, B-2b, B-2c, B-2d, or B-2e, or a salt thereof:

[0026] [Chemical formula] wherein R s1 , R 4 , L b , and R b each is as defined above and as described herein.

[0027] In some embodiments, the present disclosure provides a compound having the structure of B-3a, B-3b, B-3c, or B-3d, or a salt thereof:

[0028] [Chemical formula] wherein R s1 , R 4 , and R b each is as defined above and as described herein.

[0029] In some embodiments, the present disclosure provides a compound having the structure of B-4a, B-4b, B-4c, or B-4d, or a salt thereof:

[0030] [Chemical formula] wherein R s1 , R 4 , and R bEach of them is as defined above and as described in this specification.

[0031] In some embodiments, the present disclosure provides a compound having the structure of B-5a, B-5b, B-5c, or B-5d, or a salt thereof:

[0032] [Chemical formula] Wherein R s1 , R 4 , and R b Each of them is as defined above and as described in this specification.

[0033] In some embodiments, the present disclosure provides a compound having the structure of B-6a, B-6b, B-6c, or B-6d, or a salt thereof:

[0034] [Chemical formula] Wherein R s1 , R 4 , and R b Each of them is as defined above and as described in this specification.

[0035] In some embodiments, the present disclosure provides a compound having the structure of B-7a, B-7b, B-7c, or B-7d, or a salt thereof:

[0036] [Chemical formula] Wherein R s1 , R 4 , and R b Each of them is as defined above and as described in this specification.

[0037] In some embodiments, the present disclosure provides a compound having the structure of Formula C, or a salt thereof: wherein:

[0038]

Chemical formula

[0039] In some embodiments, the present disclosure provides a compound having the structure of formula D, or a salt thereof:

[0040]

Chemical formula

[0041] In some embodiments, the present disclosure provides a compound having the structure of Formula E, or a salt thereof:

[0042] [Chemical Formula] wherein R 4 is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or is -L w -R w and L w is a covalent bond, or an optionally substituted divalent C 1-6 aliphatic or heteroaliphatic group having from 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O- R w is -T-C(=NR w1 )N(R w2 )(R w3 ) R w1 , R w2 , and R w3 are each independently -L-R’, or a detectable moiety T is O, or S R 17 and R 18is, independently, an optionally substituted monocyclic, bicyclic or polycyclic aromatic ring of 5 to 20 members having 0 to 5 heteroatoms each, Ring C is an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 6 heteroatoms, L is, independently, a covalent bond, or an optionally substituted divalent C 1-10 aliphatic group or heteroaliphatic group having 1 to 6 heteroatoms each, and wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-, each -Cy- is, independently, an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms, each R’ is, independently, R, -OR, -C(O)R, -C(O)OR, -C(O)N(R)2, -S(O)R, or -S(O)OR, each R is, independently, -H, or a C 1~20 aliphatic group of, a C having 1 to 10 heteroatoms each 1~20 heteroaliphatic group of, a C 6~20 aryl group of, a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms each, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms each, and an optionally substituted group selected from the group consisting of combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or, two R groups are optionally and independently bonded to each other to form a covalent bond, or, two or more R groups on the same atom are optionally and independently combined with the atom to form an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms in addition to the atom, or, Two or more R groups on two or more atoms may optionally and independently, together with their intervening atoms, form an optionally substituted 3- to 30-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to those intervening atoms.

[0043] In some embodiments, the present disclosure provides a compound having the structure of Formula F, or a salt thereof:

[0044] [Chemical formula] Wherein R 4 is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L w -R w and L w is a covalent bond, or an optionally substituted divalent C 1-6 aliphatic or heteroaliphatic group having 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O- R w is -T-C(=NR w1 )N(R w2 )(R w3 ) R w1 , R w2 , and R w3 are each independently -L-R’, or a detectable moiety T is O, or S R s6 , R s7 are each independently R s Each R sis an optionally substituted group independently selected from R'', halogen, -CN, oxo, -NO2, or acyl group, acylamino group, hydroxy group, amino acid group, amine group, amide group, carbamate group, ester group, ether group, carboxylic acid group, thio group, thioalkyl group, thioester group, thioether group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, alkylsulfonyl, and arylsulfonyl, each R” is independently hydrogen, halogen, -L-R’, -L-OR’, -L-SR’, -L-C(O)OR’, -L-C(O)SR’, -L-C(O)N(R’)2, -L-OC(O)N(R’)2, -L-C(O)R’, -L-N(R’)2, -CN, -OC(R’)2COOH, -SC(R’)2COOH, -N(R’)C(R’)2COOH, or an optionally substituted group selected from alkylsulfonyl group, arylsulfonyl group, carboxylic acid ester group, ester group, ether group, amide group, carbohydrate group, amino acid group, acyl group, acyl group substituted with alkoxy, alditol group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, thioalkyl group, thioester group, and thioether group, q, x and y are each independently 0 to 4, L is independently a covalent bond, or an optionally substituted divalent C 1-10 aliphatic group or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-, each -Cy- is independently an optionally substituted 3- to 20-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms, Each R’ is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R)2, -S(O)R, or -S(O)OR, each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C 1~20 having 1 to 10 heteroatoms, a heteroaliphatic group of C 1~20 having 1 to 10 heteroatoms, an aryl group of C 6~20 a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups optionally and independently form a covalent bond with each other, or two or more R groups on the same atom optionally and independently together with the atom form an optionally substituted 3- to 20-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the atom, or two or more R groups on two or more atoms optionally and independently together with their intervening atoms form an optionally substituted 3- to 30-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the intervening atoms.

[0045] In some embodiments, the present disclosure provides a compound having the structure of formula G, or a salt thereof:

[0046]

Chemical formula

[0047]

Chemical formula

[0048] In some embodiments, the present disclosure, provides a compound having the structure of formula G, or a salt thereof:

[0049]

Chemical formula

[0050]

Chemical formula

[0051] In some embodiments, the provided compounds are biologically active and useful for one or more properties and / or activities of various biological agents such as polypeptides. In some embodiments, the provided compounds are inhibitors. In some embodiments, the provided compounds are covalent inhibitors. In some embodiments, the urea or isothiourea moiety is released after a compound containing such a moiety contacts a nucleophile, such as an agent containing -SH, -SeH, etc. In some embodiments, the provided technologies, such as compounds, compositions, methods, etc., react selectively with a specific nucleophile moiety over other nucleophile moieties. In some embodiments, the provided technology reacts selectively with a -SeH nucleophile over a -SH nucleophile. In some embodiments, the provided technology reacts selectively with a selenocysteine residue over a cysteine residue. In some embodiments, under equivalent conditions, the selectivity is about or at least about 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, 1.7, 1.8, 1.9, 2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200, 300, 400, 500, 1000-fold.

[0052] In some embodiments, the present disclosure provides techniques for introducing moieties into a system. In some embodiments, the techniques provided include generating urea from an isourea moiety or generating thiourea from an isothiourea moiety. In some embodiments, [LOAD]-R 4 is a compound having the structure of or a salt thereof, provided that [LOAD] is or comprises one or more small molecule, nucleic acid, polypeptide, lipid, and / or carbohydrate moieties. In some embodiments, [LOAD] is attached to a nucleophilic moiety, such as -Se- or -S-. In some embodiments, [LOAD] is attached to a selenocysteine residue via -Se-. In some embodiments, [LOAD] is attached to a cysteine residue via -S-.

[0053] The provided technology is useful for many applications. For example, in some embodiments, the provided technology is useful for modulating the properties and activities of polypeptides. In some embodiments, the present disclosure provides a technology for modulating the properties of polypeptides. In some embodiments, the present disclosure provides a technology for modulating the properties of polypeptides within a system, including administering or delivering the provided compound or composition to the system. In some embodiments, the present disclosure provides a technology for inhibiting the properties of polypeptides. In some embodiments, the polypeptide includes a nucleophilic moiety, such as -SeH, -SH, etc. In some embodiments, the polypeptide includes selenocysteine residues. In some embodiments, the polypeptide includes cysteine residues. In some embodiments, upon contact with the provided compound, the selenocysteine residues are covalently modified. In some embodiments, upon contact with the provided compound, the cysteine residues are covalently modified. In some embodiments, upon contact with the provided compound, the selenocysteine residues are covalently modified to a higher level compared to the cysteine residues within the same polypeptide. In some embodiments, the polypeptide includes the characteristic sequence elements of GPX4. In some embodiments, the characteristic sequence elements include amino acid residues containing -SeH. In some embodiments, the characteristic sequence elements include selenocysteine. In some embodiments, the characteristic sequence elements include amino acid residues containing -SH. In some embodiments, the characteristic sequence elements include cysteine. In some embodiments, the polypeptide is GPX4. In some embodiments, the system is an in vivo system. In some embodiments, the system is an in vitro system. In some embodiments, the system is a cell or includes cells. In some embodiments, the system is a tissue or includes tissues. In some embodiments, the system is an organ or includes organs. In some embodiments, the system is a subject. In some embodiments, the system is an animal. In some embodiments, the system is a human. In some embodiments, the activity is modulated.In some embodiments, the activity is inhibited.

[0054] In some embodiments, the technology provided can inhibit cell proliferation. In some embodiments, the technology provided provides a higher level of ferroptosis compared to the case where the technology or reference technology is absent. In some embodiments, the technology provided can induce or increase ferroptosis.

[0055] In some embodiments, the compounds provided are useful for preventing or treating various conditions, disorders or diseases. In some embodiments, the present disclosure provides a method for preventing or treating a condition, disorder or disease, the method comprising administering or delivering an effective amount of the compound or composition provided to a subject susceptible to or suffering from them. In some embodiments, the condition, disorder or disease is a proliferative condition, disorder or disease. In some embodiments, the condition, disorder or disease is cancer. In some embodiments, the condition, disorder or disease is related to GPX4. In some embodiments, the subject benefits from an increase in the level of ferroptosis.

[0056] In some embodiments, the present disclosure provides a pharmaceutical composition comprising or delivering the compound provided and a pharmaceutically acceptable carrier.

[0057] Those skilled in the art reading the present disclosure will understand that the isourea and / or isothiourea moieties described herein can be utilized for various purposes. For example, they can be utilized to replace a leaving group, such as a halogen, in various agents for many uses, including substitution of the leaving group of various biologically active compounds. In some embodiments, an electrophilic moiety comprising an isourea and / or isothiourea moiety, such as, -C(O)-CH2-R w(Here, -CH2- is optionally substituted) can be used to substitute electrophilic groups in various agents, including uses for substituting such groups in various biologically active compounds, for example, -C(O)-CH=CH2, -C(O)-C≡CH, etc.

[0058] In some embodiments, the present disclosure provides techniques for producing various compounds. In some embodiments, the present disclosure provides a method comprising reacting a first compound comprising an -OH group or a salt thereof with a second compound comprising -CN to form an isourea moiety. In some embodiments, the present disclosure provides a method comprising reacting a first compound comprising an -OH group or a salt thereof with a second compound comprising -N=C=N- to form an isourea moiety.

[0059] In some embodiments, the present disclosure provides techniques for evaluating or characterizing various compounds and compositions. Many techniques, such as cells, animal models, clinical trials, etc., can be utilized in accordance with the present disclosure. Specific useful techniques are described in the examples. In some embodiments, modifications of amino acid residues, such as selenocysteine and / or cysteine amino acid residues, can be evaluated using mass spectrometry.

[0060] As will be understood by those skilled in the art, the compounds of the present disclosure can be provided in various forms, such as salts, esters, solvates, prodrugs, etc. In some embodiments, the provided compound is in the form of a salt. In some embodiments, the provided compound is in the form of a pharmaceutically acceptable salt. In some embodiments, the provided compound is in the form of a solvate. In some embodiments, the provided compound is a prodrug. In some embodiments, the provided compound is an ester. In some embodiments, the compound is provided as a single stereoisomer. In some embodiments, the compound is provided as a mixture or in a state of two or more stereoisomers. **DETAILED DESCRIPTION OF THE INVENTION**

[0061] The technology of the present disclosure can be more easily understood by referring to the following detailed description of specific embodiments. Definitions

[0062] As used herein, unless otherwise specified, the following definitions shall apply. For the purposes of the present disclosure, chemical elements are identified according to the Periodic Table of the Elements, CAS version, Handbook of Chemistry and Physics, 75th Edition. Further, the general principles of organic chemistry are described in "Organic Chemistry", Thomas Sorrell, University Science Books, Sausalito: 1999, and "March's Advanced Organic Chemistry", 5th Edition, Editors: Smith, M. B. and March, J., John Wiley & Sons, New York: 2001.

[0063] As used herein, unless otherwise indicated by context: (i) the term "a" or "an" may be understood to mean "at least one"; (ii) the term "or / alternatively" may be understood to mean "and / or"; (iii) the terms "comprising", "comprised of", "containing" (whether used with "but not limited to") and "contains" (whether used with "but not limited to") may be understood to include the listed components or steps, whether presented by themselves or in conjunction with one or more additional components or steps; and (iv) the term "another" may be understood to mean at least an additional / second one or more; (v) the terms "about" and "substantially" may be understood to allow for standard variations, as understood by those skilled in the art; (vi) when ranges are provided, endpoints are included. Unless the context is clear otherwise, isomers of compounds are included. As would be understood by those skilled in the art, compounds can be provided, administered, or delivered in various forms, such as salts (e.g., pharmaceutically acceptable salts), solvates, hydrates, esters, prodrugs, tautomers, etc.

[0064] "Aliphatic" or "aliphatic group": As used herein, a straight-chain (i.e., unbranched) or branched, substituted or unsubstituted hydrocarbon chain that is completely saturated or contains one or more unsaturated units (not aromatic), or a substituted or unsubstituted monocyclic, bicyclic, or polycyclic hydrocarbon ring that is completely saturated or contains one or more unsaturated units (not aromatic), or a combination thereof. In some embodiments, the aliphatic group contains 1 to 50 aliphatic carbon atoms. In some embodiments, the aliphatic group contains 1 to 20 aliphatic carbon atoms. In other embodiments, the aliphatic group contains 1 to 10 aliphatic carbon atoms. In other embodiments, the aliphatic group contains 1 to 9 aliphatic carbon atoms. In other embodiments, the aliphatic group contains 1 to 8 aliphatic carbon atoms. In other embodiments, the aliphatic group contains 1 to 7 aliphatic carbon atoms. In other embodiments, the aliphatic group contains 1 to 6 aliphatic carbon atoms. In still other embodiments, the aliphatic group contains 1 to 5 aliphatic carbon atoms, and in still other embodiments, the aliphatic group contains 1, 2, 3, or 4 aliphatic carbon atoms. Suitable aliphatic groups include, but are not limited to, straight-chain or branched, substituted or unsubstituted alkyl, alkenyl, alkynyl groups, and hybrid groups thereof, such as (cycloalkyl)alkyl, (cycloalkenyl)alkyl or (cycloalkyl)alkenyl.

[0065] Alkenyl: As used herein, the term "alkenyl" refers to an aliphatic group having one or more double bonds, as defined herein.

[0066] Alkyl: As used herein, the term "alkyl" is given its ordinary meaning in the art and can include saturated aliphatic groups including straight-chain alkyl groups, branched-chain alkyl groups, cycloalkyl (alicyclic) groups, alkyl-substituted cycloalkyl groups, and cycloalkyl-substituted alkyl groups. In some embodiments, the alkyl has 1 to 100 carbon atoms. In certain embodiments, the straight-chain or branched-chain alkyl has about 1 to 20 carbon atoms in its backbone (e.g., in the case of a straight-chain, C1 to C 20, in the case of a branched chain, C2 to C 20 ) or has from about 1 to 10 carbon atoms. In some embodiments, the cycloalkyl ring has from about 3 to 10 carbon atoms in its ring structure, such rings being monocyclic, bicyclic, or polycyclic, or having from about 5, 6, or 7 carbon atoms in the ring structure. In some embodiments, the alkyl group may be a lower alkyl group, and the lower alkyl group contains 1 to 4 carbon atoms (e.g., in the case of straight-chain lower alkyl, C1 to C4).

[0067] Alkynyl: As used herein, the term "alkynyl" refers to an aliphatic group having one or more triple bonds, as defined herein.

[0068] Animal: As used herein, the term "animal" refers to any member of the animal kingdom. In some embodiments, "animal" refers to a human at any stage of development. In some embodiments, "animal" refers to a non-human animal at any stage of development. In certain embodiments, the non-human animal is a mammal (e.g., rodents, mice, rats, rabbits, monkeys, dogs, cats, sheep, cows, primates, and / or pigs). In some embodiments, animals include, but are not limited to, mammals, birds, reptiles, amphibians, fish, and / or insects. In some embodiments, the animal may be a transgenic animal, a genetically engineered animal, and / or a clone.

[0069] Aryl: As used herein, the term "aryl" is used alone or as part of a larger moiety such as "aralkyl", "aralkoxy", or "aryloxyalkyl" and refers to a monocyclic, bicyclic, or polycyclic ring system having a total of 5 to 30 ring members, wherein at least one ring in the system is aromatic. In some embodiments, the aryl group is a monocyclic, bicyclic, or polycyclic ring system having a total of 5 to 14 ring members, wherein at least one ring in the system is aromatic and each ring in the system contains 3 to 7 ring members. In some embodiments, each monocyclic ring unit is aromatic. In some embodiments, the aryl group is a biaryl group. The term "aryl" may be used interchangeably with the term "aryl ring". In certain embodiments of the present disclosure, "aryl" refers to an aromatic ring system which may have one or more substituents and includes, but is not limited to, phenyl, biphenyl, naphthyl, binaphthyl, anthracyl, etc. Also, as used herein, the scope of the term "aryl" includes groups in which an aromatic ring is fused to one or more non-aromatic rings, such as indanyl, phthalimidyl, naphthimidyl, phenanthridinyl, or tetrahydronaphthyl, etc.

[0070] Characteristic portion: As used herein, the term "characteristic portion" in its broadest sense refers to a portion of a substance whose presence (or absence) correlates with the presence (or absence) of a particular characteristic, attribute, or activity of the substance. In some embodiments, the characteristic portion of a substance is a portion that is found in that substance and related substances that share a particular characteristic, attribute, or activity, but is not found in related substances that do not share the particular characteristic, attribute, or activity. In certain embodiments, the characteristic portion shares at least one functional property with the intact substance. For example, in some embodiments, the "characteristic portion" of a protein or polypeptide includes a continuous stretch of amino acids, or a set of amino acids, or in some embodiments, a set of continuous stretches of amino acids, that together are characteristic of the protein or polypeptide. In some embodiments, each such continuous stretch generally includes at least 2, 5, 10, 15, 20, 50, or more amino acids. Generally, the characteristic portion of a substance (e.g., a protein, antibody, etc.) is one that shares at least one functional characteristic with the related intact substance in addition to the sequence and / or structural identity specified above. In some embodiments, the characteristic portion may be biologically active.

[0071] Characteristic array element: As used herein, the phrase "characteristic array element" refers to an array element found in a polymer (e.g., a polypeptide or nucleic acid) that represents a characteristic portion of that polymer. In some embodiments, the presence of a characteristic array element correlates with the presence or level of a particular activity or property of the polymer. In some embodiments, the presence (or absence) of a characteristic array element defines a particular polymer as a member (or not a member) of a particular family or group of such polymers. Characteristic array elements typically comprise at least two monomers (e.g., amino acids or nucleotides). In some embodiments, characteristic array elements comprise at least 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 20, 25, 30, 35, 40, 45, 50 or more monomers (e.g., consecutively linked monomers). In some embodiments, characteristic array elements comprise at least a first and a second stretch of contiguous monomers spaced apart by one or more spacer regions. The length of the spacer regions may vary or may not vary between polymers sharing the array element.

[0072] Comparable: The term "comparable" is used herein to refer to two (or more) sets of conditions or situations that are sufficiently similar to allow the results obtained or phenomena observed to be compared. In some embodiments, sets of comparable conditions or situations are characterized by a plurality of substantially identical features and one or a few different features. One of ordinary skill in the art will understand that sets of conditions are comparable to each other if they are characterized by a sufficient number and variety of substantially identical features to warrant a reasonable conclusion that differences in the results obtained or phenomena observed under different sets of conditions or situations are caused by, or indicative of, changes in the varying feature.

[0073] Cycloaliphatic: The terms "cycloaliphatic", "carbocyclic", "carbocyclyl", "carbocyclic radical", and "carbocycle" are used interchangeably and, as used herein, unless otherwise specified, refer to a saturated or partially unsaturated but non-aromatic cycloaliphatic monocyclic, bicyclic, or polycyclic ring system having 3 to 30 ring members as described herein. Cycloaliphatic groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, norbornyl, adamantyl, and cyclooctadienyl. In some embodiments, the cycloaliphatic group has 3 to 6 carbons. In some embodiments, the cycloaliphatic group is saturated and is a cycloalkyl. The term "cycloaliphatic" may also include aliphatic rings fused to one or more aromatic or non-aromatic rings, such as decahydronaphthyl or tetrahydronaphthyl. In some embodiments, the cycloaliphatic group is bicyclic. In some embodiments, the cycloaliphatic group is tricyclic. In some embodiments, the cycloaliphatic group is polycyclic. In some embodiments, "cycloaliphatic" refers to a C3-C6 monocyclic hydrocarbon that is either fully saturated or contains one or more unsaturated units but is not aromatic and has a single point of attachment to the remainder of the molecule, or a C8-C 10 bicyclic or polycyclic hydrocarbon, or a C9-C that is either fully saturated or contains one or more unsaturated units but is not aromatic and has a single point of attachment to the remainder of the molecule 16 refers to a polycyclic hydrocarbon.

[0074] Heteroaliphatic: As used herein, the term "heteroaliphatic" is given its ordinary meaning in the art and refers to an aliphatic group as described herein, where one or more carbon atoms are independently replaced by one or more heteroatoms (e.g., oxygen, nitrogen, sulfur, silicon, phosphorus, etc.). In some embodiments, one or more units selected from C, CH, CH2, and CH3 are independently replaced by one or more heteroatoms (including their oxidized and / or substituted forms). In some embodiments, the heteroaliphatic group is a heteroalkyl. In some embodiments, the heteroaliphatic group is a heteroalkenyl.

[0075] Heteroalkyl: As used herein, the term "heteroalkyl" is given its ordinary meaning in the art and refers to an alkyl group as described herein, where one or more carbon atoms are independently replaced by one or more heteroatoms (e.g., oxygen, nitrogen, sulfur, silicon, phosphorus, etc.). Examples of heteroalkyl groups include, but are not limited to, alkoxy, poly(ethylene glycol), alkyl-substituted amino, tetrahydrofuranyl, piperidinyl, morpholinyl, etc.

[0076] Heteroaryl: As used herein, the terms "heteroaryl" and "heteroar-" are used alone or as part of a larger moiety, for example, "heteroalkyl" or "heteroalkoxy" refer to a monocyclic, bicyclic or polycyclic ring system having a total of 5 to 30 ring members (in this system, at least one ring is aromatic and at least one aromatic ring atom is a heteroatom). In some embodiments, the heteroaryl group is a group having 5 to 10 ring atoms (i.e., monocyclic, bicyclic or polycyclic), and in some embodiments, it is 5, 6, 9, or 10 ring atoms. In some embodiments, each monocyclic ring unit is aromatic. In some embodiments, the heteroaryl group has 6, 10, or 14 π electrons shared in a cyclic array and has 1 to 5 heteroatoms in addition to carbon atoms. Heteroaryl groups include, but are not limited to, thienyl, furanyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, isothiazolyl, thiadiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, indolizinyl, purinyl, naphthyridinyl, and pteridinyl. In some embodiments, heteroaryl is a hetero-biaryl group such as, for example, bipyridyl. As used herein, the terms "heteroaryl" and "heteroar-" also include groups in which a heteroaromatic ring is fused to one or more aryl, cycloaliphatic, or heterocyclyl rings and the radical or point of attachment is on the heteroaromatic ring. Non-limiting examples include indolyl, isoindolyl, benzothienyl, benzofuranyl, dibenzofuranyl, indazolyl, benzimidazolyl, benzothiazolyl, quinolyl, isoquinolyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, 4H-quinolizinyl, carbazolyl, acridinyl, phenazinyl, phenothiazinyl, phenoxazinyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, and pyrido[2,3-b]-1,4-oxazin-3(4H)-one. The heteroaryl group can be monocyclic, bicyclic, or polycyclic.The term "heteroaryl" can be used interchangeably with the terms "heteroaryl ring", "heteroaryl group", or "heteroaromatic". Any of these terms includes a ring that is optionally substituted. The term "heteroalkyl" refers to an alkyl group substituted by a heteroaryl group, and the alkyl portion and the heteroaryl portion are independently optionally substituted.

[0077] Heteroatom: As used herein, the term "heteroatom" means an atom that is not carbon or hydrogen. In some embodiments, the heteroatom is boron, oxygen, sulfur, nitrogen, phosphorus, or silicon (including oxidized forms of nitrogen, sulfur, phosphorus, or silicon, charged forms of nitrogen (e.g., quaternized forms, forms such as iminium groups, etc.), phosphorus, sulfur, oxygen, etc.). In some embodiments, the heteroatom is silicon, phosphorus, oxygen, sulfur, or nitrogen. In some embodiments, the heteroatom is silicon, oxygen, sulfur, or nitrogen. In some embodiments, the heteroatom is oxygen, sulfur, or nitrogen.

[0078] Heterocyclic Ring: As used herein, the terms "heterocyclic ring", "heterocyclyl", "heterocyclic radical", and "heterocyclic" are used interchangeably herein and refer to a monocyclic, bicyclic, or polycyclic ring moiety (e.g., 3 to 30 members), saturated or partially unsaturated, having one or more heteroatom ring atoms. In some embodiments, the heterocyclyl group is saturated or partially unsaturated and is a stable 5- to 7-membered monocyclic or 7- to 10-membered bicyclic heterocyclic moiety having, in addition to carbon atoms, one or more, preferably 1 to 4, of the heteroatoms as defined above. When used with respect to the ring atoms of a heterocycle, the term "nitrogen" includes substituted nitrogen. By way of example, in a saturated or partially unsaturated ring having 0 to 3 heteroatoms selected from oxygen, sulfur, and nitrogen, nitrogen can be N (as in 3,4-dihydro-2H-pyrrolyl), NH (as in pyrrolidinyl), or +NR (as in N-substituted pyrrolidinyl). The heterocyclic ring can be attached to a pendant group at any heteroatom or carbon atom, resulting in a stable structure, and any ring atom can be optionally substituted. Examples of such saturated or partially unsaturated heterocyclic radicals include, but are not limited to, tetrahydrofuranyl, tetrahydrothienyl, pyrrolidinyl, piperidinyl, pyrrolinyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, decahydroquinolinyl, oxazolidinyl, piperazinyl, dioxanyl, dioxolanyl, diazepinyl, oxazepinyl, thiazepinyl, morpholinyl, and quinuclidinyl. The terms "heterocyclic ring", "heterocyclyl", "heterocyclyl ring", "heterocyclic group", "heterocyclic moiety", and "heterocyclic radical" are used interchangeably herein and also include groups in which a heterocyclyl ring is fused to one or more aryl, heteroaryl, or cycloaliphatic rings, such as, for example, indolinyl, 3H-indolyl, chromanyl, phenanthridinyl, or tetrahydroquinolinyl. The heterocyclyl group can be monocyclic, bicyclic, or polycyclic. The term "heterocyclylalkyl" refers to an alkyl group substituted with a heterocyclyl, and the alkyl and heterocyclyl moieties are independently optionally substituted.

[0079] Optionally substituted: As described herein, the compounds of the present disclosure may contain optionally substituted and / or substituted moieties. Generally, the term "substituted", whether or not preceded by the term "optionally", means that one or more hydrogens of the specified moiety are replaced by a suitable substituent. Unless otherwise specified, an "optionally substituted" group may have suitable substituents at each substitutable position of the group, and if one or more positions within any structure are substituted with one or more substituents selected from the specified groups, the substituents may be the same or different at all positions. In some embodiments, an optionally substituted group is unsubstituted. The combinations of substituents contemplated by the present disclosure preferably result in the formation of stable or chemically feasible compounds. As used herein, the term "stable" refers to compounds that do not substantially change even when subjected to the conditions that allow for their generation, detection, and in certain embodiments their recovery, purification, and use for one or more of the purposes disclosed herein. Specific substituents are described below.

[0080] Substitutable atoms, for example suitable monovalent substituents on suitable carbon atoms, are independently halogen; -(CH2) 0-4 R°; -(CH2) 0-4 OR°; -O(CH2) 0-4 R°, -O-(CH2) 0-4 C(O)OR°; -(CH2) 0-4 CH(OR°)2; -(CH2) 0-4 Ph (optionally substituted with R°); -(CH2) 0-4 O(CH2) 0-1 Ph (optionally substituted with R°); -CH=CHPh (optionally substituted with R°); -(CH2) 0-4 O(CH2) 0-1 -pyridyl (optionally substituted with R°); -NO2; -CN; -N3; -(CH2) 0-4 N(R°)2; -(CH2) 0-4 N(R°)C(O)R°; -N(R°)C(S)R°; -(CH2) 0-4N(R°)C(O)NR°2; -N(R°)C(S)NR°2; -(CH2) 0-4 N(R°)C(O)OR°; -N(R°)N(R°)C(O)R°; -N(R°)N(R°)C(O)NR°2; -N(R°)N(R°)C(O)OR°; -(CH2) 0-4 C(O)R°;-C(S)R°; -(CH2) 0-4 C(O)OR°; -(CH2) 0-4 C(O)SR°;(CH2) 0-4 C(O)OSiR°3; -(CH2) 0-4 OC(O)R°; -OC(O)(CH2) 0-4 SR°、-SC(S)SR°; -(CH2) 0-4 SC(O)R°; -(CH2) 0-4 C(O)NR°2; -C(S)NR°2; -C(S)SR°;(CH2) 0-4 OC(O)NR°2; C(O)N(OR°)R°; -C(O)C(O)R°; -C(O)CH2C(O)R°; -C(NOR°)R°;(CH2) 0-4 SSR°; -(CH2) 0-4 S(O)2R°;-(CH2) 0-4 S(O)2OR°; -(CH2) 0-4 OS(O)2R°; -S(O)2NR°2; -(CH2) 0-4 S(O)R°; -N(R°)S(O)2NR°2; -N(R°)S(O)2R°; -N(OR°)R°; -C(NH)NR°2; -Si(R°)3; -OSi(R°)3; -B(R°)2; -OB(R°)2; -OB(OR°)2; -P(R°)2; -P(OR°)2; -P(R°)(OR°); -OP(R°)2; -OP(OR°)2; -OP(R°)(OR°); -P(O)(R°)2; -P(O)(OR°)2; -OP(O)(R°)2; -OP(O)(OR°)2; -OP(O)(OR°)(SR°); -SP(O)(R°)2; -SP(O)(OR°)2; -N(R°)P(O)(R°)2; -N(R°)P(O)(OR°)2; -P(R°)2[B(R°)3]; -P(OR°)2[B(R°)3]; -OP(R°)2[B(R°)3]; -OP(OR°)2[B(R°)3]; -(C1-4 Linear or branched alkylene)ON(R°)2; or -(C 1-4 linear or branched alkylene)C(O)ON(R°)2, where each R° may be optionally substituted as defined herein and is independently hydrogen, C 1-20 C having 1-5 heteroatoms independently selected from aliphatic, nitrogen, oxygen, sulfur, silicon and phosphorus 1-20 Heteroaliphatic, -CH2-(C 6-14 Aryl), -O(CH2) 0-1 (C 6-14 aryl), -CH2- (a 5-14 membered heteroaryl ring), a 5-20 membered monocyclic, bicyclic, or polycyclic saturated, partially unsaturated, or aryl ring having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, silicon, and phosphorus, or, notwithstanding the above definitions, two independent occurrences of R° together with their intervening atoms form a 5-20 membered monocyclic, bicyclic, or polycyclic saturated, partially unsaturated, or aryl ring (having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, silicon, and phosphorus) which may be substituted as defined below.

[0081] Suitable monovalent substituents on R° (or the ring formed by two independent occurrences of R° together with their intervening atoms) are independently halogen, -(CH2), 0-2 R ● , -(Halo R ● ), -(CH2) 0-2 OH, -(CH2) 0-2 OR ● , -(CH2) 0-2 CH(OR ● )2, -O(HaloR ● ), -CN, -N3, -(CH2) 0-2 C(O)R ● , -(CH2) 0-2 C(O)OH, -(CH2) 0-2 C(O)OR ● , -(CH2) 0-2 S.R. ● , -(CH2) 0-2 SH, -(CH2) 0-2NH2, -(CH2) 0-2 NHR ● , -(CH2) 0-2 NR ● 2, -NO2, -SiR ● 3, -OSiR ● 3, C(O)SR ● , -(C 1-4 linear or branched alkylene)C(O)OR ● , or -SSR ● and wherein each R ● is unsubstituted or, when preceded by "halo", is substituted only with one or more halogens, and C 1-4 aliphatic, -CH2Ph, -O(CH2) 0-1 Ph, and is a 5- to 6-membered saturated, partially unsaturated, or aryl ring having from 0 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur. Suitable divalent substituents on the saturated carbon atoms of R° include =O and =S.

[0082] Suitable divalent substituents (e.g., on suitable carbon atoms) are independently as follows: =O, =S, =NNR * 2, =NNHC(O)R * , =NNHC(O)OR * , =NNHS(O)2R * , =NR * , =NOR * , -O(C(R * 2)) 2-3 O-, or -S(C(R * 2)) 2-3 S-. Wherein each independent occurrence of R* is hydrogen, a C 1-6 aliphatic group which may be substituted as defined below, and an unsubstituted 5- to 6-membered saturated, partially unsaturated, or aryl ring having from 0 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur. Suitable divalent substituents bonded to the adjacent replaceable carbon of an "optionally substituted" group include -O(CR * 2) 2-3 O-, wherein each independent occurrence of R* is hydrogen, a C 1-6It is selected from aliphatic groups and unsubstituted 5- to 6-membered saturated, partially unsaturated, and aryl rings having 0 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

[0083] Suitable substituents on the aliphatic group of R* are independently halogen, -R ● , -(haloR ● ), -OH, -OR ● , -O(haloR ● ), -CN, -C(O)OH, -C(O)OR ● , -NH2, -NHR ● , -NR ● 2, or -NO2, where each R ● is unsubstituted or, if preceded by "halo", is substituted only by one or more halogens and is independently a C 1-4 aliphatic group, -CH2Ph, -O(CH2) 0-1 Ph, or a 5- to 6-membered saturated, partially unsaturated, or aryl ring having 0 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

[0084] In some embodiments, suitable substituents on substitutable nitrogen are independently -R†, -NR†2, -C(O)R†, -C(O)OR†, -C(O)C(O)R†, -C(O)CH2C(O)R†, -S(O)2R†, -S(O)2NR†2, -C(S)NR†2, -C(NH)NR†2, or -N(R†)S(O)2R†. Here, each R† is independently hydrogen, a C 1-6 aliphatic group that may be substituted as defined below, unsubstituted -OPh, or an unsubstituted 5- to 6-membered saturated, partially unsaturated, or aryl ring having 0 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or, regardless of the above definition, two independent R†s together with their intervening atoms form an unsubstituted 3- to 12-membered saturated, partially unsaturated, or aryl monocyclic or bicyclic ring having 0 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

[0085] Suitable substituents on the aliphatic group of R† are, independently, halogen, -R ● , -(haloR ● ), -OH, -OR ● , -O(haloR ● ), -CN, -C(O)OH, -C(O)OR ● , -NH2, -NHR ● , -NR ● 2, or -NO2, where each R ● is unsubstituted or, when "halo" precedes, is substituted with only one or more halogens and is independently a C 1-4 aliphatic group, -CH2Ph, -O(CH2) 0-1 Ph, or a 5- to 6-membered saturated, partially unsaturated, or aryl ring having from 0 to 4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

[0086] Partially unsaturated: As used herein, the term "partially unsaturated" refers to a ring moiety that contains at least one double or triple bond. The term "partially unsaturated" is intended to encompass rings having multiple sites of unsaturation, but is not intended to include aryl or heteroaryl moieties as defined herein.

[0087] Pharmaceutical Composition: As used herein, the term "pharmaceutical composition" refers to an active agent formulated with one or more pharmaceutically acceptable carriers. In some embodiments, the active agent is present in unit doses suitable for administration in a treatment regimen that exhibits a statistically significant probability of achieving a predetermined therapeutic effect when administered to the relevant population. In some embodiments, the pharmaceutical composition can be specially formulated for administration in solid or liquid form suitable for the following uses: oral administration, e.g., drenches (aqueous or non-aqueous solutions or suspensions), tablets, e.g., buccal, sublingual, and tablets for systemic absorption, boluses, powders, granules, pastes for application to the tongue. Parenteral administration, e.g., by subcutaneous, intramuscular, intravenous, or epidural injection, e.g., as a sterile solution or suspension, or as a sustained release formulation, topical application, e.g., as a cream, ointment, or controlled release patch or spray applied to the skin, lung, or oral cavity, vaginal or rectal administration, e.g., as a pessary, cream, or foam, sublingual, intraocular, transdermal, or nasal, pulmonary, and other mucosal surface administration.

[0088] Pharmaceutically Acceptable: As used herein, the phrase "pharmaceutically acceptable" refers to compounds, materials, compositions and / or dosage forms suitable for use in contact with human and animal tissue within the scope of sound medical judgment, without undue toxicity, irritation, allergic reaction, or other problems or complications, and commensurate with a reasonable benefit / risk ratio.

[0089] Pharmaceutically Acceptable Carrier: As used herein, the term "pharmaceutically acceptable carrier" means a pharmaceutically acceptable material, composition or medium such as a liquid or solid filler, diluent, excipient, or solvent encapsulating material involved in carrying or transporting a subject compound from one organ or part of the body to another. Each carrier must be "acceptable" in the sense of being compatible with the other ingredients of the formulation and not injurious to the patient. Examples of substances that can be used as pharmaceutically acceptable carriers include saccharides such as lactose, glucose, sucrose, etc. used in pharmaceutical formulations, starches such as corn starch, potato starch, etc., celluloses and their derivatives such as sodium carboxymethyl cellulose, ethyl cellulose, cellulose acetate, etc., excipients such as powdered tragacanth, malt, gelatin, talc, cocoa butter, suppository wax, etc., oils such as peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil, soybean oil, etc., glycols such as propylene glycol, polyols such as glycerin, sorbitol, mannitol, polyethylene glycol, etc., esters such as ethyl oleate, ethyl laurate, etc., buffers such as agar, magnesium hydroxide, aluminum hydroxide, etc., alginic acid, pyrogen-free water, isotonic saline, Ringer's solution, ethyl alcohol, pH buffer solutions, polyesters, polycarbonates and / or polyanhydrides, and other non-toxic compatible substances.

[0090] Pharmaceutically acceptable salts: As used herein, the term "pharmaceutically acceptable salts" refers to salts of compounds suitable for use in pharmaceutical situations, i.e., salts suitable for contact with tissues of humans and lower animals without undue toxicity, irritation, allergic response, etc. within the scope of sound medical judgment, and salts with a reasonable benefit / risk ratio. Pharmaceutically acceptable salts are well known in the art. For example, S.M. Berge et al. describe pharmaceutically acceptable salts in detail in J. Pharmaceutical Sciences, 66:1-19 (1977). In some embodiments, pharmaceutically acceptable salts include, but are not limited to, non-toxic acid addition salts. Non-toxic acid addition salts are salts of amino groups formed with inorganic acids such as hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid, perchloric acid, or organic acids such as acetic acid, maleic acid, tartaric acid, citric acid. Using succinic acid or malonic acid, or other methods used in the art such as ion exchange. In some embodiments, pharmaceutically acceptable salts include, but are not limited to, adipate, alginate, ascorbate, aspartate, benzenesulfonate, benzoate, bisulfate, borate, butyrate, camphorate, camphorsulfonate, citrate, cyclopentanepropionate, digluconate, dodecyl sulfate, ethanesulfonate, formic acid, fumaric acid, glucoheptonic acid, glycerophosphate, gluconate, hemisulfate, heptanoate, hexanoate, hydroiodic acid, 2-hydroxy-ethanesulfonate, lactobionate, lactic acid, lauric acid, lauryl sulfate, malic acid, maleic acid, malonic acid, methanesulfonate, 2-naphthalenesulfonate, nicotinic acid, nitric acid, oleic acid, oxalic acid, palmitic acid, pamoate, pectinate, persulfate, 3-phenylpropionate, phosphoric acid, picric acid, pivalate, propionate, stearic acid, succinate, sulfate, tartrate, thiocyanate, p-toluenesulfonate, undecanoate, valerate, etc. In some embodiments, the provided compounds contain one or more acidic groups, and the pharmaceutically acceptable salts are salts of alkali, alkaline earth metals, or ammonium (e.g., ammonium salts of N(R)3, where each R is independently defined and as described in this disclosure).Representative alkali or alkaline earth metal salts include sodium, lithium, potassium, calcium, magnesium, and the like. In some embodiments, the pharmaceutically acceptable salt is a sodium salt. In some embodiments, the pharmaceutically acceptable salt is a potassium salt. In some embodiments, the pharmaceutically acceptable salt is a calcium salt. In some embodiments, the pharmaceutically acceptable salt, where appropriate, is formed using counterions such as halides, hydroxides, carboxylates, sulfates, phosphates, nitrates, C1-C6 alkyls, sulfonates, and arylsulfonates, and includes non-toxic ammonium, quaternary ammonium, and amine cations. In some embodiments, the provided compound contains two or more acid groups. In some embodiments, the pharmaceutically acceptable salts of such compounds, or generally salts, contain two or more cations that can be the same or different. In some embodiments, in the pharmaceutically acceptable salt (or generally the salt), all ionizable hydrogens in the acidic group (e.g., in an aqueous solution with a pKa of about 11, 10, 9, 8, 7, 6, 5, 4, 3, or 2 or less; in some embodiments, about 7 or less. In some embodiments, about 6 or less. In some embodiments, about 5 or less. In some embodiments, about 4 or less. In some embodiments, about 3 or less in the acidic group) are replaced by cations.

[0091] Polypeptide: As used herein, refers to a polymer chain of amino acids. In some embodiments, the polypeptide has an amino acid sequence that occurs in nature. In some embodiments, the polypeptide has an amino acid sequence that does not occur in nature. In some embodiments, the polypeptide has an artificially created amino acid sequence in that it is designed and / or produced by an act of human hand. In some embodiments, the polypeptide can comprise or be composed of natural amino acids, non-natural amino acids, or both. In some embodiments, the polypeptide can comprise or be composed of only natural amino acids or only non-natural amino acids. In some embodiments, the polypeptide can comprise D-amino acids, L-amino acids, or both. In some embodiments, the polypeptide can comprise only D-amino acids. In some embodiments, the polypeptide can comprise only L-amino acids. In some embodiments, the polypeptide can comprise one or more pendant groups or other modifications, such as modifications or attachments of one or more amino acid side chains at the N-terminus of the polypeptide, the C-terminus of the polypeptide, or any combination thereof. In some embodiments, such pendant groups or modifications can be selected from the group consisting of acetylation, amidation, lipidation, methylation, pegylation, etc., including combinations thereof. In some embodiments, the polypeptide is cyclic and / or can contain a cyclic moiety. In some embodiments, the polypeptide is not cyclic and / or does not contain a cyclic moiety. In some embodiments, the polypeptide is linear. In some embodiments, the polypeptide is a stapled polypeptide or can contain a stapled polypeptide. In some embodiments, the term "polypeptide" may be appended with the name of a reference polypeptide, activity, or structure. In such cases, it is used herein to refer to polypeptides that share the relevant activity or structure and are thus considered members of the same class or family of polypeptides.For each such class, this specification provides exemplary polypeptides within the class whose amino acid sequences and / or functions are known and / or would be known to one of ordinary skill in the art. In some embodiments, such exemplary polypeptides are reference polypeptides of a polypeptide class or family. In some embodiments, members of a polypeptide class or family exhibit significant sequence homology or identity with the reference polypeptide of that class (and in some embodiments, with all polypeptides within the class), share common sequence motifs (e.g., characteristic sequence elements), and / or share common activities (at equivalent levels or within a specified range). For example, in some embodiments, a member polypeptide exhibits a degree of sequence homology or identity with the reference polypeptide overall (at least about 30-40%, and often more than about 50%, 60%, 70%, 80%, 90%, 91%, 92%, 93%, 94%, 95%, 96%, 97%, 98%, 99% or more), and / or includes at least one region (e.g., a conserved region that is a characteristic sequence element in some embodiments or that includes a characteristic sequence element) that exhibits a very high degree of sequence identity (often more than 90% or 95%, 96%, 97%, 98%, or 99%). Such conserved regions typically include at least 3-4, and often up to 20 or more, amino acids. In some embodiments, the conserved region encompasses at least one range of at least 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 or more contiguous amino acids. In some embodiments, related polypeptides can include or be composed of fragments of a parent polypeptide. In some embodiments, useful polypeptides can include or be composed of multiple fragments. Each fragment is found in a spatial arrangement different from that found in the polypeptide of interest in the same parent polypeptide (e.g., fragments that are directly linked in the parent can be spatially separated in the polypeptide of interest or vice versa, and / or the fragments can be present in the polypeptide of interest in an order different from that in the parent).Therefore, the target polypeptide is a derivative of its parent polypeptide.

[0092] Protecting Group: As used herein, the term "protecting group" is well-known in the art and includes those described in detail in T. W. Greene and P. G. M. Wuts, "Protecting Groups in Organic Synthesis", 3rd Edition, John Wiley & Sons, 1999, the entire text of which is incorporated herein by reference. Also included are protecting groups particularly adapted for nucleoside and nucleotide chemistry as described in Current Protocols in Nucleic Acid Chemistry, edited by Serge L. Beaucage et al., June 2012, the entire text of Chapter 2 of which is incorporated herein by reference. Suitable amino protecting groups include methyl carbamate, ethyl carbamate, 9-fluorenylmethyl carbamate (Fmoc), 9-(2-sulfo)fluorenylmethyl carbamate, 9-(2,7-dibromo)fluorenylmethyl carbamate, 2,7-di-t-butyl-[9-(10,10-dioxo-10,10,10,10-tetrahydrothioxanthyl)]methyl carbamate (DBD-Tmoc), 4-methoxyphenacyl carbamate (Phenoc), 2,2,2-trichloroethyl carbamate (Troc), 2-trimethylsilylethyl carbamate (Teoc), 2-phenylethyl carbamate (hZ), 1-(1-adamantyl)-1-methylethyl carbamate (Adpoc), 1,1-dimethyl-2-haloethyl carbamate, etc. 1,1-dimethyl-2,2-dibromoethyl carbamate (DB-t-BOC), 1,1-dimethyl-2,2,2-trichloroethyl carbamate (TCBOC), 1-methyl-1-(4-biphenylyl)ethyl carbamate (Bpoc), 1-(3,5-di-t-butylphenyl)-1-methylethyl carbamate (t-Bumeoc), 2-(2'- and 4'-pyridyl)ethyl carbamate (Pyoc), 2-(N,N-dicyclohexylcarboxamide)ethylcarbamate, t-butylcarbamate (BOC), 1-adamantylcarbamate (Adoc), vinylcarbamate (Voc), allylcarbamate (Alloc), 1-isopropylallylcarbamate (Ipaoc), cinnamylcarbamate (Coc), 4-nitrocinnamylcarbamate (Noc), 8-quinolylcarbamate, N-hydroxypiperidinylcarbamate, alkyldithiocarbamate, benzylcarbamate (Cbz), p-methoxybenzylcarbamate (Moz), p-nitrobenzylcarbamate, p-bromobenzylcarbamate, p-chlorobenzylcarbamate, 2,4-dichlorobenzylcarbamate, 4-methylsulfinylbenzylcarbamate (Msz), 9-anthrylmethylcarbamate, diphenylmethylcarbamate, 2-methylthioethylcarbamate, 2-methylsulfonylethylcarbamate, 2-(p-toluenesulfonyl)ethylcarbamate, [2-(1,3-dithianyl)]methylcarbamate (Dmoc), 4-methylthiophenylcarbamate (Mtpc), 2,4-dimethylthiophenylcarbamate (Bmpc), 2-phosphonioethylcarbamate (Peoc), 2-triphenylphosphonioisopropylcarbamate (Ppoc), 1,1-dimethyl-2-cyanoethylcarbamate, m-chloro-p-acetyloxybenzylcarbamate, p-(dihydroxyboryl)benzylcarbamate, 5-benzisoxazolylmethylcarbamate, 2-(trifluoromethyl)-6-chromonylmethylcarbamate (Tcroc), m-nitrophenylcarbamate, 3,5-dimethoxybenzylcarbamate, o-nitrobenzylcarbamate, 3,4-dimethoxy-6-nitrobenzylcarbamate, phenyl(o-nitrophenyl)methylcarbamate, phenothiazinyl-(10)-carbonyl derivative, N'-p-toluenesulfonylaminocarbonyl derivative, N'-phenylaminothiocarbonyl derivative, t-amylcarbamate, S-benzylthiocarbamate, p-cyanobenzylcarbamate, cyclobutylcarbamate, cyclohexylcarbamate, cyclopentylcarbamate, cyclopropylmethylcarbamate, p-decyloxybenzylcarbamate, 2,2-Dimethoxycarbonylvinyl carbamate, o-(N,N-dimethylcarboxamido)benzyl carbamate, 1,1-dimethyl-3-(N,N-dimethylcarboxamido)propyl carbamate, 1,1-dimethylpropynyl carbamate, di(2-pyridyl)methyl carbamate, 2-furanylmethyl carbamate, 2-iodoethyl carbamate, isobornyl carbamate, isobutyl carbamate, isonicotinyl carbamate, p-(p'-methoxyphenylazo)benzyl carbamate, 1-methylcyclobutyl carbamate, 1-methylcyclohexyl carbamate, 1-methyl-1-cyclopropylmethyl carbamate, 1-methyl-1-(3,5-dimethoxyphenyl)ethyl carbamate, 1-methyl-1-(p-phenylazophenyl)ethyl carbamate, 1-methyl-1-phenylethyl carbamate, 1-methyl-1-(4-pyridyl)ethyl carbamate, phenyl carbamate, p-(phenylazo)benzyl carbamate, 2,4,6-tri-t-butylphenyl carbamate, 4-(trimethylammonium)benzyl carbamate, 2,4,6-trimethylbenzyl carbamate, formamide, acetamide, chloroacetamide, trichloroacetamide, trifluoroacetamide, phenylacetamide, 3-phenylpropanamide, picolinamide, 3-pyridylcarboxamide, N-benzoylphenylalanyl derivative, benzamide, p-phenylbenzamide, o-nitrophenylacetamide, o-nitrophenoxyacetamide, acetoacetamide, (N'-dithiobenzyl oxycarbonylamino)acetamide, 3-(p-hydroxyphenyl)propanamide, 3-(o-nitrophenyl)propanamide, 2-methyl-2-(o-nitrophenoxy)propanamide, 2-methyl-2-(o-phenylazophenoxy)propanamide, 4-chlorobutanamide, 3-methyl-3-nitrobutanamide, o-nitrosinamide, N-acetylmethionine derivative, o-nitrobenzamide, o-(benzoyloxymethyl)benzamide, 4,5-diphenyl-3-oxazolin-2-one, N-phthalimide, N-dithiasuccinimide (Dts), N-2,3-diphenylmaleimide, N-2,5-dimethylpyrrole, N-1,1,4,4-Tetramethyldisilylazacyclopentane adduct (STABASE), 5-substituted 1,3-dimethyl-1,3,5-triazacyclohexan-2-one, 5-substituted 1,3-dibenzyl-1,3,5-triazacyclohexan-2-one, 1-substituted 3,5-dinitropyridone, N-methylamine, N-allylamine, N-[2-(trimethylsilyl)ethoxy]methylamine (SEM), N-3-acetoxypropylamine, N-(1-isopropyl-4-nitro-2-oxo-3-pyrrolin-3-yl)amine, quaternary ammonium salt, N-benzylamine, N-di(4-methoxyphenyl)methylamine, N-5-dibenzosuberlylamine, N-triphenylmethylamine (Tr), N-[(4-methoxyphenyl)diphenylmethyl]amine (MMTr), N-9-phenylfluorenylmethylamine (PhF), N-2,7-dichloro-9-fluorenylmethyleneamine, N-ferrocenylmethylamino (Fcm), N-2-picolylamino N'-oxide, N-1,1-dimethylthiomethyleneamine, N-benzylideneamine, N-p-methoxybenzylideneamine, N-diphenylmethyleneamine, N-[(2-pyridyl)mesityl]methyleneamine, N-(N',N'-dimethylaminomethylene)amine, N,N'-isopropylidenediamine, N-p-nitrobenzylideneamine, N-salicylideneamine, N-5-chlorosalicylideneamine, N-(5-chloro-2-hydroxyphenyl)phenylmethyleneamine, N-cyclohexylideneamine, N-(5,5-dimethyl-3-oxo-1-cyclohexenyl)amine, N-borane derivative, N-diphenylborate derivative, N-[phenyl(pentacarbonylchromium or tungsten)carbonyl]amine, N-copper chelate, N-zinc chelate, N-nitroamine, N-nitrosoamine, amine N-oxide, diphenylphosphinamido (Dpp), dimethylthiophosphinamido (Mpt), diphenylthiophosphinamido (Ppt), dialkyl phosphoramidate, dibenzyl phosphoramidate, diphenyl phosphoramidate, benzenesulfenamide, o-nitrobenzenesulfenamide (Nps), 2,4-Dinitrobenzenesulfenamide, pentachlorobenzenesulfenamide, 2-nitro-4-methoxybenzenesulfenamide, triphenylmethylsulfenamide, 3-nitropyridinesulfenamide (Npys), p-toluenesulfonamide (Ts), benzenesulfonamide, 2,3,6-trimethyl-4-methoxybenzenesulfonamide (Mtr), 2,4,6-trimethoxybenzenesulfonamide (Mtb), 2,6-dimethyl-4-methoxybenzenesulfonamide (Pme), 2,3,5,6-tetramethyl-4-methoxybenzenesulfonamide (Mte), 4-methoxybenzenesulfonamide (Mbs), 2,4,6-trimethylbenzenesulfonamide (Mts), 2,6-dimethoxy-4-methylbenzenesulfonamide (iMds), 2,2,5,7,8-pentamethylchroman-6-sulfonamide (Pmc), methanesulfonamide (Ms), β-trimethylsilylethanesulfonamide (SES), 9-anthracenesulfonamide, 4-(4’,8’-dimethoxynaphthylmethyl)benzenesulfonamide (DNMBS), benzylsulfonamide, trifluoromethylsulfonamide, and phenacylsulfonamide are included.,

[0093] Suitably protected carboxylic acids further include, but are not limited to, carboxylic acids protected with silyl, alkyl, alkenyl, aryl, and arylalkyl groups. Examples of suitable silyl groups include trimethylsilyl, triethylsilyl, t-butyldimethylsilyl, t-butyldiphenylsilyl, triisopropylsilyl, and the like. Examples of suitable alkyl groups include methyl, benzyl, p-methoxybenzyl, 3,4-dimethoxybenzyl, trityl, t-butyl, tetrahydropyran-2-yl, and the like. Examples of suitable alkenyl groups include allyl. Examples of suitable aryl groups include optionally substituted phenyl, biphenyl, or naphthyl. Examples of suitable arylalkyl groups include optionally substituted benzyl (e.g., p-methoxybenzyl (MPM), 3,4-dimethoxybenzyl, O-nitrobenzyl, p-nitrobenzyl, p-halobenzyl, 2,6-dichlorobenzyl, p-cyanobenzyl), and 2- and 4-picolyl.

[0094] Suitable hydroxyl protecting groups include methyl, methoxymethyl (MOM), methylthiomethyl (MTM), t-butylthiomethyl, (phenyldimethylsilyl)methoxymethyl (SMOM), benzyloxymethyl (BOM), p-methoxybenzyloxymethyl (PMBM), (4-methoxyphenoxy)methyl (p-AOM), guaiacolmethyl (GUM), t-butoxymethyl, 4-pentenyl oxymethyl (POM), siloxymethyl, 2-methoxyethoxymethyl (MEM), 2,2,2-trichloroethoxymethyl, bis(2-chloroethoxy)methyl, 2-(trimethylsilyl)ethoxymethyl (SEMOR), tetrahydropyranyl (THP), 3-bromotetrahydropyranyl, tetrahydrothiopyranyl, 1-methoxycyclohexyl, 4-methoxytetrahydropyranyl (MTHP), 4-methoxytetrahydrothiopyranyl, 4-methoxytetrahydrothiopyranyl S,S-dioxide, 1-[(2-chloro-4-methyl)phenyl]-4-methoxypiperidin-4-yl (CTMP), 1,4-dioxan-2-yl, tetrahydrofuranyl, tetrahydrothiofuranyl, 2,3,3a,4,5,6,7,7a-octahydro-7,8,8-trimethyl-4,7-methanobenzofuran-2-yl, 1-ethoxyethyl, 1-(2-chloroethoxy)ethyl, 1-methyl-1-methoxyethyl, 1-methyl-1-benzyloxyethyl, 1-methyl-1-benzyloxy-2-fluoroethyl, 2,2,2-trichloroethyl, 2-trimethylsilylethyl, 2-(phenylselenyl)ethyl, t-butyl, allyl, p-chlorophenyl, p-methoxyphenyl, 2,4-dinitrophenyl, benzyl, p-methoxybenzyl, 3,4-dimethoxybenzyl, o-nitrobenzyl, p-nitrobenzyl, p-halobenzyl, 2,6-dichlorobenzyl, p-cyanobenzyl, p-phenylbenzyl, 2-picolyl, 4-picolyl, 3-methyl-2-picolyl N-oxide, diphenylmethyl, p,p'-dinitrobenzhydryl, 5-dibenzosuberyl, triphenylmethyl, α-naphthyldiphenylmethyl, p-methoxyphenyldiphenylmethyl, di(p-methoxyphenyl)phenylmethyl, tri(p-methoxyphenyl)methyl, 4-(4'-bromophenacyloxyphenyl)diphenylmethyl, 4,4',4''-tris(4,5-dichlorophthalimidophenyl)methyl, 4,4',4''-tris(levulinoyloxyphenyl)methyl, 4,4',4''-tris(benzoyloxyphenyl)methyl, 3-(imidazol-1-yl)bis(4',4''-dimethoxyphenyl)methyl, 1,1-bis(4-methoxyphenyl)-1'-pyrenylmethyl, 9-anthryl, 9-(9-phenyl)xanthenyl, 9-(9-phenyl-10-oxo)anthryl, 1,3-benzodithiolan-2-yl, benzisothiazolyl S,S-dioxide, trimethylsilyl (TMS), triethylsilyl (TES), triisopropylsilyl (TIPS), dimethylisopropylsilyl (IPDMS), diethylisopropylsilyl (DEIPS), dimethyltexylsilyl, t-butyldimethylsilyl (TBDMS), t-butyldiphenylsilyl (TBDPS), tribenzylsilyl, tri-p-xylylsilyl, triphenylsilyl, diphenylmethylsilyl (DPMS), t-butylmethoxyphenylsilyl (TBMPS), formate, benzoylformate, acetate, chloroacetate, dichloroacetate, trichloroacetate, trifluoroacetate, methoxyacetate, triphenylmethoxyacetate, phenoxyacetate, p-chlorophenoxyacetate, 3-phenylpropionate, 4-oxopentanoate (levulinic acid), 4,4-(ethylenedithio)pentanoate (levulinoyldithioacetal), pivaloate, adamantoate, crotonate, 4-methoxycrotonate, benzoate, p-phenylbenzoate, 2,4,6-trimethylbenzoate (mesitoic acid), alkyl methyl carbonate, 9-fluorenylmethyl carbonate (Fmoc), alkyl ethyl carbonate, alkyl 2,2,2-Trichloroethyl carbonate (Troc), 2-(Trimethylsilyl)ethyl carbonate (TMSEC), 2-(Phenylsulfonyl)ethyl carbonate (Psec), 2-(Triphenylphosphonio)ethyl carbonate (Peoc), alkyl isobutyl carbonate, alkyl vinyl carbonate, alkyl allyl carbonate, alkyl p-nitrophenyl carbonate, alkyl benzyl carbonate, alkyl p-methoxybenzyl carbonate, alkyl 3,4-dimethoxybenzyl carbonate, alkyl o-nitrobenzyl carbonate, alkyl p-nitrobenzyl carbonate, alkyl S-benzyl thiocarbonate, 4-Ethoxy-1-naphthyl carbonate, methyl dithiocarbonate, 2-Iodobenzoate, 4-Azidobutanoic acid, 4-Nitro-4-methylpentanoate, o-(Dibromomethyl)benzoate, 2-Formylbenzenesulfonic acid, 2-(Methylthiomethoxy)ethyl, 4-(Methylthiomethoxy)butyric acid, 2-(Methylthiomethoxymethyl)benzoate, 2,6-Dichloro-4-methylphenoxyacetic acid, 2,6-Dichloro-4-(1,1,3,3-tetramethylbutyl)phenoxyacetate, 2,4-Bis(1,1-dimethylpropyl)phenoxyacetate, chlorodiphenylacetate, isobutyric acid, monosuccinic acid, (E)-2-Methyl-2-butenoic acid, o-(Methoxycarbonyl)benzoic acid, α-Naphthoic acid, nitric acid, alkyl N,N,N’,N’-tetramethylphosphorodiamidate, alkyl N-phenylcarbamate, boric acid, dimethylphosphinothioyl, alkyl 2,4-dinitrophenyl sulfenate, sulfuric acid, methanesulfonic acid (mesylic acid), benzylsulfonic acid, and tosyl acid (Ts) are included. Protecting groups for protecting 1,2- or 1,3-diols include methylene acetal, ethylidene acetal, 1-t-butylethylidene ketal, 1-phenylethylidene ketal, (4-methoxyphenyl)ethylidene acetal, 2,2,2-trichloroethylidene acetal, acetonide, cyclopentylidene ketal, cyclohexylidene ketal, cycloheptylidene ketal, benzylidene acetal, p-methoxybenzylidene acetal, 2,4-dimethoxybenzylidene ketal, 3,4-Dimethoxybenzylidene acetal, 2-nitrobenzylidene acetal, methoxymethylene acetal, ethoxymethylene acetal, dimethoxymethylene orthoester, 1-methoxyethylidene orthoester, 1-ethoxyethylidine orthoester, 1,2-dimethoxyethylidene orthoester, α-methoxybenzylidene orthoester, 1-(N,N-dimethylamino)ethylidene derivative, α-(N,N'-dimethylamino)benzylidene derivative, 2-oxacyclopentylidene orthoester, di-t-butylsilylene group (DTBS), 1,3-(1,1,3,3-tetraisopropyldisiloxanilidene) derivative (TIPDS), tetra-t-butoxydisiloxane-1,3-diylidene derivative (TBDS), cyclic carbonate, cyclic boronate, ethyl boronate, and phenyl boronate are included.,

[0095] In some embodiments, the hydroxyl protecting group is acetyl, t-butyl, t-butoxymethyl, methoxymethyl, tetrahydropyranyl, 1-ethoxyethyl, 1-(2-chloroethoxy)ethyl, 2-trimethylsilylethyl, p-chlorophenyl, 2,4-dinitrophenyl, benzyl, benzoyl, p-phenylbenzoyl, 2,6-dichlorobenzyl, diphenylmethyl, p-nitrobenzyl, triphenylmethyl (trityl), 4,4'-dimethoxytrityl, trimethylsilyl, triethylsilyl, t-butyldimethylsilyl, t-butyldiphenylsilyl, triphenylsilyl, triisopropylsilyl, benzoylformate, chloroacetyl, trichloroacetyl, trifluoroacetyl, pivaloyl, 9-fluorenylmethyl carbonate, mesylate, tosylate, triflate, trityl, monomethoxytrityl (MMTr), 4,4'-dimethoxytrityl, (DMTr), 4,4',4''-trimethoxytrityl (TMTr), 2-cyanoethyl (CE or Cne), 2-(trimethylsilyl)ethyl (TSE), 2-(2-nitrophenyl)ethyl, 2-(4-cyanophenyl)ethyl 2-(4-nitrophenyl)ethyl (NPE), 2-(4-nitrophenylsulfonyl)ethyl, 3,5-dichlorophenyl, 2,4-dimethylphenyl, 2-nitrophenyl, 4-nitrophenyl, 2,4,6-trimethylphenyl, 2-(2-nitrophenyl)ethyl, butylthiocarbonyl, 4,4',4''-tris(benzoyloxy)trityl, diphenylcarbamoyl, levulinyl, 2-(dibromomethyl)benzoyl (Dbmb), 2-(isopropylthiomethoxymethyl)benzoyl (Ptmt), 9-phenylxanthen-9-yl (pixyl), or 9-(p-methoxyphenyl)xanthen-9-yl (MOX). In some embodiments, each hydroxyl protecting group is independently selected from acetyl, benzyl, t-butyldimethylsilyl, t-butyldiphenylsilyl, and 4,4'-dimethoxytrityl. In some embodiments, the hydroxyl protecting group is selected from the group consisting of trityl, monomethoxytrityl, and 4,4'-dimethoxytrityl groups. In some embodiments, the protecting group is attached to the sulfur atom of the phosphorothioate group.In some embodiments, the protecting group is attached to the oxygen atom of the internucleotide phosphorothioate bond. In some embodiments, the protecting group is attached to the oxygen atom of the internucleotide phosphate bond. In some embodiments, the protecting group is 2-cyanoethyl (CE or Cne), 2-trimethylsilylethyl, 2-nitroethyl, 2-sulfonylethyl, methyl, benzyl, o-nitrobenzyl, 2-(p-nitrophenyl)ethyl (NPE or Npe), 2-phenylethyl, 3-(N-tert-butylcarboxamido)-1-propyl, 4-oxopentyl, 4-methylthio-1-butyl, 2-cyano-1,1-dimethylethyl, 4-N-methylaminobutyl, 3-(2-pyridyl)-1-propyl, 2-[N-methyl-N-(2-pyridyl)]aminoethyl, 2-(N-formyl, N-methyl)aminoethyl, or 4-[N-methyl-N-(2,2,2-trifluoroacetyl)amino]butyl.

[0096] Subject: As used herein, the term "subject" or "test subject" refers to any organism to which a compound or composition is administered according to the present disclosure, for example for experimental, diagnostic, prophylactic and / or therapeutic purposes. Typical subjects include animals (such as mammals such as mice, rats, rabbits, non-human primates, and humans, insects, worms, etc.) and plants. In some embodiments, the subject is a human. In some embodiments, the subject has and / or is likely to have a disease, disorder and / or condition.

[0097] Prone to contracting: An individual who is "prone to contracting" a disease, disorder, and / or condition is an individual who has a higher risk of developing the disease, disorder, and / or condition than a member of the general population. In some embodiments, an individual who is prone to contracting a disease, disorder, and / or condition has a tendency to develop that disease, disorder, and / or condition. In some embodiments, an individual who is susceptible to a disease, disorder, and / or medical condition may not be diagnosed with that disease, disorder, and / or medical condition. In some embodiments, an individual who is susceptible to a disease, disorder, and / or medical condition may exhibit symptoms of that disease, disorder, and / or medical condition. In some embodiments, an individual who is susceptible to a disease, disorder, and / or medical condition may not exhibit symptoms of that disease, disorder, and / or medical condition. In some embodiments, an individual who is susceptible to a disease, disorder, and / or medical condition develops that disease, disorder, and / or medical condition. In some embodiments, an individual who is susceptible to a disease, disorder, and / or medical condition does not develop that disease, disorder, and / or medical condition.

[0098] Therapeutic agent: As used herein, the term "therapeutic agent" generally refers to any agent that, when administered to a subject, induces a desired effect (e.g., a desired biological, clinical, or pharmacological effect). In some embodiments, an agent is considered a therapeutic agent if it exhibits a statistically significant effect across an appropriate population. In some embodiments, an appropriate population is a population of subjects who have and / or are susceptible to a disease, disorder, or condition. In some embodiments, an appropriate population is a population of model organisms. In some embodiments, an appropriate population can be defined by one or more criteria such as age group, gender, genetic background, existing clinical condition, previous exposure to treatment, etc. In some embodiments, a therapeutic agent is a substance that, when administered to a subject in an effective amount, alleviates, ameliorates, relieves, suppresses, prevents, delays onset, reduces severity, and / or reduces incidence of one or more symptoms or features of the subject's disease, disorder, and / or condition. In some embodiments, a "therapeutic agent" is an agent that has received or requires approval by a government agency before being sold for administration to humans. In some embodiments, a "therapeutic agent" is an agent that requires a physician's prescription for administration to humans. In some embodiments, a therapeutic agent is a provided compound.

[0099] Therapeutically effective amount: As used herein, the term "therapeutically effective amount" means the amount of a substance (e.g., a therapeutic agent, composition, and / or formulation) that, when administered as part of a treatment regimen, causes a desired biological response. In some embodiments, a therapeutically effective amount of a substance is an amount sufficient to treat, diagnose, prevent, and / or delay the onset of a disease, disorder, and / or condition when administered to a subject afflicted with or susceptible to the disease, disorder, and / or condition. As will be appreciated by those skilled in the art, the effective amount of a substance can vary depending on factors such as the desired biological endpoint, the substance being delivered, the target cell or tissue, etc. For example, the effective amount of a compound in a formulation for treating a disease, disorder, and / or condition is an amount that contributes to reducing, ameliorating, alleviating, suppressing, preventing, delaying the onset of, reducing the severity of, and / or reducing the incidence of one or more symptoms or characteristics of the disease, disorder, and / or condition. In some embodiments, the therapeutically effective amount is administered as a single dose. In some embodiments, multiple unit doses are required to deliver the therapeutically effective amount.

[0100] Treatment: As used herein, the terms "treating," "treatment," or "being treated" refer to any method used to partially or completely alleviate, ameliorate, reduce, suppress, prevent, delay the onset of, reduce the severity of, and / or reduce the incidence of one or more symptoms or characteristics of a disease, disorder, and / or condition. Treatment may be administered to a subject who does not exhibit signs of a disease, disorder, and / or condition. In some embodiments, treatment may be administered to a subject who exhibits only the initial signs of a disease, disorder, and / or condition for the purpose of reducing the risk of developing a medical condition associated with the disease, disorder, and / or condition.

[0101] Unsaturated: As used herein, the term "unsaturated" means that the moiety has one or more unsaturated units.

[0102] As will be appreciated by those skilled in the art, the methods and compositions relating to the compounds described herein generally apply to tautomers, pharmaceutically acceptable salts, solvates, etc. of such compounds. In some embodiments, the compound may be provided as a tautomer, a salt, a solvate, or a combination thereof (e.g., a solvate of a salt). Description of specific embodiments

[0103] In particular, the present disclosure provides compounds and compositions, as well as methods thereof. In some embodiments, the present disclosure provides techniques useful for preventing or treating various conditions, disorders, or diseases. Specific embodiments of the techniques provided are described below by way of example. Specific embodiments of the compound

[0104] In particular, the present disclosure provides compounds containing an isourea moiety. In some embodiments, the isourea moiety is R as described herein w wherein T is O. In some embodiments, the present disclosure provides compounds containing an isothiourea moiety. In some embodiments, the isourea moiety is R as described herein w wherein T is S. In some embodiments, the present disclosure provides urea compounds. In some embodiments, the urea compound has the structure of H-R w or a tautomer thereof and / or a salt thereof, wherein T is O and each other variable is independently as described herein. In some embodiments, the present disclosure provides thiourea compounds. In some embodiments, the thiourea compound is H-R wor a tautomer and / or a salt thereof, wherein T is S and each other variable is independently as described herein. In some embodiments, the compound comprises or consists of two moieties, one of which is an isourea moiety or comprises an isourea moiety and the other is a moiety capable of providing, facilitating, or enhancing interaction with a target, such as a polypeptide. In some embodiments, the compound comprises or consists of two moieties, one of which is an isothiourea moiety or comprises an isothiourea moiety and the other is a moiety capable of providing, facilitating, or enhancing interaction with a target, such as a polypeptide. In some embodiments, the compound comprises or consists of two moieties, one of which is R w or -L w -R w or is R w or -L w -R w and the other is a moiety capable of providing, facilitating, or enhancing interaction with a target, such as a polypeptide. In some embodiments, the isourea and isothiourea moieties can be utilized as leaving groups attached to an electrophilic carbon atom in a warhead. In some embodiments, the -L w -R w described herein can be utilized as an electrophilic warhead. In some embodiments, such warheads can be utilized to replace various electrophilic warhead moieties in various compounds, such as -C(O)CH=CH2, -C(O)C≡CH, -C(O)CH2Cl, -C(O)CH2Br, -C(O)CH2I, etc., to provide compounds useful for multiple purposes, such as as inhibitors of various polypeptides (e.g., kinases, proteases, etc.).

[0105] In some embodiments, the isourea moiety is R w wherein R w is -T-C(=NR w1 )N(R w 2)(R w3) where T is -O-, and each other variable is independently as described herein. In some embodiments, the isothiourea moiety is R w where R w is -T-C(=NR w1 )N(R w2 )(R w3 ), where T is -S-, and each other variable is independently as described herein.

[0106] In some embodiments, the present disclosure provides compounds comprising R w as described herein. In some embodiments, the present disclosure provides compounds comprising -L w -R w where each variable is independently as described herein. In some embodiments, the present disclosure provides compounds comprising -C(O)-L w -R w where each variable is independently as described herein.

[0107] In some embodiments, R w is -O-C(=NR w1 )N(R w2 )(R w3 ) where each variable is independently as described herein. In some embodiments, R w is -S-C(=NR w1 )N(R w2 )(R w3 ) where each variable is independently as described herein.

[0108] Specific compounds are described below as examples. In some embodiments, the present disclosure provides a compound having the structure of Formula A or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of Formula B or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of Formula C or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of Formula D or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of Formula E or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of Formula F or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of Formula G or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of Formula H or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of [PAYLOAD]-R 4 or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of N(CN)(R w2 )(R w3 ), wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of R w1 -N=C=N-R w3 or a salt thereof, wherein each variable is independently as described herein. In some embodiments, the present disclosure provides a compound having the structure of T=C(NHR w1 )N(R w2 )(R w3 ) or a salt thereof, wherein each variable is independently as described herein.

[0109] Specific embodiments of various variables are described below by way of example. Those skilled in the art reading this disclosure will readily understand that embodiments of various variables can be combined according to this disclosure. Some combinations are described below by way of example. In some embodiments, embodiments of a variable (e.g., R) are described when describing embodiments of other variables (e.g., various embodiments of R are described when describing specific embodiments such as R 1 and R 2 ). Those skilled in the art reading this disclosure will readily understand that embodiments of a variable described when describing any one variable (e.g., the embodiments of R when describing R 1 ) can be applied to other variables that can be this variable (e.g., R 2 and R 3 that can be R, etc.). L w

[0110] In some embodiments, L w is a covalent bond or an optionally substituted divalent C 1-6 atom (e.g., C1, C2, C3, C4, C5 or C6) of an aliphatic or heteroaliphatic having 1 to 6 heteroatoms (e.g., 1, 2, 3, 4, 5, or 6 heteroatoms), and wherein one or more methylene units are optionally and independently -C(R')2-, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R')-, -C(O)S-, or -C(O)O-. In some embodiments, L w is a covalent bond or an optionally substituted divalent C 1-6is an aliphatic group, wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-. In some embodiments, Lw is a covalent bond or an optionally substituted divalent C 1-2 is an aliphatic group, wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-.

[0111] In some embodiments, as present in the various compounds exemplified herein, L w is an optionally substituted -CH2- bonded to R w or includes the same. In some embodiments, as present in the various compounds exemplified herein, L w is an optionally substituted -CH2-. In some embodiments, as present in the various compounds exemplified herein, L w is -CH2-. In some embodiments, L w is -CHD-. In some embodiments, L w is -CD2-. In some embodiments, L w is a monosubstituted -CH2-. In some embodiments, L wis a mono-substituted -CH2-. In some embodiments, such optionally substituted -CH2- is further activated by conjugation with an electron-withdrawing group, such as -C(O)-, to become more electrophilic. In some embodiments, the electron-withdrawing group is -C(O)- or includes it. In some embodiments, the electron-withdrawing group is -C(S)- or includes it. In some embodiments, L w is optionally substituted -C(O)-CH2- or includes it. In some embodiments, Lw is -C(O)-CH2-. In some embodiments, L w is optionally substituted -C(S)-CH2- or includes it. In some embodiments, Lw is -C(S)-CH2-. In some embodiments, the electron-withdrawing group is -C(N(R'))- or includes it. In some embodiments, the electron-withdrawing group is an optionally substituted aromatic ring or includes it. In some embodiments, the electron-withdrawing group is an optionally substituted heteroaromatic ring or includes it. In some embodiments, the electron-withdrawing group is L as described herein R In some embodiments, L w is -C(N(R'))-CH2-, -CH2- is optionally substituted, and R' is as described herein. In some embodiments, Lw is optionally substituted -C(O)-CHD-. In some embodiments, L w is optionally substituted -C(S)-CHD-. In some embodiments, L w is -C(N(R'))-CHD- and -CHD- is optionally substituted. In some embodiments, L w is optionally substituted -C(O)-CD2-. In some embodiments, L w is optionally substituted -C(S)-CD2-. In some embodiments, L w is -C(N(R'))-CD2- and -CD2- is optionally substituted. In some embodiments, -CH2-, -CHD-, or -CD2- is unsubstituted. In some embodiments, -CH2-, -CHD-, or -CD2- is Rw is attached to. In some embodiments, Lw is -CH(CH3)-. In some embodiments, L w is

[0112]

Chemical formula

[0113] is. In some embodiments, Lw is

[0114]

Chemical formula

[0115] is. R w

[0116] As described herein, R w is -T-C(=NR w1 ))N(R w2 )(R w3 ), and each variable is independently as described herein. In some embodiments, R w is -O-C(=NR w1 ))N(R w2 )(R w3 ), and each variable is independently as described herein. In some embodiments, R w is -S-C(=NR w1 ))N(R w2 )(R w3 ), and each variable is independently as described herein.

[0117] In some embodiments, R w1 , R w2 , and R w3 are each independently R as described herein. In some embodiments, at least one of R w1 , R w2 , and R w3w2 is -H. In some embodiments, R w1 , R w2 , and Rw3w2 One of them is -H. In some embodiments, R w1 , R w2 , and R w3w2 is one or less of -H. In some embodiments, R w1 is -H. In some embodiments, R w2 is -H. In some embodiments, R w3 is -H. In some embodiments, R w1 , R w2 , and R w3w2 are each not -H.

[0118] For example, in some embodiments, R w1 is -H, and R w2 and R w3 are each independently an optionally substituted C 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) aliphatic group, or together with the nitrogen to which they are attached, form an optionally substituted ring as described herein. In some embodiments, R w1 is -H, and R w2 and R w3 are each independently an optionally substituted C 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) aliphatic group, or together with the nitrogen to which they are attached, form an optionally substituted 3- to 10- (e.g., 3-7, 4-10, 5-10, 5-7, 3, 4, 5, 6, 7, 8, 9, or 10 etc.) membered ring having 0 to 3 (e.g., 0, 1-3, 1, 2, 3 etc.) heteroatoms in addition to the nitrogen atom. In some embodiments, R w1 is -H, and R w2 and R w3 are each independently an optionally substituted C1-10 aliphatic group. In some embodiments, Rw1 is -H, and R w2 and R w3 are each independently optionally substituted C1 - 10 alkyl. In some embodiments, R w1 is -H, and R w2 and R w3 together with the nitrogen to which they are attached form an optionally substituted 3 - 10 (e.g., 3 - 7, 4 - 10, 5 - 10, 5 - 7, 3, 4, 5, 6, 7, 8, 9, or 10, etc.) - membered ring having 0 - 3 (e.g., 0, 1 - 3, 1, 2, 3, etc.) heteroatoms in addition to the nitrogen atom. In some embodiments, R w1 is -H, and R w2 and R w3 together with the nitrogen to which they are attached form an optionally substituted 5 - 10 (e.g., 5 - 9, 5 - 7, 5, 6, 7, 8, 9, or 10, etc.) - membered ring having 0 - 3 (e.g., 0, 1 - 3, 1, 2, 3, etc.) heteroatoms in addition to the nitrogen atom. In some embodiments, R w1 is -H, and R w2 and R w3 together with the nitrogen to which they are attached form an optionally substituted 5 - 10 (e.g., 5 - 9, 5 - 7, 5, 6, 7, 8, 9, or 10, etc.) - membered ring having 0 heteroatoms in addition to the nitrogen atom. In some embodiments, R w1 is -H, and R w2 and R w3 together with the nitrogen to which they are attached form an optionally substituted 5 - 10 (e.g., 5 - 9, 5 - 7, 5, 6, 7, 8, 9, or 10, etc.) - membered ring having 1 heteroatom in addition to the nitrogen atom. In some embodiments, the additional heteroatom is nitrogen. In some embodiments, the additional heteroatom is oxygen.

[0119] In some embodiments, R w2 is -H, and R w1 and R w3 are each independently optionally substituted C 1~10 (e.g., C 1~9 , C 1~8, C 1~6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 is an aliphatic group such as), or together with their intervening atoms, forms an optionally substituted ring described herein. In some embodiments, R w2 is -H, and R w1 and R w3 are each independently an optionally substituted C 1~10 (e.g., C 1~9 , C 1~8 , C 1~6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) or together with their intervening atoms, forms an optionally substituted 3- to 10- (e.g., 3-7, 4-10, 5-10, 5-7, 3, 4, 5, 6, 7, 8, 9, or 10 etc.) membered ring having 0 to 3 (e.g., 0, 1-3, 1, 2, 3, etc.) heteroatoms in addition to the intervening atoms. In some embodiments, R w2 is -H, and R w1 and R w3 are each independently an optionally substituted C 1-10 aliphatic. In some embodiments, R w2 is -H, and R w1 and R w3 are each independently an optionally substituted C 1-10 alkyl. In some embodiments, R w2 is -H, and R w1 and R w3 together with their intervening atoms, form an optionally substituted 3- to 10- (e.g., 3-7, 4-10, 5-10, 5-7, 3, 4, 5, 6, 7, 8, 9, or 10 etc.) membered ring having 0 - 3 (e.g., 0, 1-3, 1, 2, 3, etc.) heteroatoms in addition to the intervening atoms. In some embodiments, R w2 is -H, and R w1 and R w3Combined with those intervening atoms, it forms an optionally substituted 5- to 10- (e.g., 5-9, 5-7, 5, 6, 7, 8, 9, or 10, etc.) membered ring having 0 to 3 (e.g., 0, 1-3, 1, 2, 3, etc.) heteroatoms in addition to the intervening atoms. In some embodiments, R w2 is -H, and R w1 and R w3 Combined with those intervening atoms, it forms an optionally substituted 5- to 10- (e.g., 5-9, 5-7, 5, 6, 7, 8, 9, or 10, etc.) membered ring having 0 heteroatoms in addition to the intervening atoms. In some embodiments, R w2 is -H, and R w1 and R w3 Combined with those intervening atoms, it forms an optionally substituted 5-10 (e.g., 5-9, 5-7, 5, 6, 7, 8, 9, or 10, etc.) membered ring having 1 heteroatom in addition to the intervening atoms. In some embodiments, the additional heteroatom is nitrogen. In some embodiments, the additional heteroatom is oxygen.

[0120] In some embodiments, R w2 and R w3 together with the nitrogen to which they are attached form a ring, or one of R w1 , and R w2 and R w3 together with those intervening atoms form a ring which is a 3-membered ring. In some embodiments, it is a 4-membered ring. In some embodiments, it is a 5-membered ring. In some embodiments, it is a 6-membered ring. In some embodiments, it is a 7-membered ring. In some embodiments, it is an 8-membered ring. In some embodiments, it is a 9-membered ring. In some embodiments, it is a 10-membered ring. In some embodiments, the formed ring is saturated (e.g., R w2 and R w3when formed together with the nitrogen atom to which they are attached). In some embodiments, the formed ring is partially unsaturated. In some embodiments, the formed ring is aromatic. In some embodiments, the formed ring is substituted. In some embodiments, the formed ring is unsubstituted. In some embodiments, the formed ring has one heteroatom. In some embodiments, the formed ring has two heteroatoms. In some embodiments, the formed ring has three heteroatoms. In some embodiments, the formed ring has four heteroatoms. In some embodiments, the formed ring is monocyclic. In some embodiments, the formed ring is bicyclic. In some embodiments, the formed ring is polycyclic.

[0121] In some embodiments, -N(R w2 )(R w3 ) includes rings formed together with one or more substituents, such as the nitrogen to which R w2 , R w3 , R w2 and R w3 are attached, rings formed by one of R w1 and R w2 and R w3 together with their intervening atoms, and the like. In some embodiments, -N(R w2 )(R w3 ) includes one or more halogen substituents. In some embodiments, -N(R w2 )(R w3 ) includes one or more (e.g., 1, 2, 3, etc.) -F. In some embodiments, the carbon atom at the beta position relative to the nitrogen to which R w2 and R w3 are attached (there are two chemical bonds / one atom between the carbon atom and the nitrogen atom, e.g., beta carbon-alpha carbon-nitrogen) is substituted. In some embodiments, it is substituted with -F. In some embodiments, it is mono-substituted and the substituent is -F. In some embodiments, it is substituted with two -F. In some embodiments, it is substituted with three -F. For example, in some embodiments, -N(Rw2 )(R w3 ) is

[0122]

Chem.

[0123] as follows. In some embodiments, -N(R w2 )(R w3 ) is

[0124]

Chem.

[0125] as follows. In some embodiments, -N(R w2 )(R w3 ) is

[0126]

Chem.

[0127] as follows. In some embodiments, -N(R w2 )(R w3 ) is

[0128]

Chem.

[0129] as follows. In some embodiments, -N(R w2 )(R w3 ) is

[0130]

Chem.

[0131] as follows. In some embodiments, -N(R w2 )(R w3 ) is

[0132] [Chemical formula]

[0133] is. In some embodiments, -N(R w2 )(R w3 ) is

[0134] [Chemical formula]

[0135] is. In some embodiments, -N(R w2 )(R w3 ) is

[0136] [Chemical formula]

[0137] is. In some embodiments, -N(R w2 )(R w3 ) is

[0138] [Chemical formula]

[0139] is. In some embodiments, -N(R w2 )(R w3 ) is

[0140] [Chemical formula]

[0141] is. In some embodiments, -N(R w2 )(R w3 ) is

[0142] [Chemical formula]

[0143] is. In some embodiments, -N(R w2 )(R w3 ) is

[0144]

Chemical formula

[0145] is. In some embodiments, -N(R w2 )(R w3 ) is

[0146]

Chemical formula

[0147] is. In some embodiments, -N(R w2 )(R w3 ) is

[0148]

Chemical formula

[0149] is. In some embodiments, -N(R w2 )(R w3 ) is

[0150]

Chemical formula

[0151] is. In some embodiments, -N(R w2 )(R w3 ) is

[0152]

Chemical formula

[0153] is. In some embodiments, -N(R w2 )(R w3 ) is

[0154] [Chemical formula]

[0155] is. In some embodiments, -N(R w2 )(R w3 ) is

[0156] [Chemical formula]

[0157] is. In some embodiments, -N(R w2 )(R w3 ) is

[0158] [Chemical formula]

[0159] is. In some embodiments, -N(R w2 )(R w3 ) is

[0160] [Chemical formula]

[0161] is. In some embodiments, -N(R w2 )(R w3 ) is

[0162] [Chemical formula]

[0163] is. In some embodiments, -N(R w2 )(R w3 ) is

[0164] [Chemical formula]

[0165] is. In some embodiments, -N(R w2 )(R w3 ) is

[0166]

Chem.

[0167] is. In some embodiments, -N(R w2 )(R w3 ) is. In some embodiments, -N(R w2 )(R w3 ) is

[0168]

Chem.

[0169] is. In some embodiments, -N(R w2 )(R w3 ) is

[0170]

Chem.

[0171] is. In some embodiments, -N(R w2 )(R w3 ) is

[0172]

Chem.

[0173] is. In some embodiments, -N(R w2 )(R w3 ) is

[0174]

Chem.

[0175] is. In some embodiments, R w2 is -CH2CF3. In some embodiments, R w2 and R w3 the carbon atom at the gamma position relative to the nitrogen to which they are attached (there are 3 chemical bonds / 2 atoms between the carbon atom and the nitrogen atom, e.g., gamma carbon - beta carbon - alpha carbon - nitrogen) is substituted. In some embodiments, it is substituted with -F. In some embodiments, it is monosubstituted and the substituent is -F. In some embodiments, it is disubstituted with two -F. In some embodiments, it is trisubstituted with three -F. For example, in some embodiments, -N(R w2 )(R w3 ) is

[0176]

Chemical formula

[0177] is.

[0178] In some embodiments, R w is

[0179]

Chemical formula

[0180] is. In some embodiments, R w is

[0181]

Chemical formula

[0182] is. In some embodiments, R w is

[0183]

Chemical formula

[0184] is. In some embodiments, R w is

[0185]

Chem.

[0186] is. In some embodiments, R w is

[0187]

Chem.

[0188] is. In some embodiments, R w is

[0189]

Chem.

[0190] is. In some embodiments, R w is

[0191]

Chem.

[0192] is. In some embodiments, R w is

[0193]

Chem.

[0194] is. In some embodiments, R w is

[0195]

Chem.

[0196] is. In some embodiments, Rw is

[0197]

Chem.

[0198] as follows. In some embodiments, R w is

[0199]

Chem.

[0200] as follows. In some embodiments, R w is

[0201]

Chem.

[0202] as follows. In some embodiments, R w is

[0203]

Chem.

[0204] as follows. In some embodiments, R w is

[0205]

Chem.

[0206] as follows. In some embodiments, R w is

[0207]

Chem.

[0208] as follows. In some embodiments, R w is

[0209]

Chem.

[0210] is. In some embodiments, R w is

[0211]

Chem.

[0212] is. In some embodiments, R w is

[0213]

Chem.

[0214] is. In some embodiments, R w is

[0215]

Chem.

[0216] is. In some embodiments, R w is

[0217]

Chem.

[0218] is. In some embodiments, R w is

[0219]

Chem.

[0220] is. In some embodiments, R w is

[0221]

Chem.

[0222] is. In some embodiments, R w is

[0223]

Chem.

[0224] is. In some embodiments, R w is

[0225]

Chem.

[0226] is. In some embodiments, R w is

[0227]

Chem.

[0228] is. In some embodiments, R w is

[0229]

Chem.

[0230] is. In some embodiments, R w is

[0231]

Chem.

[0232] is. In some embodiments, R w is

[0233]

Chem.

[0234] is. In some embodiments, R w is

[0235]

Chem.

[0236] is. In some embodiments, R w is

[0237]

Chem.

[0238] is. In some embodiments, R w is

[0239]

Chem.

[0240] is. In some embodiments, R w is

[0241]

Chem.

[0242] is. In some embodiments, R w is

[0243]

Chem.

[0244] is. In some embodiments, R w is

[0245] [Chemical formula]

[0246] is. In some embodiments, R w is

[0247] [Chemical formula]

[0248] is. In some embodiments, R w is

[0249] [Chemical formula]

[0250] is. In some embodiments, R w is

[0251] [Chemical formula]

[0252] is. In some embodiments, R w is

[0253] [Chemical formula]

[0254] is. In some embodiments, R w is

[0255] [Chemical formula]

[0256] is. In some embodiments, R w is

[0257] [Chemical formula]

[0258] is. In some embodiments, R w is

[0259]

Chem.

[0260] is. In some embodiments, R w is

[0261]

Chem.

[0262] is. In some embodiments, R w is

[0263]

Chem.

[0264] is. In some embodiments, R w is

[0265]

Chem.

[0266] is. In some embodiments, R w is

[0267]

Chem.

[0268] is. In some embodiments, R w is

[0269]

Chem.

[0270] is. In some embodiments, R w is

[0271]

Chemical formula

[0272] is. In some embodiments, R w is

[0273]

Chemical formula

[0274] is. In some embodiments, R w is

[0275]

Chemical formula

[0276] is. In some embodiments, R w is

[0277]

Chemical formula

[0278] is. In some embodiments, R w is

[0279]

Chemical formula

[0280] is. In some embodiments, R w is

[0281]

Chemical formula

[0282] is. In some embodiments, R w is

[0283]

Chem.

[0284] is. In some embodiments, R w is

[0285]

Chem.

[0286] is. In some embodiments, R w is

[0287]

Chem.

[0288] is. In some embodiments, R w is

[0289]

Chem.

[0290] is. In some embodiments, R w is

[0291]

Chem.

[0292] is. In some embodiments, R w is

[0293]

Chem.

[0294] is. In some embodiments, R w is

[0295] [Chemical formula]

[0296] is. In some embodiments, R w is

[0297] [Chemical formula]

[0298] is. In some embodiments, R w is

[0299] [Chemical formula]

[0300] is. In some embodiments, R w is

[0301] [Chemical formula]

[0302] is. In some embodiments, R w is

[0303] [Chemical formula]

[0304] is. In some embodiments, R w is

[0305] [Chemical formula]

[0306] is. In some embodiments, R w is

[0307]

Chem.

[0308] is. In some embodiments, R w is

[0309]

Chem.

[0310] is. In some embodiments, R w is

[0311]

Chem.

[0312] is. In some embodiments, R w is

[0313]

Chem.

[0314] is. In some embodiments, R w is

[0315]

Chem.

[0316] is. In some embodiments, R w is

[0317]

Chem.

[0318] is. In some embodiments, R w is

[0319]

Chem.

[0320] is. In some embodiments, R w is

[0321]

Chem.

[0322] is. In some embodiments, R w is

[0323]

Chem.

[0324] is. In some embodiments, R w is

[0325]

Chem.

[0326] is. In some embodiments, R w is

[0327]

Chem.

[0328] is. In some embodiments, R w is

[0329]

Chem.

[0330] is. In some embodiments, R w is

[0331]

Chemical formula

[0332] is. In some embodiments, R w is

[0333]

Chemical formula

[0334] is. In some embodiments, R w is

[0335]

Chemical formula

[0336] is. T

[0337] In some embodiments, T is O. In some embodiments, T is S. R w1

[0338] In some embodiments, R w1 is -L-R', where each variable is independently as described herein. In some embodiments, R w1 is -L-R', where the methylene unit of L bonded to R' is replaced by a moiety as described herein, such as -N(R')-. In some embodiments, R w1 is R' as described herein. In some embodiments, R w1 is R as described herein.

[0339] In some embodiments, R w1 is R as described herein. For example, in some embodiments, R w1is - H. In some embodiments, R w1 is an optionally substituted C 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 , etc.) aliphatic group. In some embodiments, R w1 is an optionally substituted C 1-10 alkyl. In some embodiments, R w1 is an optionally substituted methyl. In some embodiments, R w1 is methyl. In some embodiments, R w1 is an optionally substituted ethyl. In some embodiments, R w1 is ethyl. In some embodiments, R w1 is - CH2CF3. In some embodiments, R w1 is an optionally substituted propyl. In some embodiments, R w1 is an optionally substituted isopropyl. In some embodiments, R w1 is propyl. In some embodiments, R w1 is isopropyl. In some embodiments, R w1 is an optionally substituted C 3-10 cycloaliphatic group. In some embodiments, R w1 is an optionally substituted C 3-10 cycloalkyl. In some embodiments, R w1 is an optionally substituted cyclopropyl. In some embodiments, R w1 is cyclobutyl. In some embodiments, R w1 is cyclopentyl. In some embodiments, R w1 is cyclohexyl. In some embodiments, R w1 is an optionally substituted adamantyl. In some embodiments, R w1 has 1 to 6 (e.g., 1 to 3, 1 to 2, 1, 2, 3, 4, 5, 6, etc.) heteroatoms and is an optionally substituted C1 - 10 (e.g., C1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 and the like) is a heteroaliphatic group. In some embodiments, R w1 is an optionally substituted C having 1, 2, or 3 heteroatoms 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 and the like) is a heteroaliphatic group. In some embodiments, R w1 is an optionally substituted aryl. In some embodiments, R w1 is an optionally substituted aryl having 6 to 14 members (e.g., 6, 10, 14, etc.). In some embodiments, R w1 is an optionally substituted phenyl. In some embodiments, R w1 is an optionally substituted 5- to 20-membered (e.g., 5-14, 5-10, 5-9, 5, 6, 8, 9, etc.) heteroaryl having 1 to 10 (e.g., 1-5, 1-4, 1-3, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms. In some embodiments, R w1 is an optionally substituted 5- to 10-membered heteroaryl having 1 to 5 (e.g., 1-4, 1-3, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R w1 is an optionally substituted 5-membered heteroaryl having 1 to 4 (e.g., 1-3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R w1 is an optionally substituted 6-membered heteroaryl having 1 to 4 (e.g., 1-3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R w1 is an optionally substituted 9-membered bicyclic heteroaryl having 1 to 4 (e.g., 1-3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R w1is an optionally substituted 3- to 20-membered (e.g., 3- to 15-membered, 3- to 10-membered, 3- to 9-membered, 3- to 8-membered, 3- to 7-membered, 3- to 6-membered, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) heterocyclyl having 1 to 10 heteroatoms (e.g., 1 to 5, 1 to 3, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.). In some embodiments, R w1 is an optionally substituted 3- to 10-membered (e.g., 4- to 10-membered, 5- to 10-membered, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heterocyclyl having 1 to 4 heteroatoms (e.g., 1 to 3, 1, 2, 3, 4, etc.). In some embodiments, R w1 is an optionally substituted 3- to 10-membered (e.g., 4- to 10-membered, 5- to 10-membered, 3, 4, 5, 6, 7, 8, 9, 10, etc.) saturated ring having 0 to 5 heteroatoms (e.g., 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, etc.). In some embodiments, R w1 is an optionally substituted 3- to 10-membered (e.g., 4- to 10-membered, 5- to 10-membered, 3, 4, 5, 6, 7, 8, 9, 10, etc.) partially saturated ring having 0 to 5 heteroatoms (e.g., 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, etc.). In some embodiments, R w1is an optionally substituted group that is a combination of two or more of a C1-20 aliphatic group, a C1-20 heteroaliphatic group having 1 to 10 heteroatoms, a C6-20 aryl, a 5-20 membered heteroaryl having 1 to 10 heteroatoms, and a 3-20 membered heterocyclyl having 1 to 10 heteroatoms as described herein, wherein the combination has 1 to 30 (e.g., 1 to 20, 1 to 15, 1 to 10, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, etc.) carbon atoms and 0 to 10 (e.g., 0 to 5, 1 to 10, 1 to 5, 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms. When used in the present disclosure, in some embodiments, each heteroatom is independently selected from nitrogen, oxygen, and sulfur. In some embodiments, the heteroatom is nitrogen. In some embodiments, the heteroatom is oxygen. In some embodiments, the heteroatom is sulfur.

[0340] In some embodiments, R w1 is a detectable label, such as a fluorescent label, a radioactive label, a label useful in proteomics, an antibody label, a peptide label, etc., or comprises the same.

[0341] In some embodiments, as described herein, R w1 and R w2 together with their intervening atoms form an optionally substituted ring. In some embodiments, R w1 and R w2 together with their intervening atoms form an optionally substituted 3-10 (e.g., 3-7, 4-10, 5-10, 5-7, 3, 4, 5, 6, 7, 8, 9, or 10, etc.) membered ring having 0 to 3 (e.g., 0, 1-3, 1, 2, 3, etc.) heteroatoms in addition to their intervening atoms. In some embodiments, R w1 and R w2together with those intervening atoms, form an optionally substituted 3- to 10- (e.g., 3- to 7-, 4- to 10-, 5- to 10-, 5- to 7-, 3, 4, 5, 6, 7, 8, 9, or 10-membered) ring having, in addition to the intervening atoms, 0 to 3 (e.g., 0, 1 to 3, 1, 2, or 3) heteroatoms. In some embodiments, R w1 and R w2 together with those intervening atoms, form an optionally substituted 5- to 14- (e.g., 5- to 10-, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14-membered) ring having, in addition to the intervening atoms, 0 to 6 (e.g., 1 to 6, 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, or 6) heteroatoms. In some embodiments, R w1 and R w2 together with those intervening atoms, form an optionally substituted 5- to 10- (e.g., 5- to 9-, 5- to 7-, 5, 6, 7, 8, 9, or 10-membered) ring having, in addition to the intervening atoms, 0 to 3 (e.g., 0, 1 to 3, 1, 2, or 3) heteroatoms. In some embodiments, R w1 and R w2 together with those intervening atoms, form an optionally substituted 5- to 10- (e.g., 5- to 9-, 5- to 7-, 5, 6, 7, 8, 9, or 10-membered) ring having, in addition to the intervening atoms, 0 heteroatoms. In some embodiments, R w1 and R w2 together with those intervening atoms, form an optionally substituted 5- to 10- (e.g., 5- to 9-, 5- to 7-, 5, 6, 7, 8, 9, or 10-membered) ring having, in addition to the intervening atoms, 1 heteroatom. In some embodiments, as described herein, R w1 and R w3 together with those intervening atoms, form an optionally substituted ring. In some embodiments, R w1 and R w3combine with those intervening atoms to form an optionally substituted 3- to 10- (e.g., 3-7, 4-10, 5-10, 5-7, 3, 4, 5, 6, 7, 8, 9, or 10, etc.) membered ring having, in addition to those intervening atoms, 0 to 3 (e.g., 0, 1-3, 1, 2, 3, etc.) heteroatoms. In some embodiments, R w1 and R w3 combine with those intervening atoms to form an optionally substituted 3- to 10- (e.g., 3-7, 4-10, 5-10, 5-7, 3, 4, 5, 6, 7, 8, 9, or 10, etc.) membered ring having, in addition to those intervening atoms, 0 to 3 (e.g., 0, 1-3, 1, 2, 3, etc.) heteroatoms. In some embodiments, R w1 and R w3 combine with those intervening atoms to form an optionally substituted 5- to 14- (e.g., 5-10, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, etc.) membered ring having, in addition to those intervening atoms, 0 to 6 (e.g., 1-6, 1-5, 1-4, 1-3, 0, 1, 2, 3, 4, 5, 6, etc.) heteroatoms. In some embodiments, R w1 and R w3 combine with those intervening atoms to form an optionally substituted 5- to 10- (e.g., 5-9, 5-7, 5, 6, 7, 8, 9, or 10, etc.) membered ring having, in addition to those intervening atoms, 0 to 3 (e.g., 0, 1-3, 1, 2, 3, etc.) heteroatoms. In some embodiments, R w1 and R w3 combine with those intervening atoms to form an optionally substituted 5- to 10- (e.g., 5-9, 5-7, 5, 6, 7, 8, 9, or 10, etc.) membered ring having, in addition to those intervening atoms, 0 heteroatoms. In some embodiments, R w1 and R w3Together with those intervening atoms, it forms an optionally substituted 5- to 10- (e.g., 5-9, 5-7, 5, 6, 7, 8, 9, or 10, etc.) membered ring having, in addition to the intervening atoms, one heteroatom. In some embodiments, the additional heteroatom is nitrogen. In some embodiments, the additional heteroatom is oxygen. In some embodiments, the formed ring is a 3-membered ring. In some embodiments, it is a 4-membered ring. In some embodiments, it is a 5-membered ring. In some embodiments, it is a 6-membered ring. In some embodiments, it is a 7-membered ring. In some embodiments, it is an 8-membered ring. In some embodiments, it is a 9-membered ring. In some embodiments, it is a 10-membered ring. In some embodiments, the formed ring is substituted. In some embodiments, the formed ring is unsubstituted. In some embodiments, the formed ring has one heteroatom. In some embodiments, the formed ring has two heteroatoms. In some embodiments, the formed ring has three heteroatoms. In some embodiments, the formed ring has four heteroatoms. In some embodiments, the formed ring is monocyclic. In some embodiments, the formed ring is bicyclic. In some embodiments, the formed ring is polycyclic. In some embodiments, the formed ring is partially unsaturated. For example, in some embodiments, the formed ring is an optionally substituted 5- to 6-membered partially unsaturated ring having 1 to 2 (in some embodiments 1, in some embodiments 2) heteroatoms, one or each of which is nitrogen. In some embodiments, the formed ring is an optionally substituted 5-membered partially unsaturated ring having 1 to 2 heteroatoms, each of which is nitrogen. In some embodiments, the formed ring is aromatic. In some embodiments, the formed ring is an optionally substituted 5- to 6-membered heteroaryl having 1 to 3 (e.g., 1-2, 1, 2, 3, etc.) heteroatoms (one or more of which is nitrogen). In some embodiments, the formed ring is an optionally substituted 5-membered heteroaryl having 1 to 3 heteroatoms (one or more of which is nitrogen).In some embodiments, the ring formed is an optionally substituted 5-membered heteroaryl having one or two nitrogen atoms. In some embodiments, the ring formed is an optionally substituted 6-membered partially unsaturated ring having one, two, or three heteroatoms independently selected from nitrogen, oxygen, and sulfur. In some embodiments, the ring formed is an optionally substituted 6-membered partially unsaturated ring having one, two, or three nitrogen atoms. In some embodiments, the ring formed is an optionally substituted 6-membered heteroaryl having one, two, or three heteroatoms independently selected from nitrogen, oxygen, and sulfur. In some embodiments, the ring formed is an optionally substituted 6-membered heteroaryl having one, two, or three nitrogen atoms.

[0342] For example, in some embodiments, the formed ring is optionally substituted

[0343]

Chemical formula

[0344] is. In some embodiments, -C(=NR w1 )N(R w2 ) is optionally substituted

[0345]

Chemical formula

[0346] is. In some embodiments, -C(=NR w1 )N(R w3 ) is optionally substituted

[0347]

Chemical formula

[0348] is. In some embodiments, the formed ring is optionally substituted

[0349]

Chem.

[0350] is. In some embodiments, -C(=NR w1 )N(R w2 ) is optionally substituted

[0351]

Chem.

[0352] is. In some embodiments, -C(=NR w1 )N(R w3 ) is optionally substituted

[0353]

Chem.

[0354] is. In some embodiments, the formed ring is optionally substituted

[0355]

Chem.

[0356] is. In some embodiments, -C(=NR w1 )N(R w2 ) is optionally substituted

[0357]

Chem.

[0358] is. In some embodiments, -C(=NR w1 )N(R w3 ) is optionally substituted

[0359]

Chem.

[0360] It is. In some embodiments, the formed ring is optionally substituted

[0361]

Chemical formula

[0362] where y is independently 0, 1, 2, 3 or 4. In some embodiments, -C(=NR w1 )N(R w2 ) is optionally substituted

[0363]

Chemical formula

[0364] where y is independently 0, 1, 2, 3 or 4. In some embodiments, -C(=NR w1 )N(R w3 ) is optionally substituted

[0365]

Chemical formula

[0366] where y is independently 0, 1, 2, 3 or 4. In some embodiments, the formed ring is optionally substituted

[0367]

Chemical formula

[0368] where y is independently 0, 1, 2, 3 or 4 and

[0369]

Chemical formula

[0370] is a single bond or a double bond. In some embodiments, -C(=NR w1 )N(R w2 ) is optionally substituted

[0371]

Chemical formula

[0372] where y is independently 0, 1, 2, 3 or 4, and

[0373]

Chemical formula

[0374] is a single bond or a double bond. In some embodiments, -C(=NR w1 )N(R w3 ) is optionally substituted

[0375]

Chemical formula

[0376] where y is independently 0, 1, 2, 3 or 4, and

[0377]

Chemical formula

[0378] is a single bond or a double bond. In some embodiments, y is 0. In some embodiments, y is 1. In some embodiments, y is 2. In some embodiments, y is 3. In some embodiments, y is 4. In some embodiments, the formed ring is optionally substituted

[0379]

Chemical formula

[0380] is. In some embodiments, -C(=NR w1 )N(R w2 ) is optionally substituted

[0381]

Chemical formula

[0382] is. In some embodiments, -C(=NR w1 )N(R w3 ) is optionally substituted

[0383]

Chemical formula

[0384] is.

[0385] In some embodiments, -C(=NR w1 )N(R w2 )(R w3 ) is optionally substituted

[0386]

Chemical formula

[0387] is. In some embodiments, -C(=NR w1 )N(R w2 )(R w3 ) is optionally substituted. In some embodiments, -C(=NR w1 )N(R w2 )(R w3 ) is optionally substituted

[0388]

Chemical formula

[0389] is. In some embodiments, -C(=NR w1 )N(Rw2 )(R w3 ) is optionally substituted

[0390]

Chem.

[0391] is. In some embodiments, -C(=NR w1 )N(R w2 )(R w3 ) is optionally substituted

[0392]

Chem.

[0393] is. In some embodiments, -C(=NR w1 )N(R w2 )(R w3 ) is optionally substituted

[0394]

Chem.

[0395] is. In some embodiments, -C(=NR w1 )N(R w2 )(R w3 ) is optionally substituted

[0396]

Chem.

[0397] is. In some embodiments, -C(=NR w1 )N(R w2 )(R w3 ) is,

[0398]

Chem.

[0399] It is. In some embodiments, the formed ring is

[0400]

Chemical formula

[0401] ,

[0402]

Chemical formula

[0403] It is. In some embodiments, the formed ring is

[0404]

Chemical formula

[0405] It is. In some embodiments, the formed ring is

[0406]

Chemical formula

[0407] It is. R w2

[0408] In some embodiments, R w2 is -L-R', where each variable is independently as described herein. In some embodiments, R w2 is -L-R', where the methylene unit of L that binds to R' is substituted with a moiety such as -N(R')- as described herein. For example, in some embodiments, R w2 is -(CH2)3-N(CH3)-CH3. In some embodiments, R w2 is -C(CH2)2-C=C-CH3. In some embodiments, R w2 is -CH2-CF3. In some embodiments, Rw2 is -CH2-C=CH. In some embodiments, R w2 is R’ as described herein. In some embodiments, R w2 is R as described herein.

[0409] In some embodiments, R w2 is R as described herein. For example, in some embodiments, R w2 is -H. In some embodiments, R w2 is an optionally substituted C 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 , etc.) aliphatic group. In some embodiments, R w2 is an optionally substituted C 1-10 alkyl. In some embodiments, R w2 is an optionally substituted methyl. In some embodiments, R w2 is methyl. In some embodiments, R w2 is an optionally substituted ethyl. In some embodiments, R w2 is ethyl. In some embodiments, R w2 is -CH2CF3. In some embodiments, R w2 is an optionally substituted propyl. In some embodiments, R w2 is an optionally substituted isopropyl. In some embodiments, R w2 is propyl. In some embodiments, R w2 is isopropyl. In some embodiments, R w2 is an optionally substituted C 1-6 haloalkyl. In some embodiments, R w2 is an optionally substituted C 3-10 cycloaliphatic group. In some embodiments, R w2 is an optionally substituted C 3-10 cycloalkyl. In some embodiments, R w2is an optionally substituted cyclopropyl. In some embodiments, R w2 is cyclobutyl. In some embodiments, R w2 is cyclopentyl. In some embodiments, R w2 is cyclohexyl. In some embodiments, R w2 is an optionally substituted adamantyl. In some embodiments, R w2 is adamantyl. In some embodiments, R w2 is 1 - adamantyl. In some embodiments, R w2 is an optionally substituted C having 1 to 6 (e.g., 1 to 3, 1 to 2, 1, 2, 3, 4, 5, 6, etc.) heteroatoms 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 , etc.) heteroaliphatic group. In some embodiments, R w2 is an optionally substituted C having 1, 2, or 3 heteroatoms 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 , etc.) heteroaliphatic group. In some embodiments, R w2 is an optionally substituted oxetanyl. In some embodiments, R w2 is an optionally substituted aryl. In some embodiments, R w2 is an optionally substituted aryl having 6 to 14 (e.g., 6, 10, 14, etc.) members. In some embodiments, R w2 is an optionally substituted phenyl. In some embodiments, R w2 is an optionally substituted heteroaryl having 5 to 20 (e.g., 5 to 14, 5 to 10, 5 to 9, 5, 6, 8, 9, etc.) members and having 1 to 10 (e.g., 1 to 5, 1 to 4, 1 to 3, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms. In some embodiments, R w2is an optionally substituted 5- to 10-membered heteroaryl having 1 to 5 (e.g., 1 to 4, 1 to 3, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R w2 is an optionally substituted 5-membered heteroaryl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R w2 is an optionally substituted 6-membered heteroaryl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R w2 is an optionally substituted 9-membered bicyclic heteroaryl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R w2 is an optionally substituted 3- to 20- (e.g., 3 to 15, 3 to 10, 3 to 9, 3 to 8, 3 to 7, 3 to 6, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) membered heterocyclyl having 1 to 10 (e.g., 1 to 5, 1 to 3, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms. In some embodiments, R w2 is an optionally substituted 3- to 10- (e.g., 4 to 10, 5 to 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered heterocyclyl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R w2 is an optionally substituted 3- to 10- (e.g., 4 to 10, 5 to 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated ring having 0 to 5 (e.g., 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R w2 is an optionally substituted 3- to 10- (e.g., 4 to 10, 5 to 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered partially saturated ring having 0 to 5 (e.g., 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R w2 is a C as described herein 1-20 aliphatic group, a C having 1 to 10 heteroatoms 1-20 heteroaliphatic group, C6-20 An optionally substituted group that is a combination of two or more of aryl, 5- to 20-membered heteroaryl having 1 to 10 heteroatoms, and 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, wherein the combination has 1 to 30 (e.g., 1 to 20, 1 to 15, 1 to 10, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, etc.) carbon atoms and 0 to 10 (e.g., 0 to 5, 1 to 10, 1 to 5, 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms.

[0410] In some embodiments, R w2 is a detectable label, such as a fluorescent label, a radioactive label, a label useful in proteomics, an antibody label, a peptide label, etc., or comprises them.

[0411] In some embodiments, R w2 and R w3 together with the nitrogen to which they are attached form an optionally substituted ring, as described herein. In some embodiments, R w2 and R w3 together with the nitrogen atom to which they are attached form an optionally substituted 3- to 14 (e.g., 3 to 10, 3 to 8, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, etc.) -membered ring having 0 to 6 (e.g., 1 to 6, 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, 6, etc.) heteroatoms in addition to the nitrogen atom. In some embodiments, R w1 is -H, and R w2 and R w3 are each independently an optionally substituted C 1~10 (e.g., C 1~9 , C 1~8 , C 1~6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10is an aliphatic group such as), or together with the nitrogen to which they are attached, has 0 to 3 (e.g., 0, 1 to 3, 1, 2, 3, etc.) heteroatoms in addition to the nitrogen atom, and forms an optionally substituted 3- to 10- (e.g., 3- to 7-, 4- to 10-, 5- to 10-, 5- to 7-, 3, 4, 5, 6, 7, 8, 9, or 10, etc.) membered ring. In some embodiments, R w2 and R w3 together with the nitrogen to which they are attached, have 0 to 5 (e.g., 1 to 5, 0, 1 to 3, 1, 2, 3, 4, 5, etc.) heteroatoms in addition to the nitrogen atom, and form an optionally substituted 3- to 10- (e.g., 3- to 7-, 4- to 10-, 5- to 10-, 5- to 7-, 3, 4, 5, 6, 7, 8, 9, or 10, etc.) membered ring. In some embodiments, R w2 and R w3 together with the nitrogen to which they are attached, have 0 to 3 (e.g., 0, 1 to 3, 1, 2, 3, etc.) heteroatoms in addition to the nitrogen atom, and form an optionally substituted 3- to 10- (e.g., 3- to 7-, 4- to 10-, 5- to 10-, 5- to 7-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered ring. In some embodiments, R w2 and R w3 together with the nitrogen to which they are attached, have 0 to 3 (e.g., 0, 1 to 3, 1, 2, 3, etc.) heteroatoms in addition to the nitrogen atom, and form an optionally substituted 3- to 8- (e.g., 3- to 7-, 5- to 7-, 3, 4, 5, 6, 7, 8, etc.) membered ring. In some embodiments, R w2 and R w3 together with the nitrogen to which they are attached, have 0 to 3 (e.g., 0, 1 to 3, 1, 2, 3, etc.) heteroatoms in addition to the nitrogen atom, and form an optionally substituted 5- to 10- (e.g., 5- to 9-, 5- to 7-, 5, 6, 7, 8, 9, or 10, etc.) membered ring. In some embodiments, R w2 and R w3 together with the nitrogen to which they are attached, have 0 heteroatoms in addition to the nitrogen atom, and form an optionally substituted 5- to 10- (e.g., 5- to 9-, 5- to 7-, 5, 6, 7, 8, 9, or 10, etc.) membered ring. In some embodiments, R w2 and R w3combine with the nitrogen to which they are attached to form an optionally substituted 5- to 10- (e.g., 5-9, 5-7, 5, 6, 7, 8, 9, or 10, etc.) membered ring having, in addition to the nitrogen atom, one heteroatom. In some embodiments, the additional heteroatom is nitrogen. In some embodiments, the additional heteroatom is oxygen. In some embodiments, the ring formed is 3-membered. In some embodiments, the ring formed is 4-membered. In some embodiments, the ring formed is 5-membered. In some embodiments, the ring formed is 6-membered. In some embodiments, the ring formed is 7-membered. In some embodiments, the ring formed is 8-membered. In some embodiments, the ring formed is 9-membered. In some embodiments, the ring formed is 10-membered. In some embodiments, the ring formed is saturated. In some embodiments, the ring formed is partially unsaturated. In some embodiments, the ring formed is aromatic. In some embodiments, the formed ring is substituted. In some embodiments, the formed ring is unsubstituted. In some embodiments, the formed ring has one heteroatom. In some embodiments, the formed ring has two heteroatoms. In some embodiments, the formed ring has three heteroatoms. In some embodiments, the formed ring has four heteroatoms. In some embodiments, the formed ring is monocyclic. In some embodiments, the formed ring is bicyclic. In some embodiments, the formed ring is polycyclic. In some embodiments, the formed ring is optionally substituted

[0412]

Chemical formula

[0413] wherein x and y are each independently 0 to 4. In some embodiments, the formed ring is optionally substituted

[0414]

Chemical formula

[0415] wherein x and y are each independently from 0 to 4. In some embodiments, the formed ring is optionally substituted

[0416]

Chemical formula

[0417] wherein x and y are each independently from 0 to 4. In some embodiments, the formed ring is optionally substituted

[0418]

Chemical formula

[0419] wherein y is from 0 to 4. In some embodiments, the formed ring is optionally substituted

[0420]

Chemical formula

[0421] wherein x and y are each independently from 0 to 4, Q is optionally substituted, and is S, Si, S(O)2. In some embodiments, Q is S(O)2. In some embodiments, Q is Si(CH3)2. In some embodiments, Q is S. In some embodiments, x is 0. In some embodiments, x is 1. In some embodiments, x is 2. In some embodiments, x is 3. In some embodiments, x is 4. In some embodiments, y is 0. In some embodiments, y is 1. In some embodiments, y is 2. In some embodiments, y is 3. In some embodiments, y is 4. In some embodiments, the formed ring is optionally substituted

[0422]

Chemical formula

[0423] is. In some embodiments, the formed ring is optionally substituted

[0424]

Chemical formula

[0425] is. In some embodiments, the formed ring is optionally substituted

[0426]

Chemical formula

[0427] is. In some embodiments, the formed ring is optionally substituted

[0428]

Chemical formula

[0429] is. In some embodiments, the formed ring is

[0430]

Chemical formula

[0431] is. In some embodiments, the formed ring is optionally substituted

[0432]

Chemical formula

[0433] is. In some embodiments, the formed ring is

[0434]

Chemical formula

[0435] is. In some embodiments, the formed ring is optionally substituted

[0436]

Chem.

[0437] is. In some embodiments, the formed ring is

[0438]

Chem.

[0439] is. In some embodiments, the formed ring is optionally substituted

[0440]

Chem.

[0441] is. In some embodiments, the formed ring is

[0442]

Chem.

[0443] is. In some embodiments, the formed ring is optionally substituted

[0444]

Chem.

[0445] is.

[0446] In some embodiments, -N(R w2 )(R w3 ) is optionally substituted -NH2,

[0447] [Chemistry]

[0448] is. In some embodiments, -N(R w2 )(R w3 ) is -NH2,

[0449] [Chemistry]

[0450] is. In some embodiments, it is one of such groups. In some embodiments, it is one of such groups further substituted as described herein. R w3

[0451] In some embodiments, R w3 is -L-R', where each variable is independently as described herein. For example, in some embodiments, R' is -H. In some embodiments, R' is an optionally substituted C 1-6 aliphatic group. In some embodiments, R w3 is -L-R', where the methylene unit of L bonded to R' is substituted with a moiety such as -N(R')- as described herein. For example, in some embodiments, R w3 is -(CH2)3-N(CH3)-CH3. In some embodiments, R w3 is R' as described herein. In some embodiments, R w3 is R as described herein.

[0452] In some embodiments, R w3 is R as described herein. For example, in some embodiments, R w3 is -H. In some embodiments, R w3 is an optionally substituted C 1~10 (e.g., C 1~9 , C 1~8 , C 1~6, C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 and the like) is an aliphatic group. In some embodiments, R w3 is optionally substituted C 1~1 0 alkyl. In some embodiments, R w3 is optionally substituted methyl. In some embodiments, R w3 is methyl. In some embodiments, R w3 is optionally substituted ethyl. In some embodiments, R w3 is ethyl. In some embodiments, R w3 is -CH2CF3. In some embodiments, R w3 is optionally substituted propyl. In some embodiments, R w3 is optionally substituted isopropyl. In some embodiments, R w3 is propyl. In some embodiments, R w3 is isopropyl. In some embodiments, R w3 is optionally substituted C 3~10 cycloaliphatic group. In some embodiments, R w3 is optionally substituted C 3~10 cycloalkyl. In some embodiments, R w3 is optionally substituted cyclopropyl. In some embodiments, R w3 is cyclobutyl. In some embodiments, R w3 is cyclopentyl. In some embodiments, R w3 is cyclohexyl. In some embodiments, R w3 is optionally substituted adamantyl. In some embodiments, R w3 is optionally substituted C having 1 to 6 (for example, 1 to 3, 1 to 2, 1, 2, 3, 4, 5, 6, etc.) heteroatoms 1~10 (for example, C 1~9 , C 1~8 , C 1~6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10is a heteroaliphatic group such as). In some embodiments, R w3 is an optionally substituted C having 1, 2, or 3 heteroatoms 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 and the like) is a heteroaliphatic group. In some embodiments, R w3 is an optionally substituted aryl. In some embodiments, R w3 is an optionally substituted aryl having 6 to 14 members (e.g., 6, 10, 14, etc.). In some embodiments, R w3 is an optionally substituted phenyl. In some embodiments, R w3 is an optionally substituted heteroaryl having 1 to 10 (e.g., 1 to 5, 1 to 4, 1 to 3, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms and having 5 to 20 (e.g., 5 to 14, 5 to 10, 5 to 9, 5, 6, 8, 9, etc.) members. In some embodiments, R w3 is an optionally substituted heteroaryl having 1 to 5 (e.g., 1 to 4, 1 to 3, 1, 2, 3, 4, 5, etc.) heteroatoms and having 5 to 10 members. In some embodiments, R w3 is an optionally substituted heteroaryl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms and having 5 members. In some embodiments, R w3 is an optionally substituted heteroaryl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms and having 6 members. In some embodiments, R w3 is 2-pyridyl. In some embodiments, R w3 is 3-pyridyl. In some embodiments, R w3 is 4-pyridyl. In some embodiments, R w3 is an optionally substituted bicyclic heteroaryl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms and having 9 members. In some embodiments, R w3is an optionally substituted 3- to 20- (e.g., 3- to 15-, 3- to 10-, 3- to 9-, 3- to 8-, 3- to 7-, 3- to 6-, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) -membered heterocyclyl having 1 to 10 (e.g., 1 to 5, 1 to 3, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms. In some embodiments, R w3 is an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) -membered heterocyclyl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R w3 is an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) -membered saturated ring having 0 to 5 (e.g., 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R w3 is an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) -membered partially saturated ring having 0 to 5 (e.g., 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R w3 is a C 1~20 aliphatic group, a C 1~20 heteroaliphatic group having 1 to 10 heteroatoms, a C 6~20 aryl, a 5- to 20- membered heteroaryl having 1 to 10 heteroatoms, and an optionally substituted group which is a combination of two or more of a 3- to 20- membered heterocyclyl having 1 to 10 heteroatoms, wherein the combination has 1 to 30 (e.g., 1 to 20, 1 to 15, 1 to 10, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, etc.) carbon atoms and 0 to 10 (e.g., 0 to 5, 1 to 10, 1 to 5, 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms.

[0453] In some embodiments, R w3is a detectable label, such as a fluorescent label, a radioactive label, a label useful for proteomics, an antibody label, a peptide label, etc., or includes the same.

[0454] In some embodiments, R w1 and R w3 are both the R described herein. In some embodiments, R w1 and R w3 together with their intervening atoms form an optionally substituted ring described herein. In some embodiments, R w2 and R w3 both form an optionally substituted ring described herein. R w3 is the R described herein. In some embodiments, R w2 and R w3 together with the nitrogen to which they are attached form an optionally substituted ring described herein. In some embodiments, each of R w1 , R w2 , and R w3 is the R described herein. In some embodiments, R w1 , R w2 , and R w3 together with their intervening atoms form an optionally substituted ring described herein. R wh

[0455] In some embodiments, R wh is -OH. In some embodiments, R wh is -SH. X

[0456] As described herein, X is -O-, -S-, -C(R 1 )=, -N(R 1 )-, or optionally substituted -CH=, -CH=CH-, or -NH-. In some embodiments, X is -O-. In some embodiments, X is -S-. In some embodiments, X is -C(R 1 )=, where R 1is as described in this specification. In some embodiments, X is -N(R 1 )-, where R 1 is as described in this specification. In some embodiments, X is optionally substituted -CH=. In some embodiments, X is -CH=. In some embodiments, X is optionally substituted -CH=CH-. In some embodiments, X is -CH=CH-. In some embodiments, X is optionally substituted -NH-. In some embodiments, X is -NH-. Y

[0457] As described in this specification, Y is C or N. In some embodiments, Y is C. In some embodiments, Y is N. Z

[0458] As described in this specification, Z is C or N. In some embodiments, Z is C. In some embodiments, Z is N.

[0459]

Chemical formula

[0460] , for example, the bond between Y and Z can be a single bond or a double bond. In some embodiments, it is a single bond. In some embodiments, it is a double bond. For example, in some embodiments, Y and Z are C and the bond is a double bond. R 1

[0461] As described in this specification, R 1 is the R 9 described in this specification. In some embodiments, R 1is an optionally substituted group selected from R'', halogen, -CN, oxo, -NO2, or an acyl group, acylamino group, hydroxy group, amino acid group, amine group, amide group, carbamate group, ester group, ether group, carboxylic acid group, thio group, thioalkyl group, thioester group, thioether group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, alkylsulfonyl group, and arylsulfonyl group. In some embodiments, R 1 is R' as described herein. In some embodiments, R 1 is R as described herein.

[0462] In some embodiments, R 1 is hydrogen. In some embodiments, R 1 is not hydrogen. In some embodiments, R 1 is R' as described herein. In some embodiments, R 1 is R as described herein. R 2

[0463] As described herein, R 2 is R”, or each variable is independently as described herein.

[0464] In some embodiments, R 2 is R” as described herein. In some embodiments, R 2 is hydrogen. In some embodiments, R 2 is not hydrogen. In some embodiments, R 2 is R' as described herein. In some embodiments, R 2 is R as described herein. For example, in some embodiments, R is optionally substituted phenyl. In some embodiments, R is 4-fluorophenyl. In some embodiments, R is 4-aminophenyl. In some embodiments, R is an optionally substituted 5- to 6-membered heteroaryl, and 1 to 3 heteroatoms are independently selected from nitrogen, oxygen, and sulfur.

[0465] In some embodiments, R 2 is -L-R', where L and R' are each independently as described herein. For example, in some embodiments, L is a covalent bond. In some embodiments, L is optionally substituted -CH2-. In some embodiments, L is -Cy- as described herein. In some embodiments, L is an optionally substituted phenylene group. In some embodiments, L is an optionally substituted 1,4-phenylene group. In some embodiments, R' is R as described herein. In some embodiments, R' is an optionally substituted C 1-6 (e.g., C 1-5 , C1, C2, C3, C4, C5, C6, etc.) aliphatic group. In some embodiments, R' is an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated ring having 0-4 (e.g., 1-4, 1-3, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R' is an optionally substituted

[0466]

Chemical formula

[0467] is.

[0468] In some embodiments, R 2 is

[0469]

Chemical formula

[0470] where each variable is independently as described herein.

[0471] In some embodiments, L Ais a covalent bond. In some embodiments, the compound of formula A has the structure of formula A-I. In some embodiments, the compound of formula A has the structure of formula A-II. In some embodiments, the compound of formula A has the structure of formula A-III. R 3

[0472] As described herein, R 3 is R”, or each variable is independently as described herein.

[0473] In some embodiments, R 3 is the R” described herein. In some embodiments, R 3 is hydrogen. In some embodiments, R 3 is not hydrogen. In some embodiments, R 3 is the R’ described herein. In some embodiments, R 3 is the R described herein. For example, in some embodiments, R is optionally substituted phenyl. In some embodiments, R is 4-fluorophenyl. In some embodiments, R is 4-aminophenyl. In some embodiments, R is an optionally substituted 5- to 6-membered heteroaryl having 1 to 3 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

[0474] In some embodiments, R 3 is

[0475]

Chemical Formula

[0476] wherein each variable is independently as described herein.

[0477] In some embodiments, R 2 and R 3 one of them is -H. In some embodiments, R 2 and R 3One of them is -H and the other is not -H. In some embodiments, R 2 is -H and R 3 is not -H. In some embodiments, R 2 is not -H and R 3 is H. In some embodiments, the carbon atom to which R 2 and R 3 are attached is chiral. In some embodiments, it is R. In some embodiments, it is S. In some embodiments, the enantiomeric purity with respect to the carbon atom to which R 2 and R 3 are attached is about or at least about 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, 96%, 97%, 98%, or 99%. In some embodiments, the two R / S configurations are present at approximately the same level of about 50%. R 4

[0478] In some embodiments, R 4 contains an isourea moiety. In some embodiments, R4 contains an isourea moiety. In some embodiments, R 4 contains an isothiourea moiety. In some embodiments, R 4 is an isothiourea moiety. In some embodiments, R 4 is -L w -R w where each variable is independently as described herein. In some embodiments, R 4 is R w as described herein. In some embodiments, R 4 is -O-C(=NR w1 )N(R w2 )(R w3 ) where each variable is independently as described herein. In some embodiments, R 4 is -S-C(=NR w1 )N(R w2 )(R w3 ) where each variable is independently as described herein.

[0479] In some embodiments, R 4 is

[0480]

Chemical formula

[0481] as follows. In some embodiments, R 4 is

[0482]

Chemical formula

[0483] as follows. In some embodiments, R 4 is

[0484]

Chemical formula

[0485] as follows. In some embodiments, R 4 is

[0486]

Chemical formula

[0487] as follows. In some embodiments, R 4 is

[0488]

Chemical formula

[0489] as follows. In some embodiments, R 4 is

[0490]

Chemical formula

[0491] as follows. In some embodiments, R4 is

[0492]

Chem.

[0493] as follows. In some embodiments, R 4 is

[0494]

Chem.

[0495] as follows. In some embodiments, R 4 is

[0496]

Chem.

[0497] as follows. In some embodiments, R 4 is

[0498]

Chem.

[0499] as follows. In some embodiments, R 4 is

[0500]

Chem.

[0501] as follows. In some embodiments, R 4 is

[0502]

Chem.

[0503] as follows. In some embodiments, R 4 is

[0504]

Chem.

[0505] is. In some embodiments, R 4 is

[0506]

Chem.

[0507] is. In some embodiments, R 4 is

[0508]

Chem.

[0509] is. In some embodiments, R 4 is

[0510]

Chem.

[0511] is. In some embodiments, R 4 is

[0512]

Chem.

[0513] is. In some embodiments, R 4 is

[0514]

Chem.

[0515] is. In some embodiments, R 4 is

[0516]

Chem.

[0517] is. In some embodiments, R 4 is

[0518]

Chem.

[0519] is. In some embodiments, R 4 is

[0520]

Chem.

[0521] is. In some embodiments, R 4 is

[0522]

Chem.

[0523] is. In some embodiments, R 4 is

[0524]

Chem.

[0525] is. In some embodiments, R 4 is

[0526]

Chem.

[0527] is. In some embodiments, R 4 is

[0528]

Chem.

[0529] is. In some embodiments, R 4 is

[0530]

Chem.

[0531] is. In some embodiments, R 4 is

[0532]

Chem.

[0533] is. In some embodiments, R 4 is

[0534]

Chem.

[0535] is. In some embodiments, R 4 is

[0536]

Chem.

[0537] is. In some embodiments, R 4 is

[0538]

Chem.

[0539] is. In some embodiments, R 4 is

[0540] [Chemistry]

[0541] is. In some embodiments, R 4 is

[0542] [Chemistry]

[0543] is. In some embodiments, R 4 is

[0544] [Chemistry]

[0545] is. In some embodiments, R 4 is

[0546] [Chemistry]

[0547] is. In some embodiments, R 4 is

[0548] [Chemistry]

[0549] is. In some embodiments, R 4 is

[0550] [Chemistry]

[0551] is. In some embodiments, R 4 is

[0552] [Chemistry]

[0553] is. In some embodiments, R 4 is

[0554]

Chem.

[0555] is. In some embodiments, R 4 is

[0556]

Chem.

[0557] is. In some embodiments, R 4 is

[0558]

Chem.

[0559] is. In some embodiments, R 4 is

[0560]

Chem.

[0561] is. In some embodiments, R 4 is

[0562]

Chem.

[0563] is. In some embodiments, R 4 is

[0564]

Chem.

[0565] is. In some embodiments, R 4 is

[0566]

Chem.

[0567] is. In some embodiments, R 4 is

[0568]

Chem.

[0569] is. In some embodiments, R 4 is

[0570]

Chem.

[0571] is. In some embodiments, R 4 is

[0572]

Chem.

[0573] is. In some embodiments, R 4 is

[0574]

Chem.

[0575] is. In some embodiments, R 4 is

[0576]

Chem.

[0577] is. In some embodiments, R 4 is

[0578]

Chemical formula

[0579] is. In some embodiments, R 4 is

[0580]

Chemical formula

[0581] is. In some embodiments, R 4 is

[0582]

Chemical formula

[0583] is. In some embodiments, R 4 is

[0584]

Chemical formula

[0585] is. In some embodiments, R 4 is

[0586]

Chemical formula

[0587] is. In some embodiments, R 4 is

[0588]

Chemical formula

[0589] is. In some embodiments, R 4 is

[0590]

Chem.

[0591] is. In some embodiments, R 4 is

[0592]

Chem.

[0593] is. In some embodiments, R 4 is

[0594]

Chem.

[0595] is. In some embodiments, R 4 is

[0596]

Chem.

[0597] is. In some embodiments, R 4 is

[0598]

Chem.

[0599] is. In some embodiments, R 4 is

[0600]

Chem.

[0601] is. In some embodiments, R 4 is

[0602]

Chem.

[0603] is. In some embodiments, R 4 is

[0604]

Chem.

[0605] is. In some embodiments, R 4 is

[0606]

Chem.

[0607] is. In some embodiments, R 4 is

[0608]

Chem.

[0609] is. In some embodiments, R 4 is

[0610]

Chem.

[0611] is. In some embodiments, R 4 is

[0612]

Chem.

[0613] is. In some embodiments, R 4 is

[0614]

Chem.

[0615] is. In some embodiments, R 4 is

[0616]

Chem.

[0617] is. In some embodiments, R 4 is

[0618]

Chem.

[0619] is. In some embodiments, R 4 is

[0620]

Chem.

[0621] is. In some embodiments, R 4 is

[0622]

Chem.

[0623] is. In some embodiments, R 4 is

[0624]

Chem.

[0625] It is. In some embodiments, R 4 is

[0626]

Chemical formula

[0627] It is. In some embodiments, R 4 is

[0628]

Chemical formula

[0629] It is. In some embodiments, R 4 is

[0630]

Chemical formula

[0631] It is. In some embodiments, R 4 is

[0632]

Chemical formula

[0633] It is. In some embodiments, R 4 is

[0634]

Chemical formula

[0635] It is. In some embodiments, R 4 is

[0636]

Chemical formula

[0637] It is. In some embodiments, R4 is

[0638]

Chem.

[0639] as follows.

[0640] In some embodiments, R 4 is -L w -R wh as described herein, where each variable is independent. R 5

[0641] In some embodiments, R 5 is R” as described herein. In some embodiments, R 5 is -C(O)OR” where R” is as described herein. In some embodiments, R 5 is -C(O)N(R')2 where each R' is independent as described herein. In some embodiments, R 5 is -C(O)NHR’ where R' is as described herein. In some embodiments, R 5 is -C(O)NH2. In some embodiments, R 5 is -C(O)OR’ where R' is as described herein. For example, in some embodiments, R' is an optionally substituted C 1-6 aliphatic group. In some embodiments, R5 is -C(O)OCH3. In some embodiments, R 5 is

[0642]

Chem.

[0643] as follows. In some embodiments, R 5 is

[0644]

Chem.

[0645] is.

[0646] In some embodiments, R 5 is the R described herein. For example, in some embodiments, R 5 is -H. In some embodiments, R 5 is optionally substituted C 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C 2-10 , C 3-10 , C 4-10 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) is aliphatic. In some embodiments, R 5 is an optionally substituted C 1-6 aliphatic group. In some embodiments, R 5 is -CH3. In some embodiments, R 5 is an optionally substituted C 2-10 aliphatic group. In some embodiments, R 5 is an optionally substituted C 3-10 aliphatic group. In some embodiments, R 5 is an optionally substituted C 4-10 aliphatic group. In some embodiments, R 5 is an optionally substituted C 1-10 (e.g., C 1-9 , C 1- 8, C 1-6 , C 2-10 , C 3-10 , C 4-10 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) alkyl. In some embodiments, R 5 is an optionally substituted C1-6 alkyl. In some embodiments, R 5 is an optionally substituted C 2-10 alkyl. In some embodiments, R 5is optionally substituted C 3-10 alkyl. In some embodiments, R 5 is optionally substituted C 4-10 alkyl. In some embodiments, R 5 is C 1-6 alkyl or halo C 1-6 alkyl. In some embodiments, R 5 is C 1-6 alkyl optionally substituted with one or more -F. In some embodiments, R 5 is methyl. In some embodiments, R 5 is optionally substituted n-butyl. In some embodiments, R 5 is n-butyl. R 6

[0647] In some embodiments, R 6 is R” as described herein. In some embodiments, R 6 is -C(O)OR” where mR” is as described herein. In some embodiments, R 6 is -C(O)N(R')2 where each R' is independently as described herein. In some embodiments, R 6 is -C(O)NHR’ where R' is as described herein. In some embodiments, R 6 is -C(O)NH2. In some embodiments, R 6 is -C(O)OR’ where R' is as described herein. For example, in some embodiments, R' is optionally substituted C 1-6 aliphatic group. In some embodiments, R 6 is -C(O)OCH3. In some embodiments, R 6 is

[0648]

Chemical formula

[0649] It is. In some embodiments, R 6 is

[0650]

Chemical formula

[0651] It is.

[0652] In some embodiments, R 6 is the R described herein. For example, in some embodiments, R 6 is an optionally substituted C 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C 2-10 , C 3-10 , C 4-10 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) aliphatic group. In some embodiments, R 6 is an optionally substituted C 2-10 aliphatic group. In some embodiments, R 6 is an optionally substituted C 3-10 aliphatic group. In some embodiments, R 6 is an optionally substituted C 4-10 aliphatic group. In some embodiments, R 6 is an optionally substituted C 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C 2-10 , C 3-10 , C 4-10 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) alkyl. In some embodiments, R 6 is an optionally substituted C 2-10 alkyl. In some embodiments, R 6 is an optionally substituted C 3-10 alkyl. In some embodiments, R 6 is an optionally substituted C 4-10It is alkyl. In some embodiments, R 6 is optionally substituted n-butyl. In some embodiments, R 6 is n-butyl.

[0653] In some embodiments, R 5 and R 6 at least one of which is -H. In some embodiments, one of R5 is -H and the others are not -H. In some embodiments, R 5 and R 6 The carbon atom to which they are attached is chiral. In some embodiments, it is R. In some embodiments, it is S. In some embodiments, the enantiomeric purity with respect to the carbon atom to which R 5 and R 6 are attached is about or at least about 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, 96%, 97%, 98%, or 99%. In some embodiments, the two R / S configurations are present at approximately the same level of about 50%.

[0654] In some embodiments, one of R 2 and R 3 is -H, and one of R 5 and R 6 is -H. Alternatively, or additionally, in some embodiments, one of R 2 and R 3 is not -H, and one of R 5 and R 6 is not -H. In some embodiments, one of R 2 and R 3 is not -H, and one of R 5 and R 6 is not -H, and they are trans. In some embodiments, one of R 2 and R 3 is not -H, and one of R 5 and R 6 is not -H, and they are cis. In some embodiments, R 2 and R3 One of them is -H, and R 5 and R 6 One of them is -H, and they are trans. In some embodiments, R 2 and R 3 One of them is -H, and R 5 and R 6 One of them is -H, and they are cis. In some embodiments, R 5 The carbon to which R is attached is

[0655]

Chemical Structure

[0656] has the structure where carbon is attached to the carbon to which R7 is attached via bond a and to a nitrogen atom via bond b. In some embodiments, R 5 The carbon to which R is attached is

[0657]

Chemical Structure

[0658] has the structure where carbon is attached to the carbon to which R 7 is attached via bond a and to a nitrogen atom via bond b. R 7

[0659] In some embodiments, R 7 is R” as described herein. In some embodiments, R 7 is R’ as described herein. In some embodiments, R 7 is R as described herein. In some embodiments, R 7 is -H. R 8

[0660] In some embodiments, R 8 is R” as described herein. In some embodiments, R8 is R' as described in this specification. In some embodiments, R 8 is R as described in this specification. In some embodiments, R 8 is -H. R 9

[0661] In some embodiments, R 9 is R” as described in this specification. In some embodiments, R 9 is R' as described in this specification. In some embodiments, R 9 is R as described in this specification.

[0662] In some embodiments, R 9 is -OR and R is as described in this specification. In some embodiments, R 9 is -OR and R is optionally substituted C 1-6 is aliphatic. In some embodiments, R 9 is -OCH3.

[0663] In some embodiments, R 9 is -N(R')2 and each R' is independently as described in this specification. In some embodiments, R 9 is -N(R')2, one R' is -H, and the others are optionally substituted C 10 is an aliphatic group. In some embodiments, the others are optionally substituted adamantyl. In some embodiments, the others are 1-adamantyl.

[0664] In some embodiments, R 9 is -H. In some embodiments, R 9 is not -H.

[0665] In some embodiments, R 9 is halogen. In some embodiments, R 9 is -F. In some embodiments, R 9 is -Cl. In some embodiments, R 9is -Br. In some embodiments, R 9 is -I. In some embodiments, R 9 is -CN. In some embodiments, R 9 is oxo. In some embodiments, R 9 is -NO2. In some embodiments, R 9 is optionally substituted acyl. In some embodiments, R 9 is optionally substituted acylamino. In some embodiments, R 9 is hydroxy. In some embodiments, R 9 is optionally substituted amino acid group. In some embodiments, R 9 is optionally substituted amine. In some embodiments, R 9 is optionally substituted amide. In some embodiments, R 9 is optionally substituted carbamate group. In some embodiments, R 9 is optionally substituted ester group. In some embodiments, R 9 is optionally substituted ether group. In some embodiments, R 9 is optionally substituted carboxylic acid group. In some embodiments, R 9 is optionally substituted thio group. In some embodiments, R 9 is optionally substituted thioalkyl group. In some embodiments, R 9 is optionally substituted thioester group. In some embodiments, R 9 is optionally substituted thioether group. In some embodiments, R 9 is optionally substituted sulfate ester group. In some embodiments, R 9 is optionally substituted sulfonamide group. In some embodiments, R 9 is optionally substituted sulfoxide. In some embodiments, R 9 is optionally substituted sulfonate ester group. In some embodiments, R 9 is optionally substituted sulfone group. In some embodiments, R9 is an optionally substituted alkylsulfonyl. In some embodiments, R 9 is an optionally substituted arylsulfonyl. In some embodiments, when there are two or more Rs 9 they may be the same or different and each independently is as described herein.

[0666] In some embodiments, for example, there is one R attached to a moiety such as a ring. 9 In some embodiments, for example, there are two or more Rs attached to a moiety such as a ring, where each R 9 is independently as described herein. In some embodiments, R9 is a halogen. In some embodiments, R 9 is -F. In some embodiments, R 9 is -N(R’)2. In some embodiments, R 9 is independently -H, -N(R)2, -OR, -CN, and an optionally substituted C 9 aliphatic group. In some embodiments, R 1-6 is -N(R)2, where each R is independently -H or an optionally substituted C 9 aliphatic group. In some embodiments, R9 is -N(R)2, where each R is independently -H or an optionally substituted C 1-20 aliphatic group. In some embodiments, the occurrence of R 1-10 is -NHR, where each R is independently -H or an optionally substituted C 9 aliphatic group. In some embodiments, the occurrence of R 1-20 is -NHR, where each R is independently -H or an optionally substituted C 9 aliphatic group. In some embodiments, each R 1-10 is independently -H, -NH2, -CN, -CH3. In some embodiments, the occurrence of R 9 is an optionally substituted C 9 aliphatic group. In some embodiments, the occurrence of R 1-6 is an optionally substituted 9 aliphatic group. In some embodiments, each R

[0667]

Chem.

[0668] is. In some embodiments, R 9 one occurrence of is optionally substituted

[0669]

Chem.

[0670] is. In some embodiments, R 9 the occurrence of is para to the position where ring A is attached to the remainder of the compound. In some embodiments, each R 9 is independently halogen, or an optionally substituted C 1-20 aliphatic group or a C 1-20 heteroaliphatic group having 1 to 10 heteroatoms. In some embodiments, R 9 the occurrence of is -OCH3. R 10

[0671] In some embodiments, R 10 is the R” described herein. In some embodiments, R 10 is the R’ described herein.

[0672] In some embodiments, R 10 is the R described herein. For example, in some embodiments, R 10 is -H. In some embodiments, R 10 is an optionally substituted C 1-6 alkyl. In some embodiments, R 10 is an optionally substituted C 2-6 alkenyl. In some embodiments, R 10 is an optionally substituted C 2-6 alkynyl. In some embodiments, R 10 is C 3-10is a cycloalkyl of (e.g., 4 - 10, 5 - 10, 3, 4, 5, 6, 7, 8, 9, 10, etc. members). In some embodiments, R 10 is an optionally substituted C 6-14 aryl. In some embodiments, R 10 is an optionally substituted C 6-10 aryl. In some embodiments, R 10 is an optionally substituted C 7-15 aralkyl. In some embodiments, R 10 is a 5 - 10 - membered heteroaryl having 1 - 4 optionally substituted heteroatoms. In some embodiments, R 10 is a 3 - 10 - membered heterocyclyl having 1 - 4 optionally substituted heteroatoms. In some embodiments, R 10 is an optionally substituted C 1-10 aliphatic. In some embodiments, R 10 is an optionally substituted C 6-20 aryl. In some embodiments, R 10 is an optionally substituted phenyl. In some embodiments, R 10 is 2,4 - dimethoxyphenyl. In some embodiments, R 10 is 3 - chloro - 4 - methoxyphenyl. R 11

[0673] In some embodiments, R 11 is the R” described herein. In some embodiments, R 11 is the R’ described herein.

[0674] In some embodiments, R 11 is the R described herein. For example, in some embodiments, R 11 is - H. In some embodiments, R 11 is an optionally substituted C 1-10 aliphatic group. In some embodiments, R 11 is an optionally substituted C 1-6It is an aliphatic group. In some embodiments, R 11 is optionally substituted C 1-6 alkyl. In some embodiments, R 11 is optionally substituted C 2-6 alkenyl. In some embodiments, R 11 is optionally substituted C 2-6 alkynyl. In some embodiments, R 11 is C 3-10 (e.g., 4-10, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) cycloalkyl. In some embodiments, R 11 is optionally substituted C 5-20 (e.g., 5-15, 5-14, 5-10, 5-9, 5-6, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) aryl. In some embodiments, R 11 is optionally substituted C 6-14 aryl. In some embodiments, R 11 is optionally substituted C 6-10 aryl. In some embodiments, R 11 is optionally substituted phenyl. In some embodiments, R 11 is optionally substituted C 7-15 aralkyl. In some embodiments, R 11 is optionally substituted 5- to 20- (e.g., 5-15, 5-14, 5-10, 5-9, 5-6, 5, 6, 7, 8, 9, 10, etc.) membered heteroaryl having 1 to 10 (e.g., 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) heteroatoms. In some embodiments, R 11 is optionally substituted 5- to 10- membered heteroaryl having 1 to 5 (e.g., 1-4, 1-3, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R 11is an optionally substituted 5-membered heteroaryl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R 11 is an optionally substituted thienyl. In some embodiments, R 11 is an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered heterocyclyl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, 4, etc.) heteroatoms. R 12

[0675] In some embodiments, R 12 is R” as described herein. In some embodiments, R 12 is R’ as described herein.

[0676] In some embodiments, R 12 is R as described herein. For example, in some embodiments, R 12 is -H. In some embodiments, R 12 is an optionally substituted C 1-10 aliphatic group. In some embodiments, R 12 is an optionally substituted C 1-6 aliphatic group. In some embodiments, R 12 is an optionally substituted C 1-6 alkyl. In some embodiments, R 12 is an optionally substituted C 2-6 alkenyl. In some embodiments, R 12 is an optionally substituted C 2-6 alkynyl. In some embodiments, R 12 is C 3-10 (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.-membered) cycloalkyl. In some embodiments, R 12 is an optionally substituted C 5-20(e.g., 5 - 15, 5 - 14, 5 - 10, 5 - 9, 5 - 6, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) is aryl. In some embodiments, R 12 is optionally substituted C 6-14 aryl. In some embodiments, R 12 is optionally substituted C 6-10 aryl. In some embodiments, R 12 is optionally substituted phenyl. In some embodiments, R 12 is optionally substituted C 7-15 aralkyl. In some embodiments, R 12 is optionally substituted 5 - 20 (e.g., 5 - 15, 5 - 14, 5 - 10, 5 - 9, 5 - 6, 5, 6, 7, 8, 9, 10, etc.) - membered heteroaryl having 1 to 10 (e.g., 1 - 9, 1 - 8, 1 - 7, 1 - 6, 1 - 5, 1 - 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) heteroatoms. In some embodiments, R 12は is optionally substituted 5 - 10 - membered heteroaryl having 1 to 5 (e.g., 1 - 4, 1 - 3, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R 12 is optionally substituted 5 - membered heteroaryl having 1 to 4 (e.g., 1 - 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R 12 is optionally substituted thienyl. In some embodiments, R 12 is optionally substituted 3 - 10 (e.g., 4 - 10, 5 - 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) - membered heterocyclyl having 1 to 4 (e.g., 1 - 3, 1, 2, 3, 4, etc.) heteroatoms.

[0677] In some embodiments, R 11 and R 12 are each independently hydrogen, or C 1~20 (e.g., C 1~15 , C 1~10 , C 1~9, C 1~8 , C 1~6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 , C 11 , C 12 , C 13 , C 14 , C 15 , C 16 , C 17 , C 18 , C 19 , C 20 etc.) an aliphatic group, having 1 to 10 (for example, 1 to 9, 1 to 8, 1 to 7, 1 to 6, 1 to 5, 1 to 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms, C 1~20 (for example, C 1~15 , C 1~10 , C 1~9 , C 1~8 , C 1~6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 , C 11 , C 12 , C 13 , C 14 , C 15 , C 16 , C 17 , C 18 , C 19 , C 20 etc.) a heteroaliphatic group, having 1 to 10 (for example, 1 to 9, 1 to 8, 1 to 7, 1 to 6, 1 to 5, 1 to 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms, C 3-20(For example, members such as 3 to 15, 3 to 10, 4 to 20, 5 to 20, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) of heterocyclyl, C5 - 20 (For example, members such as 5 to 15, 5 to 14, 5 to 10, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) aryl, and 5 - 20 (For example, 5 to 15, 5 to 14, 5 to 10, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) membered heteroaryl having 1 to 10 (such as 1 to 9, 1 to 8, 1 to 7, 1 to 6, 1 to 5, 1 to 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms, which is an optionally substituted group selected from, or, R 11 and R 12 together with the carbon atom to which they are attached, form an optionally substituted C 3-10 (For example, 4 - 10, 5 - 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) non - aromatic unit having 0 - 5 (such as 1 - 5, 1 - 4, 1 - 3, 0, 1, 2, 3, 4, 5, etc.) heteroatoms.

[0678] In some embodiments, R 11 and R 12 are both R, and together with the carbon atom to which they are attached, form a ring as described herein. In some embodiments, R 11 and R 12 together with the carbon atom to which they are attached, form an optionally substituted 3 - 20 (For example, 3 - 15, 3 - 10, 4 - 20, 5 - 20, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) membered ring having 0 - 5 (such as 1 - 5, 1 - 4, 1 - 3, 0, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R 11 and R 12 together with the carbon atom to which they are attached, form an optionally substituted 3 - 10 (For example, 4 - 10, 5 - 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered ring having 0, 1, 2, or 3 heteroatoms. In some embodiments, R11 and R 12 together with the carbon atom to which they are attached form an optionally substituted 3- to 14- (e.g., 3- to 10-, 3- to 9-, 5- to 14-, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, etc.) membered alicyclic ring. In some embodiments, R 11 and R 12 together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered cycloalkyl ring. In some embodiments, R 11 and R 12 together with the carbon atom to which they are attached form an optionally substituted 3- to 14- (e.g., 3- to 10-, 3- to 9-, 5- to 14-, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, etc.) membered heterocyclyl ring having 1, 2 or 3 heteroatoms. R 13

[0679] In some embodiments, R 13 is R” as described herein. In some embodiments, R 13 is R’ as described herein. In some embodiments, R 13 is R as described herein. In some embodiments, R 13 is -H.

[0680] In some embodiments, R 13 is an optionally substituted C 1-10 aliphatic group. In some embodiments, R 13 is an optionally substituted C 1-6 aliphatic group. In some embodiments, R 13 is an optionally substituted C 1-6 alkyl.

[0681] In some embodiments, R 13 is -L-R’, where each of L and R’ is independently as described herein. In some embodiments, L is an optionally substituted divalent straight or branched chain C1-6 is an alkylene. In some embodiments, L is an optionally substituted divalent straight-chain C 1-6 is an alkylene. In some embodiments, L is an optionally substituted -CH2-. In some embodiments, L is -CH2-. In some embodiments, L is an optionally substituted -CH2-CH2-. In some embodiments, L is -CH2-CH2-. In some embodiments, R' is R as described herein. In some embodiments, R' is not -H. In some embodiments, R' is an optionally substituted aryl. In some embodiments, R' is an optionally substituted phenyl. In some embodiments, R' is -C(O)OR. In some embodiments, R' is -C(O)OEt. In some embodiments, R 13 is an optionally substituted cycloalkyl C 0-4 alkyl. In some embodiments, R 13 is an optionally substituted aryl C 0-4 alkyl. In some embodiments, R 13 is an optionally substituted heteroaryl C 0-4 alkyl. In some embodiments, R 13 is an optionally substituted aryl-S(O)2C 0-4 alkyl. R 14 R 14

[0682] In some embodiments, R 14 is R” as described herein. In some embodiments, R 14 is R' as described herein. In some embodiments, R 14 is R as described herein. In some embodiments, R 14 is R as described herein. In some embodiments, R 14 is -H.

[0683] In some embodiments, R 14 is an optionally substituted C 1-10 aliphatic group. In some embodiments, R14 is an optionally substituted C 1-6 aliphatic group. In some embodiments, R 14 is an optionally substituted C 1-6 alkyl.

[0684] In some embodiments, R 14 is -L-R', where each of L and R' is, independently, as described herein. In some embodiments, L is an optionally substituted divalent straight-chain or branched-chain C 1-6 alkylene. In some embodiments, L is an optionally substituted divalent straight-chain C 1-6 alkylene. In some embodiments, L is an optionally substituted -CH2-. In some embodiments, L is an optionally substituted -CH2-CH2-. In some embodiments, L is an optionally substituted -CH2-CH2-. In some embodiments, L is an optionally substituted -CH2-CH2-. In some embodiments, R' is the R described herein. In some embodiments, R' is not -H. In some embodiments, R' is an optionally substituted aryl. In some embodiments, R' is an optionally substituted phenyl. In some embodiments, R’ is -C(O)OR. In some embodiments, R’ is -C(O)OEt. In some embodiments, R 14 is an optionally substituted cycloalkyl C 0-4 alkyl. In some embodiments, R 14 is an optionally substituted aryl C 0-4 alkyl. In some embodiments, R 14 is an optionally substituted heteroaryl C 0-4 alkyl. In some embodiments, R 14 is an optionally substituted aryl-S(O)2C 0-4 alkyl. R15 R 15

[0685] In some embodiments, R 15is -L-R', where each of L and R' is independently as described herein. In some embodiments, L is an optionally substituted divalent C 1-6 aliphatic group, where the methylene units are substituted with -Cy- as described herein. In some embodiments, -Cy- is an optionally substituted phenylene. In some embodiments, -Cy- is an optionally substituted 1,2-phenylene. In some embodiments, L is an optionally substituted divalent C 1-6 aliphatic group, and the methylene units are substituted with -O-. In some embodiments, L is an optionally substituted -CH2-(1,2-phenylene)-O-, where -CH2- is bonded to a nitrogen atom. In some embodiments, R 15 is -L-R', where L is an optionally substituted C 1-6 alkylene and R' is as described herein. In some embodiments, R 15 is -L-R', where L is -CH2-C(O)N(R')-, -CH2- is optionally substituted and bonded to a nitrogen atom, and each R' is independently as described herein. In some embodiments, R 15 is -L-R', where L is -C(R')2-C(O)N(R')-, -C(R')2- is bonded to a nitrogen atom, and each R' is independently as described herein.

[0686] In some embodiments, L is -L”-L x -L y -L z -, where L” is a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms 1~7an aliphatic group or a heteroaliphatic group, wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-, and L x , L y , and L z are each independently a covalent bond or an optionally substituted methylene (optionally substituted by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-). In some embodiments, L x is a covalent bond, -N(R’), or -O-. In some embodiments, L y is a covalent bond, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, or -C(NR’)(NR’)-. In some embodiments, L z is a covalent bond, -N(R’)-, -N(R’)O- or -O-. In some embodiments, L x is a covalent bond. In some embodiments, L x is -N(R’)-, where R’ is as described herein. In some embodiments, L x is -O-. In some embodiments, L y is a covalent bond. In some embodiments, L y is -C(O)-. In some embodiments, L y is -C(S)-. In some embodiments, L yis -C(NR’)-, where R’ is as described herein. In some embodiments, L y is -C(O)N(R’)-, where R’ is as described herein. In some embodiments, L y is -C(S)N(R’)-, where R’ is as described herein. In some embodiments, L y is -C(NR’)(NR’)-, where each R’ is independently as described herein. In some embodiments, L z is a covalent bond. In some embodiments, L z is -N(R’)-, where R’ is as described herein. In some embodiments, L z is -N(R’)O-, where R’ is as described herein. In some embodiments, L z is -O-.

[0687] In some embodiments, L” is bonded to a nitrogen atom.

[0688] In some embodiments, R 15 is the R’ as described herein. In some embodiments, R 15 is the R as described herein. In some embodiments, R 15 is -H.

[0689] In some embodiments, R 15 is a C1-10 aliphatic group, a C 1-20 heteroaliphatic group having 1 to 10 heteroatoms, a C 3-20 heterocyclyl, a C 5-20 aryl, a 5- to 20-membered heteroaryl having 1 to 10 heteroatoms, a C 0-10 aliphatic-C 3-20 cycloalkyl, a C 0-10 aliphatic-C 3-20 heterocyclyl, a C 0-10 aliphatic-C 5-20 aryl, a C 0-10It is an optionally substituted group selected from aliphatic - 5 - to 20 - membered heteroaryl. In some embodiments, R 15 is an optionally substituted C 1~10 (e.g., 1 - 9, 1 - 8, 1 - 7, 1 - 6, 1 - 5, 1 - 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) aliphatic group. In some embodiments, R 15 is an optionally substituted C 1~6 alkyl. In some embodiments, R 15 is methyl. In some embodiments, R 15 is octyl. In some embodiments, R 15 is an optionally substituted C 1~2 aliphatic - C 5~20 aryl. In some embodiments, R 15 is an optionally substituted C 5~20 aryl. In some embodiments, R 15 is an optionally substituted 6 - to 14 - membered aryl. In some embodiments, R 15 is an optionally substituted 6 - to 10 - membered aryl. In some embodiments, R 15 is an optionally substituted phenyl. In some embodiments, R15 is an optionally substituted 5 - to 20 (e.g., 5 - 15, 5 - 14, 5 - 10, 5 - 9, 5 - 6, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) - membered heteroaryl having 1 - 10 (e.g., 1 - 9, 1 - 8, 1 - 7, 1 - 6, 1 - 5, 1 - 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms. In some embodiments, R 15is 3-cyanophenyl, 4-cyanophenyl, 3-chlorophenyl, 4-chlorophenyl, 3-fluorophenyl, 3-hydroxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-methoxycarbonylphenyl, 4-methoxycarbonylphenyl, 2,3-dichlorophenyl, 2,5-dichlorophenyl, 3,4-dichlorophenyl, 3-chloro-2-fluorophenyl, 5-chloro-2-fluorophenyl, 5-chloro-2-iodophenyl, 3-chloro-4-methoxyphenyl, 2,4-dimethoxyphenyl, 3-methylsulfonylphenyl, 4-methylsulfonylphenyl, 3-(pyrazol-3-yl)phenyl, 3-(1-methylpyrazol-3-yl)phenyl, 2-morpholinophenyl, 4-dimethylaminophenyl, or 1-oxo-2,3-dihydro-1H-inden-4-yl. In some embodiments, R 15 is optionally substituted indazolyl, chloropyridinyl, indolyl, methylindolyl, indazolyl, methylindazolyl, methylbenzo[d]imidazolyl, benzo[d]thiazolyl, benzo[c][1,2,5]oxadiazolyl, benzo[c][1,2,5]thiadiazolyl, benzo[d]thiazolyl, 1H-indazolyl, or [1,2,4]triazolo[4,3-a]pyridinyl. In some embodiments, R 15is 5-chloropyridin-3-yl, indol-5-yl, 1-methylindol-5-yl, indazol-5-yl, 1-methylindazol-7-yl, 1-methylbenzo[d]imidazol-5-yl, 1-methylbenzo[d]imidazol-6-yl, benzo[d]thiazol-5-yl, benzo[c][1,2,5]oxadiazol-4-yl, benzo[c][1,2,5]thiadiazol-4-yl, benzo[c][1,2,5]thiadiazol-5-yl, benzo[d]thiazol-5-yl, benzo[d]thiazol-6-yl, 1-methyl-1H-indazol-5-yl, 1-methyl-1H-indazol-6-yl, [1,2,4]triazolo[4,3-a]pyridin-6-yl, [1,2,4]triazolo[4,3-a]pyridin-7-yl, or [1,2,4]triazolo[4,3-a]pyridin-8-yl. In some embodiments, R 15 is an optionally substituted C having from 1 to 10 (e.g., 1 to 9, 1 to 8, 1 to 7, 1 to 6, 1 to 5, 1 to 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms 3~20 (e.g., 3 to 15, 3 to 10, 4 to 20, 5 to 20, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) of a heterocyclyl. In some embodiments, R 15 is benzo[d][1,3]dioxol-5-yl, 3-oxo-1,3-dihydroisobenzofuran-5-yl, benzo[d][1,3]dioxol-4-yl, 6-iodobenzo[d][1,3]dioxol-5-yl, or 2,2-difluorobenzo[d][1,3]dioxol-5-yl. R 16

[0690] In some embodiments, R 16 is -L-R', where L and R' are each independently as described herein. In some embodiments, L is an optionally substituted divalent C 1-6an aliphatic group, wherein the methylene units are substituted with -Cy- as described herein. In some embodiments, -Cy- is optionally substituted phenylene. In some embodiments, -Cy- is optionally substituted 1,2-phenylene. In some embodiments, L is optionally substituted divalent C 1-6 an aliphatic group, wherein the methylene units are substituted with -O-. In some embodiments, L is optionally substituted -CH2-(1,2-phenylene)-O-, wherein -CH2- is bonded to a nitrogen atom. In some embodiments, R 16 is -L-R', wherein L is optionally substituted C 1-6 alkylene and R' is as described herein. In some embodiments, R 16 is -L-R', wherein L is -CH2-C(O)N(R')-, wherein -CH2- is optionally substituted and bonded to a nitrogen atom and each R' is independently as described herein. In some embodiments, R 16 is -L-R', wherein L is -C(R')2-C(O)N(R')-, wherein -C(R')2- is bonded to a nitrogen atom and each R' is independently as described herein.

[0691] In some embodiments, L is -L”-L x -L y -L z -, wherein L” is a covalent bond or an optionally substituted divalent C 1~7 aliphatic or heteroaliphatic group having from 1 to 6 heteroatoms, wherein one or more methylene units are optionally and independently substituted with -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-. Also, L x 、L y 、and L zis independently a covalent bond or methylene optionally substituted (optionally substituted with -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-). In some embodiments, L x is a covalent bond, -N(R’), or -O-. In some embodiments, L y is a covalent bond, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, or -C(NR’)(NR’)-. In some embodiments, L z is a covalent bond, -N(R’)-, -N(R’)O- or -O-. In some embodiments, L x is a covalent bond. In some embodiments, L x is -N(R’)-, where R’ is as described herein. In some embodiments, L x is -O-. In some embodiments, L y is a covalent bond. In some embodiments, L y is -C(O)-. In some embodiments, L y is -C(S)-. In some embodiments, L y is -C(NR’)-, where R’ is as described herein. In some embodiments, L y is -C(O)N(R’)-, where R’ is as described herein. In some embodiments, Ly is -C(S)N(R’)-, and R’ is as described herein. In some embodiments, L y is -C(NR’)(NR’)-, where each R’ is independently as described herein. In some embodiments, L z is a covalent bond. In some embodiments, L z is -N(R’)-, where R’ is as described herein. In some embodiments, Lz is -N(R’)O-, where R’ is as described herein. In some embodiments, L z is -O-.

[0692] In some embodiments, L” is bonded to a nitrogen atom.

[0693] In some embodiments, R 16 is the R’ as described herein. In some embodiments, R 16 is the R as described herein. In some embodiments, R 16 is -H.

[0694] In some embodiments, R 16 is a C 1-10 aliphatic group, a C 1-20 heteroaliphatic group having 1 to 10 heteroatoms, a C 3-20 heterocyclyl, a C 5-20 aryl, a 5- to 20-membered heteroaryl having 1 to 10 heteroatoms, a C 0-10 aliphatic-C 3-20 cycloalkyl, a C 0-10 aliphatic-C 3-20 heterocyclyl, a C 0-10 aliphatic-C5-20 aryl, a C 0-10 aliphatic-5- to 20-membered heteroaryl, which is an optionally substituted group selected from. In some embodiments, R 16 is an optionally substituted C 1~10 (e.g., 1 to 9, 1 to 8, 1 to 7, 1 to 6, 1 to 5, 1 to 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) aliphatic group. In some embodiments, R 16 is an optionally substituted C 1~10 alkyl. In some embodiments, R 16 is an optionally substituted C 1~6 alkyl. In some embodiments, R 16 is methyl. In some embodiments, R 16 is octyl. In some embodiments, R 16is optionally substituted aryl C 0~4 alkyl. In some embodiments, R 16 is optionally substituted C 1~2 aliphatic-C 5~20 aryl. In some embodiments, R 16 is optionally substituted C 5~20 aryl. In some embodiments, R 16 is optionally substituted 6- to 14-membered aryl. In some embodiments, R 16 is optionally substituted 6- to 10-membered aryl. In some embodiments, R 16 is optionally substituted phenyl. In some embodiments, R 16 is optionally substituted 5- to 20- (e.g., 5- to 15-, 5- to 14-, 5- to 10-, 5- to 9-, 5- to 6-, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) membered heteroaryl having 1 to 10 (e.g., 1 to 9, 1 to 8, 1 to 7, 1 to 6, 1 to 5, 1 to 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms. In some embodiments, R 16 is optionally substituted C 3~14 (e.g., 3 to 10, 4 to 14, 5 to 10, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, etc.) cycloaliphatic group. In some embodiments, R 16 is optionally substituted 3- to 20- (e.g., 3- to 15-, 3- to 10-, 4- to 20-, 5- to 20-, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) membered heterocyclyl having 1 to 6 (e.g., 1 to 5, 1 to 4, 1 to 3, 1, 2, 3, 4, 5, 6, etc.) heteroatoms. In some embodiments, in the formula, R 16 is optionally substituted phenyl, thienyl, thiazolyl, tetrahydropyranyl or cyclohexyl. In some embodiments, R 16is 4-chloro-benzyl, 4-methoxy-benzyl, benzyl, 4-hydroxy-benzyl, 3-cyano-benzyl, 3-fluoro-benzyl, 3-hydroxy-benzyl, 4-cyano-benzyl, 4-fluoro-benzyl, methyl, cyclopropylmethyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, 4-methoxycarbonylcyclohexyl, phenyl, 3-aminophenyl, 4-aminophenyl, 2-fluorophenyl, 4-fluorophenyl, 3-nitrophenyl, 4-nitrophenyl, 1-methoxycarbonylmethoxyphenyl, 3-(2-hydroxyethyl)phenyl, 4-(2-hydroxyacetamido)phenyl, 2-thienyl, 5-thiazolyl, 4-pyridyl, or tetrahydro-2H-pyran-4-yl. In some embodiments, R 16 is 3-methylphenyl. In some embodiments, R 16 is

[0695]

Chemical formula

[0696] In some embodiments, R 16 is 3-indolyl. In some embodiments, R 16 is

[0697]

Chemical formula

[0698] In some embodiments, R

[0699] In some embodiments, R 15 and R 16 are R, and together with the atoms to which they are attached, form an optionally substituted ring as described herein. In some embodiments, R 15 and R 16Together with the nitrogen atom to which they are attached, in addition to the nitrogen atom to which they are attached, form an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) -membered saturated or partially unsaturated ring having 0 to 4 (e.g., 1 to 4, 1 to 3, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R 15 and R 16 Together with the nitrogen atom to which they are attached, in addition to the nitrogen atom to which they are attached, form an optionally substituted 3- to 10- membered saturated or partially unsaturated ring having 0 to 4 heteroatoms. R 17

[0700] In some embodiments, R 17 is an optionally substituted 5- to 20- (e.g., 5- to 15-, 5- to 14-, 5- to 10-, 5- to 9-, 5- to 6-, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) -membered monocyclic, bicyclic or polycyclic aromatic ring having 0 to 5 heteroatoms. In some embodiments, R 17 is an optionally substituted 5- to 6- membered heteroaryl having 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R 17 is optionally substituted phenyl. In some embodiments, R 17 is an optionally substituted 8- to 10- membered bicyclic aromatic ring having 0 to 4 (e.g., 1 to 4, 1 to 3, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R 17 is substituted. In some embodiments, one or more substituents are independently halogen. In some embodiments, one or more substituents are independently -F or -Cl. In some embodiments, each substituent is independently -F or -Cl. In some embodiments, there are one or two substituents. In some embodiments, R 17 is phenyl optionally substituted with 1, 2, or 3 substituents each independently -F or -Cl. In some embodiments, R17 is unsubstituted. R 18

[0701] In some embodiments, R 18 is an optionally substituted monocyclic, bicyclic, or polycyclic aromatic ring having from 0 to 5 heteroatoms and from 5 to 20 (e.g., 5 to 15, 5 to 14, 5 to 10, 5 to 9, 5 to 6, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) ring members. In some embodiments, R 18 is an optionally substituted 5- to 6-membered heteroaryl having from 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R 18 is optionally substituted phenyl. In some embodiments, R 18 is an optionally substituted bicyclic aromatic ring having from 0 to 4 (e.g., 1 to 4, 1 to 3, 0, 1, 2, 3, 4, etc.) heteroatoms and from 8 to 10 ring members. In some embodiments, R 18 is substituted. In some embodiments, one or more substituents are independently halogen. In some embodiments, one or more substituents are independently -F or -Cl. In some embodiments, each substituent is independently -F or -Cl. In some embodiments, there are one or two substituents. In some embodiments, R 18 is phenyl optionally substituted with 1, 2, or 3 substituents each independently -F or -Cl. In some embodiments, R 18 is unsubstituted. L A

[0702] As described herein, L A is the L described herein. In some embodiments, L A is a covalent bond. In some embodiments, L A is an optionally substituted divalent C having from 1 to 6 (e.g., 1, 2, 3, 4, 5, or 6) heteroatoms 1~10 (e.g., C 1~6, C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 is an aliphatic or heteroaliphatic group (such as), where one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-. In some embodiments, L A is an optionally substituted divalent C 1-10 (e.g., C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) aliphatic group, where one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-. In some embodiments, L A is an optionally substituted divalent C 1-6 (e.g., C1, C2, C3, C4, C5, or C6) aliphatic group, where one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-. In some embodiments, L A is an optionally substituted divalent C 1-4is an aliphatic group, wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-. In some embodiments, L A is an optionally substituted divalent C 1-2 aliphatic group, wherein one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)N(R’)-, -C(O)N(R’)-, -C(S)N(R’)-, -C(NR’)N(R’)-, -N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-. In some embodiments, L A is an optionally substituted divalent C 1-10 (e.g., C 1-6 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 , etc.) aliphatic group. In some embodiments, the divalent aliphatic group is linear. In some embodiments, the divalent aliphatic group is branched. In some embodiments, the divalent aliphatic group is saturated. In some embodiments, the divalent aliphatic group is partially unsaturated. In some embodiments, L A is or includes an optionally substituted -CH2-. In some embodiments, L A is or includes -CH2-. In some embodiments, L A is or includes -Cy- as described herein. For example, in some embodiments, L A is an optionally substituted phenylene. In some embodiments, L A is an optionally substituted 1,4-phenylene. ring

[0703] As described herein, various groups or moieties in the present disclosure are rings, for example, ring A, ring C, ring P, -Cy-, two or more R groups (and / or, for example, groups that can be R such as R’, R”, R s , R w1 , R w2 , R w3 , etc.), which are formed together with their intervening atoms to form a ring or contain a ring. Unless otherwise specified, the rings are optionally substituted. Specific rings are described herein by way of example.

[0704] In some embodiments, the ring is an optionally substituted 3- to 20- (e.g., 5-, 6-, 7-, 8-, 9-, 10-, 11-, 12-, 13-, 14-, 15-, 16-, 17-, 18-, 19-, or 20-) membered monocyclic, bicyclic, or polycyclic ring having 0 to 5 (e.g., 0, 1, 2, 3, 4, or 5) heteroatoms. In some embodiments, the ring is monocyclic. In some embodiments, the ring is bicyclic. In some embodiments, the ring is polycyclic. In some embodiments, the ring is saturated. In some embodiments, the ring is partially unsaturated. In some embodiments, the ring is aromatic. In some embodiments, the ring is a 3-membered ring. In some embodiments, the ring is a 4-membered ring. In some embodiments, the ring is a 5-membered ring. In some embodiments, the ring is a 6-membered ring. In some embodiments, the ring is a 7-membered ring. In some embodiments, the ring is an 8-membered ring. In some embodiments, the ring is a 9-membered ring. In some embodiments, the ring is a 10-membered ring. In some embodiments, the ring is an 11-membered ring. In some embodiments, the ring is a 12-membered ring. In some embodiments, the ring is a 13-membered ring. In some embodiments, the ring is a 14-membered ring. In some embodiments, the ring is a 15-membered ring. In some embodiments, the ring is a 16-membered ring. In some embodiments, the ring is a 17-membered ring. In some embodiments, the ring is an 18-membered ring. In some embodiments, the ring is a 19-membered ring. In some embodiments, the ring is a 20-membered ring. In some embodiments, the ring is bicyclic or polycyclic and comprises two or more monocyclic ring units. For example, an indole ring is bicyclic and has two monocyclic ring units, one of which is a 5-membered ring and the other is a 6-membered ring. In some embodiments, each monocyclic ring unit is independently an optionally substituted 3- to 10-, 3- to 8-, 3- to 7-, 3- to 6-, 4- to 10-, 5- to 10-, 5- to 9-, 5- to 8-, 5- to 7-, 5- to 6-, 3-, 4-, 5-, 6-, 7-, 8-, 9-, or 10-membered saturated, partially unsaturated, or aromatic ring having 0 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms. In some embodiments, each monocyclic ring unit is independently a 3- to 7-membered ring. In some embodiments, the monocyclic ring unit is a 3-membered ring. In some embodiments, the monocyclic ring unit is a 4-membered ring. In some embodiments, the monocyclic ring unit is a 5-membered ring.In some embodiments, the monocyclic ring unit is a 6-membered ring. In some embodiments, the monocyclic ring unit is a 7-membered ring. In some embodiments, the monocyclic ring unit is an 8-membered ring. In some embodiments, the monocyclic ring unit is a 9-membered ring. In some embodiments, the monocyclic ring unit is a 10-membered ring. In some embodiments, as described herein, each heteroatom is independently selected from nitrogen, oxygen, and sulfur. In some embodiments, the monocyclic ring unit is saturated. In some embodiments, the monocyclic ring unit is partially unsaturated. In some embodiments, the monocyclic ring unit is aromatic. In some embodiments, the monocyclic ring unit is heteroaromatic. In some embodiments, one ring atom of the monocyclic ring unit is a heteroatom. In some embodiments, two or more ring atoms of the monocyclic ring unit are each independently heteroatoms. In some embodiments, three or more ring atoms of the monocyclic ring unit are each independently heteroatoms. In some embodiments, four or more ring atoms of the monocyclic ring unit are each independently heteroatoms.

[0705] In some embodiments, the ring or its monocyclic unit is an optionally substituted alicyclic ring having 3 to 20 (e.g., 3 to 15, 3 to 10, 3 to 9, 3 to 8, 3 to 7, 3 to 6, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.). In some embodiments, the ring or its monocyclic unit is an optionally substituted cycloalkyl ring having 3 to 20 (e.g., 3 to 15, 3 to 10, 3 to 9, 3 to 8, 3 to 7, 3 to 6, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.). In some embodiments, the ring or its monocyclic unit is an optionally substituted heteroaliphatic ring having 3 to 20 (e.g., 3 to 15, 3 to 10, 3 to 9, 3 to 8, 3 to 7, 3 to 6, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) and having 1 to 6 (e.g., 1, 2, 3, 4, 5, or 6, etc.) heteroatoms. In some embodiments, the ring or its monocyclic unit is an optionally substituted heterocyclyl ring having 3 to 20 (e.g., 3 to 15, 3 to 10, 3 to 9, 3 to 8, 3 to 7, 3 to 6, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) and having 1 to 6 (e.g., 1, 2, 3, 4, 5, or 6, etc.) heteroatoms. In some embodiments, the ring or its monocyclic unit is an optionally substituted phenyl ring. In some embodiments, the ring or its monocyclic unit is an optionally substituted 5-membered heteroaryl ring having 1 to 4 heteroatoms. In some embodiments, the ring or its monocyclic unit is an optionally substituted 6-membered heteroaryl ring having 1 to 4 heteroatoms. In some embodiments, at least one heteroatom is nitrogen. In some embodiments, each heteroatom is independently selected from nitrogen, oxygen, and sulfur. Ring A

[0706] In some embodiments, ring A is an optionally substituted monocyclic, bicyclic or polycyclic ring having from 0 to 10 (e.g., 1 to 10, 1 to 9, 1 to 8, 1 to 7, 1 to 6, 1 to 5, 1 to 4, 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) heteroatoms and having from 3 to 20 (e.g., 3 to 15, 3 to 10, 4 to 20, 5 to 20, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) members. In some embodiments, ring A is an optionally substituted ring as described herein.

[0707] In some embodiments, ring A is an optionally substituted aromatic ring having from 0 to 6 (e.g., 1 to 6, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, 6, etc.) heteroatoms. In some embodiments, ring A is an optionally substituted monocyclic aromatic ring having from 0 to 4 (e.g., 1 to 4, 1 to 3, 0, 1, 2, 3, 4, etc.) heteroatoms or includes the same. In some embodiments, ring A is optionally substituted phenyl. In some embodiments, ring A is optionally substituted pyridyl. In some embodiments, ring A is optionally substituted pyrazolyl. In some embodiments, ring A is phenyl. In some embodiments, ring A is optionally substituted tetrahydro-2H-pyranyl. In some embodiments, ring A is tetrahydro-2H-pyranyl. In some embodiments, ring A is an optionally substituted monocyclic non-aromatic ring unit having from 0 to 6 heteroatoms or includes the same. In some embodiments, ring A is optionally substituted piperidyl. In some embodiments, ring A is optionally substituted

[0708]

Chemical Formula

[0709] and wherein, "*" represents an atom bonded to L A In some embodiments, ring A is optionally substituted

[0710]

Chem.

[0711] and wherein, "*" represents an atom bonded to L A In some embodiments, ring A is optionally substituted

[0712]

Chem.

[0713] and wherein, "*" represents an atom bonded to L A In some embodiments, ring A

[0714]

Chem.

[0715] and wherein, "*" represents an atom bonded to L A In some embodiments, ring A is bonded to one or more Rs, each of which is independently as described herein. In some embodiments, R is an optionally substituted C

[0716] In some embodiments, R is an optionally substituted C aliphatic group. In some embodiments, R is an optionally substituted C heteroaliphatic group having 1 to 10 heteroatoms. In some embodiments, R 1~20 In some embodiments, R is an optionally substituted heteroaryl C 1~20 alkyl. In some embodiments, R s is a halogen. In some embodiments, R 0-4 is -C(O)N(R')2, where each R' is independently as described herein. In some embodiments, R s is -S(O)N(R'), where R' is independently as described herein. In some embodiments, R s is -C(O)N(R')2, where each R' is independently as described herein. In some embodiments, R s is -S(O)N(R'), where R' is independently as described herein. In some embodiments, R sis -S(O)2N(R’)2, and each R’ is independently as described herein. In some embodiments, R s generation is optionally substituted

[0717]

Chemical formula

[0718] is. In some embodiments, R s generation is optionally substituted

[0719]

Chemical formula

[0720] is.

[0721] In some embodiments, ring A is an optionally substituted 3 - to 10 - membered (e.g., 4 - to 10 - membered, 5 - to 10 - membered, 3, 4, 5, 6, 7, 8, 9, 10, etc.) saturated ring having 0 to 4 (e.g., 1 to 4, 1 to 3, 0, 1, 2, 3, 4, etc.) heteroatoms. Ring B

[0722] In some embodiments, ring B is an optionally substituted monocyclic, bicyclic or polycyclic ring having from 0 to 6 (e.g., 1 to 6, 1 to 5, 1 to 4, 0, 1, 2, 3, 4, 5, 6, etc.) heteroatoms and having from 3 to 20 (e.g., 3 to 15, 3 to 10, 4 to 20, 5 to 20, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) members. In some embodiments, ring B is an optionally substituted ring as described herein. In some embodiments, ring B is an optionally substituted monocyclic ring having from 0 to 6 (e.g., 1 to 6, 1 to 5, 1 to 4, 1 to 3, 0, 1, 2, 3, 4, 5, 6, etc.) heteroatoms and having from 3 to 8 (e.g., 4 to 8, 5 to 8, 3, 4, 5, 6, 7, 8, 9, 10, etc.) members. In some embodiments, ring B is an optionally substituted 5- or 6-membered partially unsaturated ring having 1, 2, or 3 heteroatoms. In some embodiments, ring B is an optionally substituted 5-membered partially unsaturated ring having 1, 2, or 3 heteroatoms. In some embodiments, ring B is

[0723]

Chemical formula

[0724] wherein, "*" represents

[0725]

Chemical formula

[0726] an atom bonded to, and X 1 , X 2 , X 3 , and X 4 are each independently -O-, -S-, -N(-)-, -C(-)=, or optionally substituted -CH(-)-, -CH= or -NH-, provided that X 1 , X 2 , X 3 , and X 4At least one of them is -N(-)-, -C(-)=, or optionally substituted -CH(-)-. In some embodiments, ring B is

[0727]

Chemical formula

[0728] where " * " represents

[0729]

Chemical formula

[0730] an atom bonded to, and X 1 , X 3 , and X 4 are each independently -O-, -S-, or optionally substituted -CH= or -NH-, and X 2 is -N(-)-, -C(-)=, or optionally substituted -CH(-)-.

[0731] In some embodiments, X 1 is -O-. In some embodiments, X 1 is -S-. In some embodiments, X 1 is -N(-)-. In some embodiments, X 1 is -C(-)=. In some embodiments, X 1 is optionally substituted -CH(-)-. In some embodiments, X 1 is optionally substituted -CH=. In some embodiments, X 1 is optionally substituted -NH-.

[0732] In some embodiments, X 2 is -O-. In some embodiments, X 2 is -S-. In some embodiments, X 2 is -N(-)-. In some embodiments, X 2is -C(=)-. In some embodiments, X 2 is optionally substituted -CH(-)-. In some embodiments, X 2 is optionally substituted -CH=. In some embodiments, X 2 is optionally substituted -NH-.

[0733] In some embodiments, X 3 is -O-. In some embodiments, X 3 is -S-. In some embodiments, X 3 is -N(-)-. In some embodiments, X 3 is -C(=)-. In some embodiments, X 3 is optionally substituted -CH(-)-. In some embodiments, X 3 is optionally substituted -CH=. In some embodiments, X 3 is optionally substituted -NH-.

[0734] In some embodiments, X 4 is -O-. In some embodiments, X 4 is -S-. In some embodiments, X 4 is -N(-)-. In some embodiments, X 4 is -C(=)-. In some embodiments, X 4 is optionally substituted -CH(-)-. In some embodiments, X 4 is optionally substituted -CH=. In some embodiments, X 4 is optionally substituted -NH-.

[0735] In some embodiments, ring B is an optionally substituted 5- to 8-, e.g., 5-, 6-, 7-, or 8-membered monocyclic ring having from 0 to 4 (e.g., 1 to 4, 1 to 3, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, ring B is an optionally substituted 5- to 8-, e.g., 5-, 6-, 7-, or 8-membered monocyclic ring having from 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, ring B is an optionally substituted 5-membered ring having from 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, ring B is an optionally substituted 6-membered ring having from 1 to 4 (e.g., 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, ring B is an optionally substituted 5-membered ring having 2 heteroatoms. In some embodiments, ring B is an optionally substituted 6-membered ring having 2 heteroatoms. In some embodiments, the heteroatom is nitrogen. In some embodiments, the heteroatom is sulfur. For example, in some embodiments, ring B is optionally substituted

[0736] [Chemical formula]

[0737] and is. In some embodiments, ring B is

[0738] [Chemical formula]

[0739] and is. Ring C

[0740] In some embodiments, ring C is an optionally substituted monocyclic, bicyclic or polycyclic ring having from 0 to 6 (e.g., 1 to 6, 1 to 5, 1 to 4, 0, 1, 2, 3, 4, 5, 6, etc.) heteroatoms and having from 3 to 20 (e.g., 3 to 15, 3 to 10, 4 to 20, 5 to 20, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) members. In some embodiments, ring C is an optionally substituted ring as described herein.

[0741] In some embodiments, ring C is an optionally substituted 5- to 8-membered, e.g., 5, 6, 7, or 8-membered monocyclic non-aromatic ring having from 0 to 4 (e.g., 1 to 4, 1 to 3, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, ring C is an optionally substituted 3- to 10 (e.g., 4 to 10, 5 to 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered monocyclic saturated ring having from 0 to 4 (e.g., 1 to 4, 1 to 3, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, ring C is an optionally substituted 5- to 10 (e.g., 5 to 9, 5, 6, 7, 8, 9, 10, etc.) membered monocyclic saturated ring having one or two nitrogen atoms. In some embodiments, ring C is an optionally substituted 5-membered monocyclic saturated ring having two nitrogen atoms. In some embodiments, ring C is an optionally substituted 6-membered monocyclic saturated ring having two nitrogen atoms. In some embodiments, ring C is an optionally substituted 7-membered monocyclic saturated ring having two nitrogen atoms. In some embodiments, ring C is an optionally substituted 8-membered monocyclic saturated ring having two nitrogen atoms. In some embodiments, ring C is an optionally substituted 9-membered monocyclic saturated ring having two nitrogen atoms. In some embodiments, ring C is an optionally substituted 10-membered monocyclic saturated ring having two nitrogen atoms. In some embodiments, ring C is attached to the remainder of the compound through two nitrogen atoms. In some embodiments, ring C is an optionally substituted divalent piperidyl. In some embodiments, ring C is an optionally substituted divalent piperazinyl. In some embodiments, ring C is an optionally substituted divalent 2,7-diazaspiro[3.5]nonyl.

[0742] In some embodiments, ring C has a structure such that the compound of formula E or a salt thereof is the compound of formula F or a salt thereof. Ring P

[0743] As described herein, ring P is an optionally substituted monocyclic, bicyclic or polycyclic ring having 0 to 5 (e.g., 0, 1, 2, 3, 4 or 5) heteroatoms and having 3 to 20 (e.g., 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20) ring members. In some embodiments, ring P is monocyclic. In some embodiments, ring P is bicyclic. In some embodiments, ring P is polycyclic. In some embodiments, ring P is saturated. In some embodiments, ring P is partially unsaturated. In some embodiments, ring P is aromatic. In some embodiments, ring P is a 3-membered ring. In some embodiments, ring P is a 4-membered ring. In some embodiments, ring P is a 5-membered ring. In some embodiments, ring P is a 6-membered ring. In some embodiments, ring P is a 7-membered ring. In some embodiments, ring P is an 8-membered ring. In some embodiments, ring P is a 9-membered ring. In some embodiments, ring P is a 10-membered ring. In some embodiments, ring P is an 11-membered ring. In some embodiments, ring P is a 12-membered ring. In some embodiments, ring P is a 13-membered ring. In some embodiments, ring P is a 14-membered ring. In some embodiments, ring P is a 15-membered ring. In some embodiments, ring P is a 16-membered ring. In some embodiments, ring P is a 17-membered ring. In some embodiments, ring P is an 18-membered ring. In some embodiments, ring P is a 19-membered ring. In some embodiments, ring P is a 20-membered ring. In some embodiments, the monocyclic ring unit in ring P is an optionally substituted 5- to 6-membered aromatic ring having 0 to 4 (e.g., 0, 1, 2, 3 or 4) heteroatoms and containing Z and Y as ring atoms. In some embodiments, such an aromatic ring is a 5-membered ring. In some embodiments, such an aromatic ring is a 6-membered ring. In some embodiments, such an aromatic ring is substituted. In some embodiments, such an aromatic ring is unsubstituted.In some embodiments, such an aromatic ring has one heteroatom, in some embodiments, two heteroatoms, in some embodiments, three heteroatoms, in some embodiments, four heteroatoms, and in some embodiments, at least one heteroatom is nitrogen. In some embodiments, ring P is an optionally substituted phenyl ring. In some embodiments, ring P is an optionally substituted pyrrole ring. In some embodiments, ring P is an optionally substituted indole ring.

[0744] In some embodiments, each monocyclic ring unit in ring P is independently an optionally substituted 3- to 10-, 3- to 8-, 3- to 7-, 3- to 6-, 4- to 10-, 5- to 10-, 5- to 9-, 5- to 8-, 5- to 7-, 5- to 6-, 3-, 4-, 5-, 6-, 7-, 8-, 9-, or 10-membered saturated, partially unsaturated or aromatic ring having from 0 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms. In some embodiments, each monocyclic ring unit is independently a 3- to 7-membered ring. In some embodiments, the monocyclic ring unit is a 3-membered ring. In some embodiments, the monocyclic ring unit is a 4-membered ring. In some embodiments, the monocyclic ring unit is a 5-membered ring. In some embodiments, the monocyclic ring unit is a 6-membered ring. In some embodiments, the monocyclic ring unit is a 7-membered ring. In some embodiments, the monocyclic ring unit is an 8-membered ring. In some embodiments, the monocyclic ring unit is a 9-membered ring. In some embodiments, the monocyclic ring unit is a 10-membered ring. In some embodiments, as described herein, each heteroatom is independently selected from nitrogen, oxygen and sulfur. In some embodiments, the monocyclic ring unit is saturated. In some embodiments, the monocyclic ring unit is partially unsaturated. In some embodiments, the monocyclic ring unit is aromatic. In some embodiments, the monocyclic ring unit is heteroaromatic. In some embodiments, one ring atom of the monocyclic ring unit is a heteroatom. In some embodiments, two or more ring atoms of the monocyclic ring unit are each independently heteroatoms. In some embodiments, three or more ring atoms of the monocyclic ring unit are each independently heteroatoms. In some embodiments, four or more ring atoms of the monocyclic ring unit are each independently heteroatoms. R s

[0745] In some embodiments, R s is R” as described herein. In some embodiments, R s is R’ as described herein. In some embodiments, R s is R as described herein.

[0746] In some embodiments, Rs is -H. In some embodiments, R s is not -H.

[0747] In some embodiments, R s is a halogen. In some embodiments, R s is -F. In some embodiments, R s is -Cl. In some embodiments, R s is -Br. In some embodiments, R s is -I. In some embodiments, R s is -CN. In some embodiments, R s is oxo. In some embodiments, R s is -NO2. In some embodiments, R s is an optionally substituted acyl group. In some embodiments, R s is an optionally substituted acylamino group. In some embodiments, R s is a hydroxy group. In some embodiments, R s is an optionally substituted amino acid group. In some embodiments, R s is an optionally substituted amine group. In some embodiments, R s is an optionally substituted amide group. In some embodiments, Rs is an optionally substituted carbamate group. In some embodiments, R s is an optionally substituted ester group. In some embodiments, R s is an optionally substituted ether group. In some embodiments, R s is an optionally substituted carboxylic acid group. In some embodiments, R s is an optionally substituted thio group. In some embodiments, R s is an optionally substituted thioalkyl group. In some embodiments, R s is an optionally substituted thioester group. In some embodiments, R s is an optionally substituted thioether group. In some embodiments, R sis an optionally substituted sulfate group. In some embodiments, R s is an optionally substituted sulfonamide group. In some embodiments, R s is an optionally substituted sulfoxide group. In some embodiments, R s is an optionally substituted sulfonate ester group. In some embodiments, R s is an optionally substituted sulfone. In some embodiments, R s is an optionally substituted alkylsulfonyl. In some embodiments, R s is an optionally substituted arylsulfonyl. In some embodiments, when there are two or more Rs, they may be the same or different, and each is independently as described herein.

[0748] In some embodiments, for example, there is one occurrence of R s attached to a moiety such as a ring. In some embodiments, there are two or more occurrences of R s and, as described herein, each occurrence of R s is attached to a moiety where each occurrence is independent, for example, a ring. In some embodiments, the occurrence of R s is a halogen. In some embodiments, the occurrence of R s is -F. In some embodiments, the occurrence of R s is -Cl. In some embodiments, the occurrence of R s is -N(R')2. In some embodiments, each occurrence of R s is independently -H, -N(R)2, -OR, -CN, and an optionally substituted C 1-6 aliphatic group. In some embodiments, the occurrence of R s is -N(R)2 and each R is independently -H or an optionally substituted C 1~20 aliphatic group. In some embodiments, the occurrence of R s is -N(R)2 and each R is independently -H or an optionally substituted C1-10 aliphatic group. In some embodiments, R sThe occurrence of -NHR, where each R is independently -H or an optionally substituted C 1~20 is an aliphatic group. In some embodiments, R s The occurrence of -NHR, where each R is independently -H or an optionally substituted C 1~10 is an aliphatic group. In some embodiments, each R is independently -H, -NH2, -CN, -CH3. In some embodiments, R s The occurrence of is an optionally substituted C 1~6 is an aliphatic group. In some embodiments, R s The occurrence of is an optionally substituted methyl. In some embodiments, R s The occurrence of is a methyl optionally substituted with 1 to 3 fluoros. In some embodiments, R s The occurrence of is -CF3. In some embodiments, R S The occurrence of is an optionally substituted

[0749]

Chemical Structure

[0750] is. In some embodiments, R S One occurrence of is an optionally substituted

[0751]

Chemical Structure

[0752] is. In some embodiments, R S The occurrence of is para to the position where ring A is attached to the rest of the compound. In some embodiments, each R S is independently a halogen, or an optionally substituted C 1~20 aliphatic group or a C with 1 to 10 heteroatoms 1~20 heteroaliphatic group. In some embodiments, R s The occurrence of is -OCH3. In some embodiments, R s The occurrence of is -OCF3. In some embodiments, Rs The generation of -S(O)2-R'. In some embodiments, R s The generation of -S(O)2-R. In some embodiments, R s The generation of -S(O)2-CH3.

[0753] R s6

[0754] In some embodiments, R s6 is the R described herein. In some embodiments, R s is as described. In some embodiments, R s6 is the R” described herein. In some embodiments, R s6 is the R’ described herein. In some embodiments, R s6 is the R described herein.

[0755] In some embodiments, R s6 is -H. In some embodiments, R s6 is not -H. In some embodiments, R s6 is a halogen. In some embodiments, R s6 is -F. In some embodiments, R s6 is -Cl. In some embodiments, R s6 is -Br. In some embodiments, R s6 is -I. In some embodiments, R s6 is -CN. In some embodiments, each R s6 is independently a halogen or -CN. In some embodiments, each R s6 is independently -F or -Cl. R s7

[0756] In some embodiments, R s7 is the R described herein. In some embodiments, R s is as described. In some embodiments, R s7 is the R” described herein. In some embodiments, R s7 is the R’ described herein. In some embodiments, Rs7 is R as described herein.

[0757] In some embodiments, R s7 is -H. In some embodiments, R s7 is not -H. In some embodiments, R s7 is halogen. In some embodiments, R s7 is -F. In some embodiments, R s7 is -Cl. In some embodiments, R s7 is -Br. In some embodiments, R s7 is -I. In some embodiments, Rs7 is -CN. In some embodiments, each Rs7 is independently halogen or -CN. In some embodiments, each R s7 is independently -F or -Cl. R 8a

[0758] In some embodiments, R 8a is R as described herein s In some embodiments, R 8a is an optionally substituted C 1-6 aliphatic group. In some embodiments, R 8a is optionally substituted methyl.

[0759] In some embodiments, R 8a is -L-R', where each variable is independently as described herein. In some embodiments, R' is an optionally substituted 6- to 10-membered aryl. In some embodiments, R' is optionally substituted phenyl. In some embodiments, R8a is -L-R, where each variable is independently as described herein. In some embodiments, L is optionally substituted -CH2-. In some embodiments, L is -CH2-. In some embodiments, R is not -H. In some embodiments, R is optionally substituted phenyl. For example, in some embodiments, R is 2-chlorophenyl.

[0760] In some embodiments, R 8a is

[0761] [Chemical formula]

[0762] wherein each variable is independently as described herein. In some embodiments, L A is optionally substituted -CH2-. In some embodiments, L A is -CH2-. In some embodiments, ring A is optionally substituted phenylene. In some embodiments, ring A is optionally substituted 1,2-phenylene. In some embodiments, q is 0. In some embodiments, q is 1 to 10. In some embodiments, q is 1. In some embodiments, each R m is independently R s as described herein. In some embodiments, R m is halogen. In some embodiments, each R m is independently halogen. In some embodiments, R m is -F. In some embodiments, R m is -Cl. In some embodiments, R m is -Br. In some embodiments, R m is -I. In some embodiments, each R m that is halogen is independently -F or -Cl. In some embodiments, each substituent (if any) on ring A is independently halogen. In some embodiments, it is independently -F or -Cl. In some embodiments, it is -Cl. R m

[0763] In some embodiments, R m is R s as described herein. In some embodiments, R mis R as described in this specification. In some embodiments, R m is R' as described in this specification. In some embodiments, R m is R as described in this specification.

[0764] In some embodiments, R m is a halogen. In some embodiments, R m is -F. In some embodiments, R m is -Cl. In some embodiments, R m is -Br. In some embodiments, R m is -I. In some embodiments, R m is -CN. In some embodiments, R m is oxo. In some embodiments, R m is -NO2. In some embodiments, R m is an optionally substituted group selected from an acyl group, an acylamino group, a hydroxy group, an amino acid group, an amine group, an amide group, a carbamate group, an ester group, an ether group, a carboxylic acid group, a thio group, a thioalkyl group, a thioester group, a thioether group, a sulfate ester group, a sulfonamide group, a sulfoxide group, a sulfonate ester group, a sulfone group, an alkylsulfonyl group, and an arylsulfonyl group. L R

[0765] In some embodiments, L R is

[0766]

Chemical formula

[0767] wherein each variable is independently as described in this specification. In some embodiments, L R is

[0768]

Chemical formula

[0769] and where "*" represents an atom bonded to R 4 as described herein. In some embodiments, L R is

[0770]

Chemical formula

[0771] and where "*" represents an atom bonded to R 4 as described herein. For example, in some embodiments, L R is optionally substituted

[0772]

Chemical formula

[0773] and where the nitrogen atom is bonded to L b herein.

[0774] In some embodiments, L R is an optionally substituted bicyclic or tricyclic ring, and the monocyclic ring is an optionally substituted 6-membered heteroaryl ring containing =N-C*(-)=N-, where "*" represents an atom bonded to R 4 herein. In some embodiments, L b is bonded to different monocyclic rings. In some embodiments, L R is optionally substituted

[0775]

Chemical formula

[0776] and where "*" represents an atom bonded to R 4 herein. In some embodiments, L R is optionally substituted

[0777] [Chemical formula]

[0778] wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0779] [Chemical formula]

[0780] wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0781] [Chemical formula]

[0782] wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0783] [Chemical formula]

[0784] wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0785] [Chemical formula]

[0786] wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0787]

Chem.

[0788] and wherein, "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0789]

Chem.

[0790] and wherein, "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0791]

Chem.

[0792] and wherein, "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0793]

Chem.

[0794] and wherein, "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0795]

Chem.

[0796] and wherein, "*" represents an atom bonded to R 4 In some embodiments, LR is optionally substituted

[0797]

Chem.

[0798] and wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0799]

Chem.

[0800] and wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0801]

Chem.

[0802] and wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0803]

Chem.

[0804] and wherein "*" represents an atom bonded to R 4 In some embodiments, L R is optionally substituted

[0805]

Chem.

[0806] and wherein "*" represents an atom bonded to R4 represents an atom bonded to L. In some embodiments, L R is optionally substituted

[0807]

Chem.

[0808] where " * " represents an atom bonded to R 4 represents an atom bonded to L. In some embodiments, L R is optionally substituted

[0809]

Chem.

[0810] where " * " represents an atom bonded to R 4 represents an atom bonded to L. In some embodiments, L R is optionally substituted

[0811]

Chem.

[0812] where " * " represents an atom bonded to R 4 represents an atom bonded to L. In some embodiments, L R is optionally substituted

[0813]

Chem.

[0814] where " * " represents an atom bonded to R 4 represents an atom bonded to R. In some embodiments, the ring may exist in tautomeric forms (e.g., -C(OH)= and -C(O)-).

[0815] In some embodiments, L R is -Cy- as described herein.

[0816] In some embodiments, L R is

[0817] [Chemical formula]

[0818] wherein R s1 , R s2 and R s3 are each independently an R as described herein s . In some embodiments, L R is

[0819] [Chemical formula]

[0820] wherein R s1 , R s2 and R s3 are each independently an R as described herein s . In some embodiments, the nitrogen atom is bonded to L b . In some embodiments, L R is

[0821] [Chemical formula]

[0822] wherein each variable is independently as described herein, and "*" indicates an atom bonded to R 4 . In some embodiments, L R is

[0823] [Chemical formula]

[0824] wherein each variable is independently as described herein, and "*" indicates an atom bonded to R 4represents an atom bonded to. In some embodiments, L R is

[0825] [Chemical Formula]

[0826] wherein each variable is, independently, as described herein, and "*" represents an atom bonded to R 4 represents an atom bonded to.

[0827] In some embodiments, Z’ is -C(R s4 ), where R s4 is R s as described herein. In some embodiments, Z’ is -C(R s4 ), where R s4 is R’ as described herein. In some embodiments, Z’ is -C(R s4 ), where R s4 is R as described herein. In some embodiments, R s4 is an aliphatic group such as C 1~10 (e.g., C 1~9 , C 1~8 , C 1~6 , C 2~10 , C 3~10 , C 4~10 , C 1 , C 2 , C 3 , C 4 , C 5 , C 6 , C 7 , C 8 , C 9 , C 10 etc.), or a C 1~10 having 1 to 5 (e.g., 1 to 4, 1, 2, 3, 4, 5, etc.) heteroatoms (e.g., C 1~9 , C 1~8 , C 1~6 , C 2~10 , C 3~10 , C 4~10 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10a heteroaliphatic group such as), an aryl having 6 to 10 (for example, 6, 7, 8, 9, 10, etc.) members, a heteroaryl having 1 to 4 (for example, 1 to 3, 1, 2, 3, 4, etc.) heteroatoms and having 5 to 10 (for example, 5, 6, 7, 8, 9, 10, etc.) members, and a heterocyclyl having 1 to 5 (for example, 1 to 4, 2 to 5, 1, 2, 3, 4, 5, etc.) heteroatoms and having 3 to 10 (for example, 4 to 10, 5 to 10, 5 to 7, 5 to 6, 3, 4, 5, 6, 7, 8, 9, 10, etc.) members, which is an optionally substituted group. In some embodiments, R s4 is -H. In some embodiments, R s4 is -halogen. In some embodiments, R s4 is -F. In some embodiments, R s4 is -Cl. In some embodiments, R s4 is -Br. In some embodiments, R s4 is -I. In some embodiments, R s4 is -CN. In some embodiments, R s4 is -N(R’)2, where each R’ is independently as described herein. In some embodiments, R s4 is -N(R’)2, where each R’ is independently -H or an optionally substituted C 1-6 aliphatic group. In some embodiments, R s4 is -N(R’)2, where each R’ is independently an optionally substituted C 1-6 aliphatic group. In some embodiments, R s4 is an optionally substituted -NH2. In some embodiments, R s4 is -NH2. In some embodiments, R s4 is an optionally substituted C 1-10 (for example, C 1-9 , C1-8 , C 1-6 , C 2-10 , C 3-10 , C 4-10 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) aliphatic group. In some embodiments, R s4is an optionally substituted C having 1 to 5 (e.g., 1 to 4, 2 to 5, 1, 2, 3, 4, 5, etc.) heteroatoms 1~10 (e.g., C 1-9 、C 1-8 、C 1-6 、C 2-10 、C 3-10 、C 4-10 、C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) heteroaliphatic group. In some embodiments, R s4 is an optionally substituted 3- to 10- (e.g., 3 to 9, 4 to 10, 5 to 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered heterocyclyl having 1 to 5 (e.g., 1 to 4, 2 to 5, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R s4 is optionally substituted

[0828]

Chemical formula

[0829] is.

[0830] In some embodiments, Z” is -C(R s5 ), where R s5 is the Rs described herein. In some embodiments, Z” is -C(R s5 ), where R s5 is the R’ described herein. In some embodiments, Z” is -C(R s5 ), where R s5 is the R described herein. In some embodiments, R s5 is -H. In some embodiments, R s5 is -halogen. In some embodiments, R s5 is -F. In some embodiments, R s5 is -Cl. In some embodiments, R s5 is -Br. In some embodiments, R s5 is -I. In some embodiments, R s5is -CN. In some embodiments, R s5 is -N(R’)2, where each R’ is independently as described herein. In some embodiments, R s5 is -N(R’)2, where each R’ is independently -H or an optionally substituted C 1-6 aliphatic group. In some embodiments, R s5 is -N(R’)2, and each R’ is independently an optionally substituted C 1-6 aliphatic. In some embodiments, R s5 is an optionally substituted -NH2. In some embodiments, R s5 is -NH2. In some embodiments, R s5 is an optionally substituted C 1-10 (e.g., C 1-9 , C 1-8 , C 1-6 , C 2-10 , C 3-10 , C 4-10 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) aliphatic group. In some embodiments, R s5 is an optionally substituted C 1~10 (e.g., C 1~9 , C 1~8 , C 1~6 , C 2~10 , C 3~10 , C 4~10 , C1, C2, C3, C4, C5, C6, C7, C8, C9, C 10 etc.) heteroaliphatic having 1 to 5 (e.g., 1 to 4, 2 to 5, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R s5 is an optionally substituted 3- to 10- (e.g., 3- to 9-, 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered heterocyclyl having 1 to 5 (e.g., 1 to 4, 2 to 5, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, R s5 is -OR, where R is as described herein. In some embodiments, R s5 is -OR, where R is an optionally substituted C 1~6It is an aliphatic group. In some embodiments, R s5 is -OH. In some embodiments, R s5 is -OCH3.

[0831] In some embodiments, R s1 is the R described herein s . In some embodiments, R s1 is the R' described herein. In some embodiments, R s1 is the R described herein. In some embodiments, R s1 is -N(R')2, where each R' is independent as described herein. In some embodiments, R s1 is -N(R')2, where each R' is independently -H or an optionally substituted C 1-6 aliphatic group. In some embodiments, in some embodiments, R s1 is -NHR', where R' is an optionally substituted C 1-6 aliphatic group. In some embodiments, R s1 is -NHR', where R' is -H or an optionally substituted C 1-6 alkyl. In some embodiments, R s1 is an optionally substituted -NH2. In some embodiments, R s1 is -NH2. In some embodiments, R s1 is -NHCH3. In some embodiments, R s1 is -NHCD3. In some embodiments, R s1 is -NHCH2CH3. In some embodiments, R s1 is -NHCH2CH2CH3. In some embodiments, R s1 is -NHCH(CH3)2. In some embodiments, R s1 is -N(CH3)2. In some embodiments, R s1 is

[0832]

Chemical formula

[0833] is. In some embodiments, R s1 is

[0834]

Chem.

[0835] is. In some embodiments, R s1 is -NHCH2CF3. In some embodiments, R s1 is -NHCH2CHF2. In some embodiments, R s1 is -NHCH2C≡CH. In some embodiments, R s1 is -NHCH2CH═CH2. In some embodiments, R s1 is optionally substituted

[0836]

Chem.

[0837] is. In some embodiments, R s1 is

[0838]

Chem.

[0839] is. In some embodiments, R s1 is

[0840]

Chem.

[0841] is. In some embodiments, R s1 is -OR’, where R’ is as described herein. In some embodiments, R s1 is -OR, where R is as described herein. In some embodiments, Rs1 is -OR, and R is an optionally substituted C 1-6 aliphatic group. In some embodiments, R s1 is -OH. In some embodiments, R s1 , when being -OH, the ring or the compound may exist in the form of tautomers. In some embodiments, -C(OH)= may exist as -C(O)-. In some embodiments, -C(OH)=N- may exist as -C(O)-NH-. In some embodiments, R s1 is -OCH3. In some embodiments, R s1 is a halogen. In some embodiments, R s1 is -F. In some embodiments, R s1 is -Cl. In some embodiments, R s1 is -Br. In some embodiments, R s1 is -I. In some embodiments, R s1 is -H. In some embodiments, R s1 is -CF3. In some embodiments, R s1 is -CHF2.

[0842] In some embodiments, R s4 is an optionally substituted

[0843]

Chemical formula

[0844] is. In some embodiments, R s4 is

[0845]

Chemical formula

[0846] is. In some embodiments, R s4 is an optionally substituted

[0847] [Chemistry]

[0848] is. In some embodiments, R s4 is

[0849] [Chemistry]

[0850] is. In some embodiments, R s4 is optionally substituted

[0851] [Chemistry]

[0852] is. In some embodiments, R s4 is

[0853] [Chemistry]

[0854] is. In some embodiments, R s4 is -N(R’)2. In some embodiments, R s4 is -NH2. In some embodiments, R s4 is -OR’. In some embodiments, R s4 is -O(CH(CH3)2. In some embodiments, R s4 is optionally substituted C 1-6 aliphatic group. In some embodiments, R s4 is an aliphatic group optionally substituted with -OR°, where R° is -H or C 1-6 aliphatic group. In some embodiments, R 1-6 is C(CH3)2OH. s4 is C(CH3)2OH.

[0855] In some embodiments, R s2is R as described in this specification s In some embodiments, R s2 is R' as described in this specification. In some embodiments, R s2 is R as described in this specification. In some embodiments, R s2 is -H. In some embodiments, R s2 is an optionally substituted C 1-6 aliphatic group. In some embodiments, R s2 is an optionally substituted C 1-6 alkyl.

[0856] In some embodiments, R s3 is R as described in this specification s In some embodiments, R s3 is R' as described in this specification. In some embodiments, R s3 is R as described in this specification. In some embodiments, R s3 is -H. In some embodiments, R s3 is an optionally substituted C 1-6 aliphatic. In some embodiments, R s3 is an optionally substituted C 1-6 alkyl.

[0857] In some embodiments, R s2 and R s3 are each independently R as described in this specification. In some embodiments, both are -H. In some embodiments, each is independently -H or a C 1-6 aliphatic group. In some embodiments, each is independently an optionally substituted C 1-6 aliphatic group. In some embodiments, each is independently an optionally substituted C 1-6 alkyl. In some embodiments, R s2 and R s3 are the same. In some embodiments, R s2 and R s3 are different. In some embodiments, R s2 and R s3Both are methyl. In some embodiments, R s2 is -H and R s3 is methyl.

[0858] In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 3-8, 4-10, 5-10, 5-9, 5-8, 5-7, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated or partially unsaturated ring having 0 to 4 (e.g., 1-4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form an optionally substituted 3- to 6-membered saturated or partially unsaturated carbocyclic ring. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form an optionally substituted 3- to 6-membered saturated or partially unsaturated ring having 1 to 4 heteroatoms. In some embodiments, the heteroatom is nitrogen. In some embodiments, the heteroatom is oxygen. In some embodiments, the heteroatom is sulfur. In some embodiments, the formed ring is saturated. In some embodiments, the formed ring is partially unsaturated. In some embodiments, the formed ring is 3-membered. In some embodiments, the formed ring is 4-membered. In some embodiments, the formed ring is 5-membered. In some embodiments, the formed ring is 6-membered. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form an optionally substituted cyclopropyl ring. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form a cyclopropyl ring. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form a cyclobutyl ring. In some embodiments, Rs2 and R s3 together with the carbon atom to which they are attached form a cyclopentyl ring. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form a cyclohexyl ring. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form an optionally substituted 3- to 6-membered saturated ring having an oxygen atom. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form an optionally substituted

[0859]

Chemical formula

[0860] to form. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached

[0861]

Chemical formula

[0862] to form. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached form an optionally substituted

[0863]

Chemical formula

[0864] to form. In some embodiments, R s2 and R s3 together with the carbon atom to which they are attached

[0865]

Chemical formula

[0866] to form.

[0867] In some embodiments, L R is the L described herein. In some embodiments, L R is -C≡C-. In some embodiments, L R is optionally substituted -CH=CH-. In some embodiments, L R is -C(O)-. In some embodiments, L R is -C(S)-. In some embodiments, L R is -C(NR”), where R” is as described herein. In some embodiments, L R is a covalent bond. In some embodiments, L R is the L described herein. In some embodiments, L R is optionally substituted C 1-6 (e.g., C 1-4 , C1, C2, C3, C4, C5, C6, etc.) alkylene. In some embodiments, L R is optionally substituted C 2-6 (e.g., C2, C3, C4, C5, C6, etc.) alkenylene. In some embodiments, L R is optionally substituted C 2-6 (e.g., C2, C3, C4, C5, C6, etc.) alkynylene. In some embodiments, L R is -Cy- as described herein. In some embodiments, L R is optionally substituted C 3-10 (e.g., C 4-10 , C 5-10 , C3, C4, C5, C6, C7, C8, C9, C 10 , etc.) cycloalkylene. In some embodiments, L R is optionally substituted C 6-14 (e.g., C6, C 10etc.) is an arylene. In some embodiments, L R is an optionally substituted C 7-15 aralkylene. In some embodiments, L R is an optionally substituted 5- to 14- (e.g., 5- to 10-, 5- to 9-, 5, 6, 9, 10, 14, etc.) membered heteroarylene having 1 to 5 (e.g., 1 to 2, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, L R is an optionally substituted 3- to 14- (e.g., 3- to 20-, 5- to 10-, 5- to 10-, 5- to 6-, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, etc.) membered ring, or a heterocyclylene having 1 to 5 (e.g., 1 to 3, 1, 2, 3, 4, 5, etc.) heteroatoms. Ring L

[0868] In some embodiments, ring L is an optionally substituted monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms, as described herein. In some embodiments, ring L is the ring described herein, for example, in the section on ring A. In some embodiments, ring L is an optionally substituted monocyclic aromatic ring unit having 0 to 4 (e.g., 0 to 3, 2 to 4, 0, 1, 2, 3, 4, etc.) heteroatoms, or includes the same. In some embodiments, ring L is an optionally substituted monocyclic aromatic unit having 1 to 4 heteroatoms, or includes the same. In some embodiments, ring L contains -N=C*(-)-, where "*" represents the atom bonded to R 4 and "-N=C*(-)-N=" where "*" represents the atom bonded to R 4 . In some embodiments, ring L is

[0869] [Chemical formula]

[0870] . In some embodiments, ring L is

[0871]

Chem.

[0872] It is. Ring L is an optionally substituted bicyclic aromatic unit having 0 to 6 heteroatoms or includes it.

[0873] In some embodiments, ring L is an optionally substituted monocyclic, bicyclic or polycyclic ring having 1 to 10 (e.g., 2 to 10, 3 to 10, 2 to 5, 2 to 4, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, etc.) heteroatoms and having 5 to 20 (e.g., 5 to 15, 5 to 10, 5 to 9, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, etc.) members. In some embodiments, ring L is monocyclic. In some embodiments, ring L is bicyclic. In some embodiments, ring L is polycyclic. In some embodiments, ring L is an optionally substituted 6-membered monocyclic aromatic ring unit having 0 to 4 (e.g., 1 to 4, 0, 1, 2, 3, 4, etc.) heteroatoms or includes it. In some embodiments, ring L is an optionally substituted monocyclic non-aromatic ring unit having 0 to 4 (e.g., 1 to 4, 0, 1, 2, 3, 4, etc.) heteroatoms or includes it. In some embodiments, the monocyclic ring unit bonded to R 4 is an optionally substituted 5- to 6-membered heteroaryl ring having 1 to 5 (e.g., 1 to 4, 2 to 5, 2 to 4, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, the monocyclic ring unit bonded to R 4 is an optionally substituted 6-membered heteroaryl ring having 1 to 5 (e.g., 1 to 4, 2 to 5, 2 to 4, 1, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, the monocyclic ring unit bonded to R 4The monocyclic ring unit attached to is an optionally substituted 6-membered heteroaryl ring having 2 to 5 (e.g., 2 to 4, 2, 3, 4, 5, etc.) heteroatoms. In some embodiments, it has at least 1 nitrogen atom. In some embodiments, it has at least 2 nitrogen atoms. In some embodiments, ring L is bicyclic or polycyclic. In some embodiments, ring L comprises an optionally substituted partially unsaturated monocyclic ring unit. In some embodiments, ring L comprises a 3- to 10- (e.g., 5- to 10-, 5- to 10-, 5- to 6-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered partially unsaturated ring having 0 to 6 (e.g., 1 to 6, 1 to 3, 0, 1, 2, 3, 4, 5, 6, etc.) heteroatoms. In some embodiments, ring L comprises a 5- to 6-membered partially unsaturated ring having 1 to 3 (e.g., 1 to 2, 1, 2, 3, etc.) heteroatoms. In some embodiments, the unsaturation is due to fusion to a monocyclic ring unit attached to . In some embodiments, in addition to the monocyclic ring unit attached to , ring L comprises a monocyclic ring unit that is a monocyclic aromatic ring unit. In some embodiments, such a monocyclic aromatic unit is an optionally substituted 5- to 6-membered aromatic ring having 0 to 4 (e.g., 1 to 4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, such a monocyclic aromatic unit is an optionally substituted 5-membered heteroaryl having 1 to 4 (e.g., 1 to 4, 1 to 3, 1 to 2, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, at least 1 heteroatom is nitrogen. In some embodiments, each heteroatom is nitrogen. 4 and is due to fusion to a monocyclic ring unit attached to . In some embodiments, 4 In addition to the monocyclic ring unit attached to , ring L comprises a monocyclic ring unit that is a monocyclic aromatic ring unit. In some embodiments, such a monocyclic aromatic unit is an optionally substituted 5- to 6-membered aromatic ring having 0 to 4 (e.g., 1 to 4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, such a monocyclic aromatic unit is an optionally substituted 5-membered heteroaryl having 1 to 4 (e.g., 1 to 4, 1 to 3, 1 to 2, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, at least 1 heteroatom is nitrogen. In some embodiments, each heteroatom is nitrogen.

[0874] In some embodiments, ring L is or comprises an optionally substituted bicyclic aromatic unit having 0 to 6 heteroatoms. In some embodiments, ring L is or comprises an optionally substituted 9-membered bicyclic aromatic unit having 0 to 6 heteroatoms.

[0875] In some embodiments, ring L is optionally substituted

[0876]

Chem.

[0877] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0878]

Chem.

[0879] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0880]

Chem.

[0881] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0882]

Chem.

[0883] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0884]

Chem.

[0885] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0886] [Chemistry]

[0887] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0888] [Chemistry]

[0889] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0890] [Chemistry]

[0891] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0892] [Chemistry]

[0893] and wherein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0894] [Chemistry]

[0895] and wherein "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0896] [Chemistry]

[0897] and here, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0898]

Chemical formula

[0899] and here, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0900]

Chemical formula

[0901] and here, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0902]

Chemical formula

[0903] and here, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0904]

Chemical formula

[0905] and here, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0906]

Chemical formula

[0907] and herein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0908]

Chemical formula

[0909] and herein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0910]

Chemical formula

[0911] and herein, "*" represents an atom bonded to R 4 In some embodiments, ring L is optionally substituted

[0912]

Chemical formula

[0913] and the nitrogen atom is bonded to R 4 In some embodiments, ring L is a monocyclic ring unit not bonded to R

[0914] In some embodiments, ring L is bonded to L 4 by a monocyclic ring unit not bonded to R b In some embodiments, L L b

[0915] In some embodiments, L b is the L described herein. In some embodiments, L b is -L b1 -L b2 -L b3 -L b4 -L b5 - and herein, L b1 L b2 L b3 Lb4 and L b5 is, independently, L’ as described herein. In some embodiments, L b1 is attached to ring L.

[0916] In some embodiments, L b is -C(R’)2-N(R’)-C(O)-, where each R’ is independently as described herein. In some embodiments, L b is -C(R’)2-N(R’)-C(O)-C≡C-, where each R’ is independently as described herein. In some embodiments, L b is -C(R’)2-N(R’)-C(O)-C(R’)2-OS(O)2-, where each R’ is independently as described herein. In some embodiments, L b is -C(R’)2-N(R’)-C(O)-C(R’)2-OS(O)2-O-, where each R’ is independently as described herein. In some embodiments, -C(R’) 2 - is attached to L R In some embodiments, L b is -CH2-N(R’)-C(O)-, where -CH2- is optionally substituted and R’ is as described herein. In some embodiments, L b is -CH2-N(R’)-C(O)-C≡C-, where -CH2- is optionally substituted and R’ is as described herein. In some embodiments, L b is -CH2-N(R’)-C(O)-C(R’)2-OS(O)2-, where -CH2- is optionally substituted and each R’ is independently as described herein. In some embodiments, L b is -CH2-N(R’)-C(O)-C(R’)2-OS(O)2-O-, where -CH2- is optionally substituted and each R’ is independently as described herein. In some embodiments, -CH2- is attached to L R In some embodiments, -L R -L b- does not include -C(R’)2-N(R’)-C(O)-C≡C-, where each R’ is independently as described herein. In some embodiments, -L R -L b - does not include -C(R’)2-N(R’)-C(O)-C(R’)2-OS(O)2-, where each R’ is independently as described herein. In some embodiments, -L R -L b - does not include -C(R’)2-N(R’)-C(O)-C(R’)2-OS(O)2-O-, where each R’ is independently as described herein. In some embodiments, -L R -L b - does not include -C(R’)2-N(R’)-C(O)-C(R’)2-, where each R’ is independently as described herein. In some embodiments, -C(R’)2- is R 4 is attached to.

[0917] In some embodiments, L b is -Cy- as described herein.

[0918] In some embodiments, L b is optionally substituted phenyl. In some embodiments, L b is phenyl optionally substituted with -OMe or a halogen (e.g., -F, -Cl, -Br, or -I). In some embodiments, L b is phenyl. In some embodiments, L b is

[0919]

Chemical formula

[0920] where " * " represents the point of attachment to L R In some embodiments, L b is phenyl. In some embodiments, L b is

[0921] [Chemical formula]

[0922] and where " * " represents the point of attachment to L R In some embodiments, L b is

[0923] [Chemical formula]

[0924] and where " * " represents the point of attachment to L R In some embodiments, R b is - H and L b is

[0925] [Chemical formula]

[0926] and where " * " represents the point of attachment to L R In some embodiments, R b is - H and L b is

[0927] [Chemical formula]

[0928] and where " * " represents the point of attachment to L R In some embodiments, L b is

[0929] [Chemical formula]

[0930] and where " * " represents the point of attachment to L R In some embodiments, L

[0931] In some embodiments, Lb is a divalent optionally substituted 5- or 6-membered heteroaryl ring having from 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms. In some embodiments, L b is a divalent optionally substituted 5- or 6-membered heteroaryl ring having 1 nitrogen heteroatom. In some embodiments, L b is divalent optionally substituted pyridinyl. In some embodiments, L b is divalent pyridinyl optionally substituted with a halogen (e.g., (-F, -Cl, -Br, or -I) or -OR°, where R° is C 1-6 is an aliphatic group (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl). In some embodiments, L b is

[0932]

Chemical formula

[0933] and where " * " represents the point of attachment to L R In some embodiments, L b is

[0934]

Chemical formula

[0935] and where " * " represents the point of attachment to L R In some embodiments, L b is divalent pyridinyl. In some embodiments, L b is

[0936]

Chemical formula

[0937] and where " * " represents the point of attachment to L R In some embodiments, L b is

[0938] [Chemical formula]

[0939] and wherein, "*" represents the point of attachment to L R In some embodiments, L b is a divalent optionally substituted 5- or 6-membered heteroaryl ring having two nitrogen heteroatoms. In some embodiments, L b is a divalent optionally substituted pyrimidinyl. In some embodiments, L b is a divalent pyrimidinyl. In some embodiments, L b is

[0940] [Chemical formula]

[0941] and wherein "*" represents the point of attachment to L R In some embodiments, L b is a divalent optionally substituted pyridazinyl. In some embodiments, L b is a divalent pyridazinyl. In some embodiments, L b is

[0942] [Chemical formula]

[0943] and wherein "*" represents the point of attachment to L R In some embodiments, L b is a divalent optionally substituted 5- or 6-membered heteroaryl ring having one nitrogen and one sulfur heteroatom. In some embodiments, L b is a divalent optionally substituted thiazolyl. In some embodiments, L b is a divalent thiazolyl. In some embodiments, L bis

[0944]

Chem.

[0945] and here "*" represents the bonding point to L R represents the bonding point to L

[0946] In some embodiments, L b is a divalent optionally substituted 6- to 12-membered cycloalkyl ring. In some embodiments, L b is a divalent optionally substituted 5- to 6-membered cycloalkyl ring. In some embodiments, L b is a divalent optionally substituted 6-membered cycloalkyl ring. In some embodiments, L b is a divalent optionally substituted 5-membered cycloalkyl ring. In some embodiments, L b is a divalent optionally substituted 5-membered cycloalkyl ring. In some embodiments, L b is C 1-6 an aliphatic (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl) or halogen (e.g., -F, -Cl, -Br, -I) optionally substituted divalent cyclohexanyl. In some embodiments, L b is

[0947]

Chem.

[0948] is

[0949] In some embodiments, L b is a divalent optionally substituted 6- to 12-membered heterocyclyl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms. In some embodiments, L bis a divalent optionally substituted 6- to 12-membered heterocyclyl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from nitrogen, oxygen, or sulfur. In some embodiments, L b is a divalent optionally substituted 9- to 10-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from nitrogen, oxygen, or sulfur. In some embodiments, L b is an optionally substituted divalent 9-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from nitrogen, oxygen, or sulfur. In some embodiments, L b is an optionally substituted divalent 9-membered heteroaryl ring having 1 oxygen heteroatom.

[0950] In some embodiments, L b is an optionally substituted divalent 2,3-dihydrobenzofuranyl. In some embodiments, L b is C 1-6 an optionally substituted divalent 2,3-dihydrobenzofuranyl with an aliphatic group (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl) or a halogen (e.g., -F, -Cl, -Br, -I). In some embodiments, L b is a divalent 2,3-dihydrobenzofuranyl. In some embodiments, L b is

[0951]

Chemical formula

[0952] wherein "*" represents the bonding point to L R . In some embodiments, R b is -H and L b is

[0953]

Chemical formula

[0954] and here, "*" represents the attachment point to L R represents the attachment point to L

[0955] In some embodiments, L b is a divalent optionally substituted 10-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from nitrogen, oxygen, or sulfur. In some embodiments, L b is a divalent optionally substituted 10-membered heteroaryl ring having one oxygen heteroatom. In some embodiments, L b is a divalent optionally substituted chromanyl. In some embodiments, R b is -H and L b is chromanyl. In some embodiments, R b is -H and L b is

[0956]

Chemical formula

[0957] is. In some embodiments, R b is -H and L b is

[0958]

Chemical formula

[0959] and here, "*" represents the attachment point to L R represents the attachment point to L

[0960] In some embodiments, L b is a divalent optionally substituted 10- to 15-membered tricyclic heterocyclyl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms. In some embodiments, L bis a divalent optionally substituted 10- to 15-membered tricyclic heterocyclyl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from oxygen, nitrogen, or sulfur. In some embodiments, L b is a divalent optionally substituted 10- to 15-membered tricyclic heterocyclyl having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from oxygen, nitrogen, or sulfur, wherein the tricyclic heterocyclyl comprises two spiro rings and two fused rings. In some embodiments, L b is a divalent optionally substituted 12-membered tricyclic heterocyclyl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from oxygen, nitrogen, or sulfur. In some embodiments, L b is a divalent optionally substituted spiro[chroman-4,1'-cyclopropyl. In some embodiments, L b is a divalent spiro[chroman-4,1'-cyclopropyl. In some embodiments, R b is -H, and L b is spiro[chroman-4,1'-cyclopropyl. In some embodiments, R b is -H, and L b is

[0961]

Chemical formula

[0962] is.

[0963] In some embodiments, L b is a divalent optionally substituted 6- to 12-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms. In some embodiments, L b is a divalent optionally substituted 6- to 12-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from nitrogen, oxygen, or sulfur. In some embodiments, L bis a divalent optionally substituted 9- to 10-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from nitrogen, oxygen, or sulfur. In some embodiments, L b is a divalent optionally substituted 9-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms selected from nitrogen, oxygen, or sulfur. In some embodiments, L b is a divalent optionally substituted 9-membered heteroaryl ring having two nitrogen heteroatoms.

[0964] In some embodiments, L b is a divalent optionally substituted imidazopyridinyl. In some embodiments, L b is a divalent optionally substituted imidazo[1,5-a]pyridinyl. In some embodiments, L b is C 1-6 a divalent imidazo[1,5-a]pyridinyl optionally substituted with aliphatic (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl) or halogen (e.g., -F, -Cl, -Br, -I). In some embodiments, L b is a divalent imidazo[1,5-a]pyridinyl. In some embodiments, L b is

[0965]

Chemical formula

[0966] wherein "*" represents the point of attachment to L R .

[0967] In some embodiments, L b is a divalent optionally substituted indazolyl. In some embodiments, L b is a divalent indazolyl, and C 1-6Optionally substituted with an aliphatic group (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl) or a halogen (e.g., -F, -Cl, -Br, -I). In some embodiments, L b is optionally substituted

[0968]

Chemical formula

[0969] and here, "*" represents the bonding point to L R In some embodiments, L b is optionally substituted

[0970]

Chemical formula

[0971] and here, "*" represents the bonding point to L R In some embodiments, L

[0972] In some embodiments, L b is a divalent optionally substituted benzimidazolyl group. In some embodiments, L b is a divalent optionally substituted benzo[d]imidazolyl group. In some embodiments, L b is a C 1-6 divalent benzo[d]imidazolyl group optionally substituted with an aliphatic group (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl) or a halogen (e.g., -F, -Cl, -Br, -I). In some embodiments, L b is optionally substituted

[0973]

Chemical formula

[0974] and here, "*" represents the bonding point to L R In some embodiments, L bis optionally substituted

[0975] [Chemical formula]

[0976] and wherein "*" represents the point of attachment to L R In some embodiments, L b is optionally substituted

[0977] [Chemical formula]

[0978] and wherein "*" represents the point of attachment to L R In some embodiments, L b is optionally substituted

[0979] [Chemical formula]

[0980] and wherein "*" represents the point of attachment to L R In some embodiments, L

[0981] In some embodiments, L b is a divalent optionally substituted 9-membered heteroaryl ring having three nitrogen heteroatoms. In some embodiments, L b is an optionally substituted divalent pyrazolylpyrimidinyl. In some embodiments, L b is an optionally substituted divalent pyrazolyl[1,5-a]pyrimidinyl. In some embodiments, L b is a C 1-6 aliphatic group (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl) or halogen (e.g., -F, -Cl, -Br, -I) optionally substituted divalent pyrazolyl[1,5-a]pyrimidinyl. In some embodiments, L b is optionally substituted

[0982]

Chem.

[0983] and wherein "*" represents a point of attachment to L R In some embodiments, L b is

[0984]

Chem.

[0985] and wherein "*" represents a point of attachment to L R In some embodiments, L

[0986] In some embodiments, L b is *-N(R’)-Cy-, wherein "*" represents a point of attachment to L R In some embodiments, L b is *-N(H)-Cy-, wherein "*" represents a point of attachment to L R In some embodiments, L b is

[0987]

Chem.

[0988] In some embodiments, L b is

[0989]

Chem.

[0990] In some embodiments, L b is

[0991]

Chem.

[0992] is as follows. L b1

[0993] In some embodiments, L b1 is the L' described herein. In some embodiments, L b1 is a covalent bond. In some embodiments, L b1 is not a covalent bond. In some embodiments, L b1 is optionally substituted -CH2- or includes it. In some embodiments, L b1 is -CH2- or includes it. In some embodiments, L b1 is -C(R')2- or includes it, where each R' is independently as described herein. In some embodiments, the two R's of -C(R')2- together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated or partially unsaturated ring having 0 to 4 (e.g., 1-4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, the two R's of -C(R')2- together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated ring having 0 to 2 (e.g., 1-2, 0, 1, 2, etc.) heteroatoms. In some embodiments, L b1 is -CHR'- or includes it, where R' is as described herein. In some embodiments, L b1 is -CHR'- or includes it, where R' is optionally substituted aryl or heteroaryl. In some embodiments, L b1 is -CHR'- or includes it, where R' is optionally substituted phenyl. In some embodiments, L b1 is -N(R')- or includes it, where R' is as described herein. In some embodiments, L b1is -NH- or includes it. In some embodiments, L b1 is -C(O)- or includes it. In some embodiments, L b1 is -Cy- as described herein or includes it. In some embodiments, L b1 is -Cy- or includes it, where -Cy- is an optionally substituted divalent saturated or partially unsaturated 3- to 7- (e.g., 3- to 6-, 3, 4, 5, 6, 7, etc.) membered ring having 0 to 2 (e.g., 1 to 2, 0, 1, 2, etc.) heteroatoms. In some embodiments, L b1 is -Cy- or includes it, where -Cy- is an optionally substituted divalent saturated 6-membered ring having 1 to 2 heteroatoms which are nitrogen. L b2

[0994] In some embodiments, L b2 is L’ as described herein. In some embodiments, L b2 is a covalent bond. In some embodiments, L b2 is not a covalent bond. In some embodiments, Lb2 is optionally substituted -CH2- or includes it. In some embodiments, L b2 is -CH2- or includes it. In some embodiments, L b2is -C(R’)2- or includes it, where each R’ is independently as described herein. In some embodiments, two R’s of -C(R’)2 together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated or partially unsaturated ring having 0 to 4 (e.g., 1-4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, two R’s of -C(R’)2 together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated ring having 0 to 2 (e.g., 1-2, 0, 1, 2, etc.) heteroatoms. In some embodiments, L b2 is -CHR’- or includes it, where R’ is as described herein. In some embodiments, L b2 is -CHR’- or includes it, where R’ is optionally substituted aryl or heteroaryl. In some embodiments, L b2 is -CHR’- or includes it, where R’ is optionally substituted phenyl. In some embodiments, L b2 is -N(R’)- or includes it, where R’ is as described herein. In some embodiments, L b2is -N(R’)- or includes it, where R’ is an optionally substituted ring, for example, a cycloaliphatic group (for example, an optionally substituted saturated or partially unsaturated 3- to 10-membered ring (for example, 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) cycloaliphatic), a cycloheteroaliphatic group (for example, an optionally substituted saturated or partially unsaturated 3- to 10-membered ring (for example, 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) ring having 1 to 4 (for example, 1-3, 1, 2, 3, 4, etc.) heteroatoms), an aryl (for example, an optionally substituted 6- to 10-membered ring), or includes it. (For example, 6, 8, 9, 10, etc.) aryl, heteroaryl (for example, an optionally substituted 5- to 10-membered (for example, 5-6, 5-9, 5, 7, 8, 9, 10, etc.) heteroaryl having 1 to 4 (for example, 1-3, 1, 2, 3, 4, etc.) heteroatoms), etc. In some embodiments, L b2 is -N(R’)- or includes it, where R’ is an optionally substituted 5- to 10-membered (for example, 6-10, 5-9, 5, 6, 7, 8, 9, 10, etc.) aryl or a heteroaryl having 0 to 4 (for example, 1-4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, L b2 is -N(R’)-, and R’ is an optionally substituted phenyl. In some embodiments, L b2 is -NH- or includes it. In some embodiments, L b2 is -C(O)N(R’)- or includes it. Here, R’ is as described herein. In some embodiments, L b2 is -C(O)N(R’)- or includes it. Here, R’ is an optionally substituted 5- to 10- (for example, 6-10, 5-9, 5, 6, 7, 8, 9, 10, etc.) membered aryl or a heteroaryl having 0 to 4 (for example, 1-4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, L b2 is -C(O)N(R’)- or includes it. Here, R’ is an optionally substituted phenyl. In some embodiments, L b2 is -C(O)NH- or includes it. In some embodiments, L b2is -C(O)- or contains it. In some embodiments, L b2 is, as described herein, -Cy- or contains it. In some embodiments, L b2 is, as described herein, -Cy- or contains it. In some embodiments, L b2 is -Cy- or contains it, where -Cy- is an optionally substituted divalent saturated or partially unsaturated 3- to 7- (e.g., 3- to 6-, 3, 4, 5, 6, 7, etc.) membered ring having 0 to 2 (e.g., 1 to 2, 0, 1, 2, etc.) heteroatoms. In some embodiments, L b2is -Cy- or contains it, where -Cy- is an optionally substituted divalent saturated 6-membered ring having 1 to 2 heteroatoms which are nitrogen. In some embodiments, -Cy- is an optionally substituted bicyclic ring, where at least one monocyclic ring is an optionally substituted phenyl ring. In some embodiments, -Cy- is an optionally substituted bicyclic ring, where at least one monocyclic ring is an optionally substituted 5- to 6-membered heteroaryl ring having 1 to 3 (e.g., 1 to 2, 1, 2, 3, etc.) heteroatoms. In some embodiments, -Cy- is an optionally substituted bicyclic ring, where each monocyclic ring is independently an optionally substituted phenyl or 5- to 6-membered heteroaryl ring having 1 to 3 (e.g., 1 to 2, 1, 2, 3, etc.) heteroatoms. In some embodiments, -Cy- is an optionally substituted bicyclic ring, where one monocyclic ring is an optionally substituted phenyl or 5- to 6-membered heteroaryl ring having 1 to 3 (e.g., 1 to 2, 1, 2, 3, etc.) heteroatoms, and the other monocyclic ring is an optionally substituted non-aromatic 3- to 10 (e.g., 3 to 9, 4 to 10, 5 to 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered ring having 1 to 4 (e.g., 1 to 2, 1 to 3, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, -Cy- is an optionally substituted divalent cyclic aliphatic ring having 3 to 10 (e.g., 3 to 9, 5 to 10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) members. In some embodiments, -Cy- is an optionally substituted 6-membered cycloalkyl ring. In some embodiments, -Cy- is an optionally substituted phenylene. In some embodiments, -Cy- is an optionally substituted 1,4-phenylene. In some embodiments, -Cy- is 1,4-phenylene.In some embodiments, -Cy- is an optionally substituted divalent cyclohexyl. In some embodiments, -Cy- is an optionally substituted 1,4-cyclohexyl. In some embodiments, -Cy- is 1,4-cyclohexyl. In some embodiments, -Cy- is an optionally substituted divalent piperidyl ring. In some embodiments, -Cy- is a divalent piperidyl ring. In some embodiments, the divalent piperidyl ring is 2-valent 1,2-piperidyl. In some embodiments, the divalent piperidyl ring is L at 1'. b1 is bonded to. In some embodiments, the divalent piperidyl ring is 2-valent 1,4-piperidyl. In some embodiments, -Cy- is an optionally substituted divalent piperazinyl ring. In some embodiments, -Cy- is a divalent piperazinyl ring. In some embodiments, the divalent piperidyl ring is 2-valent 1,2-piperazinyl. In some embodiments, the divalent piperidyl ring is 2-valent 1,4-piperazinyl. In some embodiments, -Cy- is an optionally substituted 5- to 6-membered divalent heteroaryl ring. In some embodiments, -Cy- is an optionally substituted 5-membered divalent heteroaryl ring. In some embodiments, -Cy- is an optionally substituted 6-membered divalent heteroaryl ring having one or three nitrogen atoms. In some embodiments, -Cy- is an optionally substituted 6-membered divalent heteroaryl ring having a nitrogen atom. In some embodiments, -Cy- is an optionally substituted divalent pyridinyl ring. In some embodiments, -Cy- is a divalent pyridinyl ring. In some embodiments, the divalent pyridinyl ring is 2,5-2-valent pyridinyl. In some embodiments, the divalent pyridinyl ring is L at 2'. b1 is bonded to. In some embodiments, the divalent pyridinyl ring is L at 5'. b1 is bonded to. In some embodiments, the divalent pyridinyl ring is 3,5-2-valent pyridinyl. In some embodiments, the divalent pyridinyl ring is L at 3'. b1 is bonded to. In some embodiments, the divalent pyridinyl ring is L at 5'. b1 is bonded to. Lb3

[0995] In some embodiments, L b3 is the L’ described herein. In some embodiments, L b3 is a covalent bond. In some embodiments, L b3 is not a covalent bond. In some embodiments, L b3 is optionally substituted -CH2- or includes it. In some embodiments, L b3 is -CH2- or includes it. In some embodiments, L b3 is -C(R’)2- or includes it, where each R’ is independently as described herein. In some embodiments, the two R’s of -C(R’)2- together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3- to 9-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated or partially unsaturated ring having 0 to 4 (e.g., 1 to 4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, the two R’s of -C(R’)2- together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3- to 9-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated ring having 0 to 2 (e.g., 1 to 2, 0, 1, 2, etc.) heteroatoms. In some embodiments, L b3 is -CHR’- or includes it, where R’ is as described herein. In some embodiments, L b3 is -CHR’- or includes it, where R’ is optionally substituted aryl or heteroaryl. In some embodiments, L b3 is -CHR’- or includes it, where R’ is optionally substituted phenyl. In some embodiments, L b3 is -N(R’)- or includes it, where R’ is as described herein. In some embodiments, L b3 is -NH- or includes it. In some embodiments, L b3is -C(O)- or includes it. In some embodiments, L b3 is -Cy- as described herein or includes it. In some embodiments, L b3 is -O- or includes it. In some embodiments, L b3 is -S- or includes it. L b4

[0996] In some embodiments, L b4 is L’ as described herein. In some embodiments, L b4 is a covalent bond. In some embodiments, L b4 is not a covalent bond. In some embodiments, L b4 is -C≡C-. In some embodiments, L b4 is optionally substituted -CH2- or includes it. In some embodiments, L b4 is -CH2- or includes it. In some embodiments, L b4 is optionally substituted -CH2-O- or includes it. In some embodiments, L b4 is -CH2-O- or includes it. In some embodiments, L b4 is -C(R’)2- or includes it, where each R’ is independently as described herein. In some embodiments, two R’s of -C(R’)2- together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated or partially unsaturated ring having 0 to 4 (e.g., 1-4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, two R’s of -C(R’)2- together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated ring having 0 to 2 (e.g., 1-2, 0, 1, 2, etc.) heteroatoms. In some embodiments, L b4is -CHR'- or includes it, where R' is as described herein. In some embodiments, L b4 is -CHR'- or includes it, where R' is optionally substituted aryl or heteroaryl. In some embodiments, L b4 is -CHR'- or includes it, where R' is optionally substituted phenyl. In some embodiments, L b4 is -N(R')- or includes it, where R' is as described herein. In some embodiments, L b4 is -NH- or includes it. In some embodiments, L b4 is, -C(O)- or includes it. In some embodiments, L b4is -Cy- as described herein or includes it. In some embodiments, -Cy- is an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered divalent cycloaliphatic ring. In some embodiments, -Cy- is an optionally substituted 6-membered cycloalkyl ring. In some embodiments, -Cy- is an optionally substituted divalent cyclohexyl. In some embodiments, -Cy- is an optionally substituted 3- to 10- (e.g., 4- to 10-, 5- to 10-, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered divalent heterocyclyl ring having 1 to 3 (e.g., 1 to 2, 1, 2, 3, etc.) heteroatoms. In some embodiments, -Cy- is an optionally substituted 6-membered divalent heterocyclyl ring having 1 to 3 (e.g., 1 to 2, 1, 2, 3, etc.) heteroatoms. In some embodiments, -Cy- is an optionally substituted 5-membered divalent heterocyclyl ring having 1 or 2 heteroatoms. In some embodiments, -Cy- is an optionally substituted saturated ring. In some embodiments, -Cy- is an optionally substituted 5- to 6-membered divalent heteroaryl ring having 1 to 3 (e.g., 1 to 2, 1, 2, 3, etc.) heteroatoms. In some embodiments, -Cy- is an optionally substituted divalent phenylene. In some embodiments, -Cy- is an optionally substituted divalent 1,4-phenylene. In some embodiments, -Cy- is divalent 1,4-phenylene. In some embodiments, -Cy- is an optionally substituted divalent naphthyl. In some embodiments, L b4 is -O- or includes it. In some embodiments, L b4 is -S- or includes it. L b5

[0997] In some embodiments, L b5 is L’ as described herein. In some embodiments, L b5 is a covalent bond. In some embodiments, L b5 is not a covalent bond. In some embodiments, Lb5 is optionally substituted -CH2- or includes it. In some embodiments, L b5 is -CH2- or includes it. In some embodiments, L b5 is optionally substituted -CH2O- or includes it. In some embodiments, L b5 is -CH2O- or includes it. In some embodiments, L b5 is -C(R’)2- or includes it, where each R’ is as described herein. In some embodiments, two R’s of -C(R’)2- together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated or partially unsaturated ring having 0 to 4 (e.g., 1-4, 0, 1, 2, 3, 4, etc.) heteroatoms. In some embodiments, two R’s of -C(R’)2- together with the carbon atom to which they are attached form an optionally substituted 3- to 10- (e.g., 3-9, 5-10, 3, 4, 5, 6, 7, 8, 9, 10, etc.) membered saturated ring having 0 to 2 (e.g., 1-2, 0, 1, 2, etc.) heteroatoms. In some embodiments, L b5 is -CHR’- or includes it, where R’ is as described herein. In some embodiments, L b5 is -CHR’- or includes it, where R’ is optionally substituted aryl or heteroaryl. In some embodiments, L b5 is -CHR’- or includes it, where R’ is optionally substituted phenyl. In some embodiments, L b5 is -N(R’)- or includes it, where R’ is as described herein. In some embodiments, L b5 is -NH- or includes it. In some embodiments, L b5 is -C(O)- or includes it. In some embodiments, L b5 is -Cy- or includes it as described herein. In some embodiments, L b5is -O- or contains it. In some embodiments, L b5 is -S- or contains it. In some embodiments, L b5 is -S(O)2- or contains it. In some embodiments, L b5 is -OS(O)2- or contains it. L’

[0998] In some embodiments, L’ is a covalent bond or an optionally substituted divalent C 1-2 aliphatic or heteroaliphatic group having 1 to 2 heteroatoms, wherein one or more methylene units are optionally and independently -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)--N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-substituted. In some embodiments, L’ is a covalent bond. In some embodiments, L’ is an optionally substituted divalent C 1-2 aliphatic or heteroaliphatic group having 1 to 2 heteroatoms, wherein one or more methylene units are optionally and independently -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O)N(R’)-, O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)--N(R’)C(O)N(R’)-, -N(R’)C(O)O-, -S(O)-, -S(O)2-, -S(O)2N(R’)-, -C(O)S-, or -C(O)O-substituted. In some embodiments, L’ is an optionally substituted divalent C 1-2 aliphatic group. In some embodiments, L’ is an optionally substituted divalent C 1-2is an alkylene, where one or more methylene units are optionally and independently replaced by -C(R’)2-, -Cy-, -O-, -S-, -N(R’)-, -C(O)-, -C(S)-, -C(NR’)-, -C(O...

Claims

1. A compound having the structure of formula B-1, or a salt thereof: 【Chemical 1】 Wherein, L ｂ is L and R ｂ is R'', and R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ wherein L ｗ is a covalent bond or an optionally substituted divalent C １－６ aliphatic group or heteroaliphatic group having 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently selected from the group consisting of -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-; R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ )(R ｗ３ ), and R ｗ１ 、R ｗ２ 、and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, Each R″ is independently hydrogen, halogen, -L-R′, -L-OR′, -L-SR′, -L-C(O)OR′, -L-C(O)SR′, -L-C(O)N(R′) ２ , -L-OC(O)N(R′) ２ , -L-C(O)R′, -L-N(R′) ２ , -CN, -OC(R′) ２ COOH, -SC(R′) ２ COOH, -N(R′)C(R′) ２ COOH, or an optionally substituted group selected from an alkylsulfonyl group, an arylsulfonyl group, a carboxylic acid ester group, an ester group, an ether group, an amide group, a carbohydrate group, an amino acid group, an acyl group, an acyl group substituted with an alkoxy, an alditol group, a sulfate ester group, a sulfonamide group, a sulfoxide group, a sulfonic acid ester group, a sulfone group, a thioalkyl group, a thioester group, and a thioether group, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic group or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- Each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms, Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ , a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ , a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or Two R groups are optionally and independently covalently bonded to each other, or Two or more R groups on the same atom are optionally and independently together with the atom to form an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms in addition to the atom, or Two or more R groups on two or more atoms are optionally and independently together with their intervening atoms to form an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 30 members having 0 to 10 heteroatoms in addition to the intervening atoms, R ｓ１ , R ｓ２ and R ｓ３ are each independently R", halogen, -CN, an oxo group, -NO ２ or an optionally substituted group selected from the group consisting of an acyl group, an acylamino group, a hydroxyl group, an amino acid group, an amine group, an amide group, a carbamate group, an ester group, an ether group, a carboxylic acid group, a thio group, a thioalkyl group, a thioester group, a thioether group, a sulfate ester group, a sulfonamide group, a sulfoxide group, a sulfonate ester group, a sulfone group, an alkylsulfonyl group and an arylsulfonyl group.

2. A compound having the structure of formula B, or a salt thereof: [Chemical 2] Wherein, L Ｒ is 【Chemical 3】 , L, -C≡C-, optionally substituted -CH=CH-, -C(O)-, -C(S)-, or -C(NR'')-, L ｂ is L and R ｂ is R", Ring L is an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms. R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ wherein L ｗ is a covalent bond, or an optionally substituted divalent C １－６ aliphatic group or heteroaliphatic group having 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-; R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ )(R ｗ３ ) and R ｗ１ 、R ｗ２ 、and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, Each R ｓ is independently an optionally substituted group selected from R'', halogen, -CN, oxo, -NO ２ , or an acyl group, acylamino group, hydroxy group, amino acid group, amine group, amide group, carbamate group, ester group, ether group, carboxylic acid group, thio group, thioalkyl group, thioester group, thioether group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, alkylsulfonyl group, and arylsulfonyl group, q is 0 to 10, Each R″ is independently hydrogen, halogen, —L—R′, —L—OR′, —L—SR′, —L—C(O)OR′, —L—C(O)SR′, —L—C(O)N(R′) ２ , —L—OC(O)N(R′) ２ , —L—C(O)R′, —L—N(R′) ２ , —CN, —OC(R′) ２ COOH, —SC(R′) ２ COOH, —N(R′)C(R′) ２ COOH, or an optionally substituted group selected from an alkylsulfonyl group, an arylsulfonyl group, a carboxylic acid ester group, an ester group, an ether group, an amide group, a carbohydrate group, an amino acid group, an acyl group, an acyl group substituted with an alkoxy, an alditol group, a sulfate ester group, a sulfonamide group, a sulfoxide group, a sulfonic acid ester group, a sulfone group, a thioalkyl group, a thioester group, and a thioether group, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-, Each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms, Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ having 1 to 10 heteroatoms, a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or Two R groups are optionally and independently covalently bonded to each other, or Two or more R groups on the same atom are optionally and independently together with the atom to form an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 20 members having 0 to 10 heteroatoms in addition to the atom, or Two or more R groups on two or more atoms are optionally and independently together with their intervening atoms to form an optionally substituted monocyclic, bicyclic or polycyclic ring of 3 to 30 members having 0 to 10 heteroatoms.

3. L Ｒ is [Chemical Formula 4] The compound according to claim 2, wherein it is

4. L Ｒ is optionally substituted [Chemical Formula 5] , here, the nitrogen atom is bonded to L ｂ and L Ｒ is optionally substituted 【Chemical Formula 6】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical Formula 7】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical Formula 8】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical Formula 9】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical Formula 10】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical 11】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical 12】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical 13】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical Formula 14】 , where "*" represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is 【Chemical 15】 and here, the nitrogen atom is bonded to L ｂ wherein, R ｓ１ R ｓ２ and R ｓ３ are each independently R ｓ or, L Ｒ is 【Chemical 16】 and here, the nitrogen atom is bonded to L ｂ wherein, R ｓ１ , R ｓ２ and R ｓ３ are each independently R ｓ respectively. The compound according to claim 2, characterized in that

5. The compound is a compound having the structure of B-1a, B-1b, B-1c, or B-1d, or a salt thereof: 【Chemical 17】 The compound is a compound having the structure of B-2a, B-2b, B-2c, B-2d, or B-2e, or a salt thereof: 【Chemical Formula 18】 The compound is a compound having a structure of B-3a, B-3b, B-3c, or B-3d, or a salt thereof: 【Chemical Formula 19】 The compound is a compound having a structure of B-4a, B-4b, B-4c, or B-4d, or a salt thereof: 【Chemical 20】 The compound is a compound having a structure of B-5a, B-5b, B-5c, or B-5d, or a salt thereof: 【Chemical 21】 However, the compound is a compound having a structure of B-6a, B-6b, B-6c, or B-6d, or a salt thereof: 【Chemical 22】 However, the compound is a compound having a structure of B-7a, B-7b, B-7c, or B-7d, or a salt thereof: 【Chemical 23】 The compound according to claim 1 or 2, characterized in that:

6. R ｓ１ is -N(R') ２ , -OR, an optionally substituted C １－６ aliphatic group (e.g., -CF ３ or CHF ２ ), or a halogen The compound according to any one of claims 1 to 5, characterized in that:

7. R ｓ１ is -H, -NH ２ , -Cl, -NHCH ３ , -CHF ２ , -CF ３ , -NHCD ３ , -NHCH ２ CH ３ , -NHCH ２ CH ２ CH ３ , -NHCH(CH ３ ) ２ , -N(CH ３ ) ２ , -NHCH ２ CF ３ , -NHCH ２ CHF ２ , -NHCH ２ CH=CH ２ , -OH, -OCH ３ , 【Chemical Formula 24】 is The compound according to any one of claims 1 to 5, characterized in that:

8. R ｓ２ and R ｓ３ each independently is -H, or an optionally substituted C １－６ aliphatic group The compound according to any one of claims 1 to 7, characterized in that:

9. R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached form an optionally substituted 3- to 10-membered saturated or partially unsaturated ring having 0 to 4 heteroatoms, an optionally substituted 3- to 6-membered saturated or partially unsaturated carbocyclic ring, or an optionally substituted 3- to 6-membered saturated or partially unsaturated ring having 1 to 4 heteroatoms, The compound according to any one of claims 1 to 7, characterized in that:

10. R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached form an optionally substituted cyclopropyl ring, R ｓ２ and R ｓ３ together with the carbon atom to which they are attached form a cyclopropyl ring, Here, R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached form an optionally substituted cyclobutyl ring, R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached form an optionally substituted cyclopentyl ring, R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached form a cyclopentyl ring, R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached form an optionally substituted cyclohexyl ring, R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached form a cyclohexyl ring, R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached, are optionally substituted 【Chemical Formula 25】 forming R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached, 【Chemical 26】 forming R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached, are optionally substituted 【Chemical 27】 forming, or R ｓ２ and R ｓ３ together with the carbon atoms to which they are attached, 【Chemical formula 28】 forming The compound according to claim 9, characterized in that:

11. L Ｒ is 【Chemical Formula 29】 wherein "*" represents an atom bonded to R ４ and indicates an atom bonded to R ｓ１ is R ｓ and Z' is -N= or -C(R ｓ４ )= and "Z" is -N=, or -C(R ｓ５ )=, and R ｓ４ and R ｓ５ each is independently R ｓ is, The compound according to claim 2, characterized in that:

12. L Ｒ is 【Chemical 30】 and wherein "*" represents an atom bonded to R ４ or L Ｒ is 【Chemical Formula 31】 wherein "*" represents an atom bonded to R ４ indicating an atom bonded to The compound according to claim 11, characterized in that:

13. R ｓ１ is -N(R') ２ or -OR, or R ｓ１ is -H, -NH ２ or -NHCH ３ and is The compound according to any one of claims 11 to 12, characterized in that:

14. R ｓ４ is an optionally substituted group selected from -H, -halogen, -CN, -N(R') ２ (for example, -NH ２ ), or a C １－１０ aliphatic group, a C １－１０ heteroaliphatic group having 1 to 5 heteroatoms, a 6- to 10-membered aryl group, a 5- to 10-membered heteroaryl group having 1 to 4 heteroatoms, and a 3- to 10-membered heterocyclyl group having 1 to 5 heteroatoms The compound according to any one of claims 11 to 13, characterized in that:

15. R ｓ４ is optionally substituted -OCH(CH ３ ) ２ , 【Chemical 32】 is The compound according to claim 11 or 12, characterized in that:

16. R ｓ５ is selected from -H, -halogen (e.g., -F), -N(R') ２ (e.g., -NH ２ or -NHCH ３ ), -OR (e.g., or -OH or -OCH ３ ), or C １－１０ an optionally substituted group selected from an aliphatic group, a C heterofatty group having 1 to 5 heteroatoms, a C １－１０ aryl group, a 5- to 8-membered heteroaryl group having 1 to 4 heteroatoms, and a 3- to 10-membered heterocyclyl group having 1 to 5 heteroatoms ５－８ ​ The compound according to any one of claims 11 to 15, characterized in that:

17. L Ｒ is optionally substituted 【Chemical 33】 wherein "*" represents an atom bonded to R ４ indicating an atom bonded to L Ｒ is optionally substituted 【Chemical Formula 34】 wherein "*" represents an atom bonded to R ４ indicating an atom bonded to L Ｒ is optionally substituted 【Chemical 35】 wherein "*" represents an atom bonded to R ４ indicating an atom bonded to L Ｒ is optionally substituted 【Chemical 36】 and where " * " represents an atom bonded to R ４ indicates an atom bonded to L Ｒ is optionally substituted 【Chemical 37】 where " * " represents an atom bonded to R ４ indicating an atom bonded to L Ｒ is optionally substituted 【Chemical Formula 38】 wherein "*" represents an atom bonded to R ４ represents an atom bonded to, or L Ｒ is optionally substituted 【Chemical Formula 39】 where " * " represents an atom bonded to R ４ indicating an atom bonded to The compound according to any one of claims 11 to 16, characterized in that:

18. The compound is in a tautomeric form bonded to the ring and containing =O, or in another tautomeric form where =O is present as -OH (for example, provided that -OH is R ｓ１ is). The compound according to any one of the preceding claims, characterized in that:

19. L Ｒ is a covalent bond, an optionally substituted C １－６ alkylene group, an optionally substituted methylene group, an optionally substituted C ２－６ alkenylene group, an optionally substituted C ２－６ alkynylene group, an optionally substituted C ３－１０ cycloalkylene group, an optionally substituted C ６－１４ arylene group, an optionally substituted C ７－１５ aralkylene group, a 5- to 14-membered heteroarylene group having 1 to 5 optionally substituted heteroatoms, or L Ｒ is a 3- to 14-membered heterocyclylene group having 1 to 5 optionally substituted heteroatoms, The compound according to claim 2, characterized in that:

20. L ｂ is - L ｂ１ -L ｂ２ -L ｂ３ -L ｂ４ -L ｂ５ - and, provided that L ｂ１ , L ｂ２ , L ｂ３ , L ｂ４ and L ｂ５ are each independently L', where each L' is independently a covalent bond or an optionally substituted divalent C １－２ aliphatic or heteroaliphatic group having 1 to 2 heteroatoms, and one or more methylene units are optionally and independently -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')--N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted, and L ｂ１ is attached to ring L The compound according to any one of the preceding claims, characterized in that:

21. L ｂ is -Cy- The compound according to any one of the preceding claims, characterized in that:

22. L ｂ is optionally substituted phenyl or an optionally substituted divalent 5- or 6-membered heteroaryl ring having 0 to 4 (e.g., 1 to 4, 0, 1, 2, 3, 4, etc.) heteroatoms The compound according to claim 21, characterized in that:

23. L ｂ is an optionally substituted phenyl group, pyridinyl group, pyridazinyl group, pyrimidinyl group, or thiazolyl group, The compound according to claim 21, characterized in that:

24. L ｂ is a phenyl group, pyridinyl group, pyridazinyl group, pyrimidinyl group, thiazolyl group optionally substituted with a halogen (e.g., (-F, -Cl, -Br, or -I) or -OR), provided that R is C １－６ an aliphatic group (e.g., methyl group, ethyl group, n-propyl group, s-propyl group, or isopropyl group). The compound according to claim 21, characterized in that:

25. L ｂ is 【Chemical Formula 40】 and provided that "*" represents the connection point to L Ｒ represents the connection point to The compound according to claim 21, characterized in that:

26. L ｂ is an optionally substituted divalent 6- to 12-membered heterocyclyl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms, or L ｂ is an optionally substituted divalent 10- to 15-membered tricyclic heterocyclyl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms, or L ｂ is an optionally substituted divalent 6- to 12-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms, The compound according to claim 21, characterized in that:

27. L ｂ is optionally substituted 2,3-dihydrobenzofuranyl, chromanyl, or spiro[chroman-4,1'-cyclopropyl], The compound according to claim 21, characterized in that

28. L ｂ is optionally C １－６ a divalent 2,3-dihydrobenzofuranyl, chromanyl, or spiro[chroman-4,1'-cyclopropyl] group substituted with an aliphatic group (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl) or a halogen (e.g., -F, -Cl, -Br, -I), The compound according to claim 21, characterized in that

29. L ｂ is 【Chemical Formula 41】 and provided that "*" represents the connection point to L Ｒ represents the connection point to L L ｂ is an optionally substituted divalent chromanyl, or R ｂ is -H and L ｂ is 【Chemical 42】 and where "*" represents the connection point to L Ｒ represents the connection point to R ｂ is -H and L ｂ is 【Chemical 43】 and where " * " represents a connection point to L Ｒ and represents a connection point to R ｂ is -H and L ｂ is 【Chemical 44】 and where "*" represents a connection point to L Ｒ represents a connection point to R ｂ is -H and L ｂ is 【Chemical 45】 is The compound according to claim 21, characterized in that

30. L ｂ is an optionally substituted divalent 6- to 12-membered heteroaryl ring having 1 to 4 (e.g., 0, 1, 2, 3, or 4) heteroatoms The compound according to claim 21, characterized in that

31. L ｂ is optionally substituted divalent imidazo[1,5-a]pyridinyl, indazolyl, benzo[d]imidazolyl, or pyrazolo[1,5-a]pyrimidinyl, The compound according to claim 21, characterized in that

32. L ｂ is imidazo[1,5-a]pyridinyl, and L ｂ is optionally C １－６ a divalent imidazo[1,5-a]pyridinyl, indazolyl, benzo[d]imidazolyl, or pyrazolo[1,5-a]pyrimidinyl optionally substituted with an aliphatic group (e.g., methyl, ethyl, n-propyl, s-propyl, or isopropyl) or a halogen (e.g., -F, -Cl, -Br, -I), The compound according to claim 21, characterized in that

33. L ｂ is 【Chemical Formula 46】 and where "*" represents the connection point to L Ｒ represents the connection point to The compound according to claim 21, characterized in that

34. L ｂ is *-N(R')-Cy-, where "*" represents the point of attachment to L Ｒ and The compound according to claim 21, characterized in that

35. L ｂ is 【Chemical 47】 and where "*" represents the point of attachment to L Ｒ representing the point of attachment to The compound according to claim 21, characterized in that

36. L ｂ is 【Chemical 48】 and where " * " represents a connection point to L Ｒ representing a connection point to The compound according to claim 21, characterized in that

37. R ｂ is not hydrogen, The compound according to any one of the preceding claims, characterized in that

38. R ｂ is hydrogen, an optionally substituted C １－２０ aliphatic group (e.g., methyl, (e.g., -CF ３ ), ethyl, isopropyl, -C ０－４ alkyl-C≡CH, or propargyl), an optionally substituted C ３－２０ cycloaliphatic group (e.g., cyclopropyl, cyclopentyl, or cyclohexyl), an optionally substituted C having 1 to 10 heteroatoms １－２０ heteroaliphatic group, -CN, -OH, -OCH ３ , -OCH(CH ２ CH ３ ), ２ , -OCH ２ CH ２ CH ２ CH ３ , -OCH ２ CH ２ CH ２ CH ２ CH ２ CH ３ , -N(R') ２ (e.g., -N(CH ２ CH ３ ), ２ ), a sulfone group (e.g., -S(O ２ )CH ３ ), an optionally substituted C ６－２０ aryl group (e.g., phenyl or naphthyl), an optionally substituted 5- to 20-membered heteroaryl group (e.g., pyridyl), an optionally substituted 3- to 20-membered heterocyclyl group having 1 to 10 heteroatoms (e.g., tetrahydro-2H-pyranyl, morpholinyl, 2-oxa-5-azabicyclo[2.2.1]heptanyl, or 3-oxa-8-azabicyclo[3.2.1]octanyl). The compound according to any one of the preceding claims, characterized in that

39. R ｂ is optionally substituted tetrahydro-2H-pyranyl, morpholinyl, 3,6-dihydro-2H-pyranyl, azetidinyl, pyrrolidinyl, piperidinyl, silinanil, 2-oxa-5-azabicyclo[2.2.1]heptanyl, 3-oxa-8-azabicyclo[3.2.1]octanyl, The compound according to any one of claims 1 to 38, characterized in that

40. R ｂ is 4 - tetrahydro - 2H - pyranyl, 【Chemical 49】 is is The compound according to any one of claims 1 to 38, characterized in that

41. R ｂ is -O-R', where R' is an optionally substituted 3- to 8-membered saturated or partially unsaturated carbocyclic ring, an optionally substituted phenyl, or an optionally substituted 3- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from nitrogen, oxygen, or sulfur. The compound according to any one of claims 1 to 38, characterized in that

42. R ｂ is 【Chemical Formula 50】 is The compound according to any one of claims 1 to 38, characterized in that

43. A compound having the structure of formula A', or a salt thereof: 【Chemical Formula 51】 In the formula, ring P is an optionally substituted monocyclic, bicyclic or polycyclic ring having 0 to 5 heteroatoms and having 5 to 20 members, 【Chemical 52】 is a single bond or a double bond, Y and Z are each independently C or N, R ２ and R ３ are each independently R", or 【Chemical 53】 and R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ is, L ｗ is a covalent bond or an optionally substituted divalent C １－６ aliphatic group or heteroaliphatic group having 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted, R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ )(R ｗ３ ), and R ｗ１ 、R ｗ２ 、and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, R ５ and R ６ is each independently R” or -C(O)OR”, R ７ and R ８ are each independently R", ring A is an optionally substituted monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms and having 3 to 20 members, L Ａ is L and R ９ and R ｓ are each independently an optionally substituted group selected from R", halogen, -CN, oxo, -NO ２ , or an acyl group, acylamino group, hydroxy group, amino acid group, amine group, amide group, carbamate group, ester group, ether group, carboxylic acid, thio group, thioalkyl group, thioester group, thioether group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, alkylsulfonyl group, and arylsulfonyl group, p and q are each independently 0 to 10, Each R″ is independently hydrogen, halogen, —L—R′, —L—OR′, —L—SR′, —L—C(O)OR′, —L—C(O)SR′, —L—C(O)N(R′) ２ , —L—OC(O)N(R′) ２ , —L—C(O)R′, —L—N(R′) ２ , —CN, —OC(R′) ２ COOH, —SC(R′) ２ COOH, —N(R′)C(R′) ２ COOH, or an optionally substituted group selected from an alkylsulfonyl group, an arylsulfonyl group, a carboxylic acid ester group, an ester group, an ether group, an amide group, a carbohydrate group, an amino acid group, an acyl group, an acyl group substituted with an alkoxy, an alditol group, a sulfate ester group, a sulfonamide group, a sulfoxide group, a sulfonic acid ester group, a sulfone group, a thioalkyl group, a thioester group, and a thioether group, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic group or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-, each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms and having 3 to 20 members, Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ having 1 to 10 heteroatoms, a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups are optionally and independently covalently bonded to each other, or two or more R groups on the same atom are optionally and independently combined with the atom to form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or Two or more R groups on two or more atoms may optionally and independently, together with their intervening atoms, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to those intervening atoms, X is -O-, -S-, -C(R １ )=, -N(R １ )-, or optionally substituted -CH=, -CH=CH-, or -NH- and t is 0 - 9, R １ is R ９ and or a compound having the structure of Formula C, or a salt thereof: 【Chemical 54】 In the formula, R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ is, L ｗ is a covalent bond or an optionally substituted divalent C １－６ aliphatic or heteroaliphatic group having 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-; R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ )(R ｗ３ ), and R ｗ１ 、 R ｗ２ 、 and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, R １０ 、R １１ 、R １２ 、R １３ 、and R １４ are each independently R", Each R” is independently hydrogen, halogen, -L-R’, -L-OR’, -L-SR’, -L-C(O)OR’, -L-C(O)SR’, -L-C(O)N(R’) ２ , -L-OC(O)N(R’) ２ , -L-C(O)R’, -L-N(R’) ２ , -CN, -OC(R’) ２ COOH, -SC(R’) ２ COOH, -N(R’)C(R’) ２ COOH, and Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic or heteroaliphatic group, and here, one or more methylene units are optionally and independently, -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted, each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms, Each R is independently halogen, -H, or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ , a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ , a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups may optionally and independently form a covalent bond with each other, or two or more R groups on the same atom may optionally and independently, together with the atom, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or two or more R groups on two or more atoms may optionally and independently, together with their intervening atoms, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to those intervening atoms, or a compound having the structure of Formula D, or a salt thereof: 【Chemical Formula 55】 In the formula, R １５ and R １６ are each independently -L-R', R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ wherein L ｗ is a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－６ aliphatic group or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ )(R ｗ３ ), and R ｗ１ 、R ｗ２ 、and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms, Each R is independently halogen, -H, or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ , a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ , a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups may optionally and independently form a covalent bond with each other, or two or more R groups on the same atom may optionally and independently, together with the atom, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or two or more R groups on two or more atoms may optionally and independently, together with their intervening atoms, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to those intervening atoms, or a compound having the structure of Formula E, or a salt thereof: 【Chemical Formula 56】 In the formula, R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ is, L ｗ is a covalent bond or an optionally substituted divalent C １－６ aliphatic or heteroaliphatic group having 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ )(R ｗ３ ), and R ｗ１ 、R ｗ２ 、and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, R １７ and R １８ are each independently an optionally substituted monocyclic, bicyclic or polycyclic aromatic ring having 0 to 5 heteroatoms and having 5 to 20 ring members, ring C is an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 6 heteroatoms, L is, independently, a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ having 1 to 10 heteroatoms, a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups may optionally and independently form a covalent bond with each other, or Two or more R groups on the same atom may optionally and independently combine with the atom to form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or, Two or more R groups on two or more atoms may optionally and independently combine with their intervening atoms to form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to the intervening atoms, or, A compound having the structure of Formula F, or a salt thereof: 【Chemical 57】 In the formula, R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ is, L ｗ is a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－６ aliphatic group or heteroaliphatic group, and here, one or more methylene units are optionally and independently -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ )(R ｗ３ ), and R ｗ１ 、 R ｗ２ 、 and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, R ｓ６ and R ｓ７ are each independently Rs, Each R ｓ is independently an optionally substituted group selected from R'', halogen, -CN, oxo, -NO ２ , or an acyl group, acylamino group, hydroxy group, amino acid group, amine group, amide group, carbamate group, ester group, ether group, carboxylic acid group, thio group, thioalkyl group, thioester group, thioether group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, alkylsulfonyl, and arylsulfonyl, Each R″ is independently hydrogen, halogen, —L—R′, —L—OR′, —L—SR′, —L—C(O)OR′, —L—C(O)SR′, —L—C(O)N(R′) ２ , —L—OC(O)N(R′) ２ , —L—C(O)R′, —L—N(R′) ２ , —CN, —OC(R′) ２ COOH, —SC(R′) ２ COOH, —N(R′)C(R′) ２ COOH, or an optionally substituted group selected from an alkylsulfonyl group, an arylsulfonyl group, a carboxylic acid ester group, an ester group, an ether group, an amide group, a carbohydrate group, an amino acid group, an acyl group, an acyl group substituted with an alkoxy, an alditol group, a sulfate ester group, a sulfonamide group, a sulfoxide group, a sulfonic acid ester group, a sulfone group, a thioalkyl group, a thioester group, and a thioether group, q, x and y are each independently 0 to 4, L is, independently, a covalent bond, or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic group or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or a C １～２０ aliphatic group, a C with 1 to 10 heteroatoms １～２０ heteroaliphatic group, C ６～２０ aryl group, a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and an optionally substituted group selected from the group consisting of combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups may optionally and independently form a covalent bond with each other, or, Two or more R groups on the same atom may optionally and independently combine with the atom to form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or, Two or more R groups on two or more atoms may optionally and independently combine with their intervening atoms to form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to the intervening atoms, or, A compound having the structure of Formula G, or a salt thereof: 【Chemical Formula 58】 In the formula, Ring B is an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms, R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ is, L ｗ is a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－６ aliphatic group or heteroaliphatic group, and wherein one or more methylene units are optionally and independently —C(R′) ２ —, —Cy—, —O—, —S—, —N(R′)—, —C(O)—, —C(S)—, —C(NR′)—, —C(O)N(R′)—, —C(S)N(R′)—, —C(NR′)N(R′)—, —N(R′)C(O)N(R′)—, —N(R′)C(O)O—, —S(O)—, —S(O) ２ —, —S(O) ２ N(R′)—, —C(O)S—, or —C(O)O— substituted R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ ),(R ｗ３ ) and R ｗ１ 、R ｗ２ 、and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, R ８ａ is R ｍ or 【Chemical Formula 59】 and, L Ａ is L and Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ an aliphatic or heteroaliphatic group, and here, one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms, Ring A is an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms, Each R ｍ is independently R ｓ and Each R ｓ is independently an optionally substituted group selected from R'', halogen, -CN, oxo, -NO ２ , or an acyl group, acylamino group, hydroxy group, amino acid group, amine group, amide group, carbamate group, ester group, ether group, carboxylic acid group, thio group, thioalkyl group, thioester group, thioether group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, alkylsulfonyl, and arylsulfonyl, Each R″ is independently hydrogen, halogen, —L—R′, —L—OR′, —L—SR′, —L—C(O)OR′, —L—C(O)SR′, —L—C(O)N(R′) ２ , —L—OC(O)N(R′) ２ , —L—C(O)R′, —L—N(R′) ２ , —CN, —OC(R′) ２ COOH, —SC(R′) ２ COOH, —N(R′)C(R′) ２ COOH, or an optionally substituted group selected from an alkylsulfonyl group, an arylsulfonyl group, a carboxylic acid ester group, an ester group, an ether group, an amide group, a carbohydrate group, an amino acid group, an acyl group, an acyl group substituted with an alkoxy, an alditol group, a sulfate ester group, a sulfonamide group, a sulfoxide group, a sulfonic acid ester group, a sulfone group, a thioalkyl group, a thioester group, and a thioether group, q is independently 0 to 10, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ having 1 to 10 heteroatoms, a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups may optionally and independently form a covalent bond with each other, or, Two or more R groups on the same atom may optionally and independently combine with the atom to form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or, Two or more R groups on two or more atoms may optionally and independently, together with their intervening atoms, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to those intervening atoms. Or, A compound having the structure of formula H, or a salt thereof: 【Chemical Formula 60】 In the formula, R ４ is an isourea or isothiourea moiety, or contains an isourea or isothiourea moiety, or -L ｗ -R ｗ wherein L ｗ is a covalent bond, or an optionally substituted divalent C having 1 to 6 heteroatoms １－６ aliphatic group or heteroaliphatic group, and wherein one or more methylene units are optionally and independently, -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted R ｗ is -T-C(=NR ｗ１ ),N(R ｗ２ )(R ｗ３ ), and R ｗ１ 、R ｗ２ 、and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, R ５ is, independently, R", or -C(O)OR", R ２ is R", or 【Chemical Formula 61】 and L Ａ is L and Ring A is an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms. R ９ and R ｓ are each independently an optionally substituted group selected from R'', halogen, -CN, oxo, -NO ２ , or an acyl group, acylamino group, hydroxy group, amino acid group, amine group, amide group, carbamate group, ester group, ether group, carboxylic acid group, thio group, thioalkyl group, thioester group, thioether group, sulfate ester group, sulfonamide group, sulfoxide group, sulfonate ester group, sulfone group, alkylsulfonyl, and arylsulfonyl; p and q are each independently 0 to 10, Each R″ is independently hydrogen, halogen, —L—R′, —L—OR′, —L—SR′, —L—C(O)OR′, —L—C(O)SR′, —L—C(O)N(R′) ２ , —L—OC(O)N(R′) ２ , —L—C(O)R′, —L—N(R′) ２ , —CN, —OC(R′) ２ COOH, —SC(R′) ２ COOH, —N(R′)C(R′) ２ COOH, or an optionally substituted group selected from an alkylsulfonyl group, an arylsulfonyl group, a carboxylic acid ester group, an ester group, an ether group, an amide group, a carbohydrate group, an amino acid group, an acyl group, an acyl group substituted with an alkoxy, an alditol group, a sulfate ester group, a sulfonamide group, a sulfoxide group, a sulfonic acid ester group, a sulfone group, a thioalkyl group, a thioester group, and a thioether group, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic or heteroaliphatic group, and here, one or more methylene units are optionally and independently -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted Each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms. Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ , a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ , a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or Two R groups may optionally and independently form a covalent bond with each other, or Two or more R groups on the same atom may optionally and independently, together with the atom, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or Two or more R groups on two or more atoms may optionally and independently, together with their intervening atoms, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to those intervening atoms.

44. R ４ is -L ｗ -R ｗ and provided that L ｗ is a covalent bond or an optionally substituted divalent C １－６ aliphatic or heteroaliphatic group having from 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-; R ｗ is - T - C(=NR ｗ１ ), N(R ｗ２ )(R ｗ３ ), and R ｗ１ 、 R ｗ２ 、 and R ｗ３ are each independently, -L-R', or a detectable moiety, T is O or S, Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic or heteroaliphatic group, and wherein one or more methylene units are optionally and independently -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted Each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms. Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ having 1 to 10 heteroatoms, a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or Two R groups may optionally and independently form a covalent bond with each other, or Two or more R groups on the same atom may optionally and independently, together with the atom, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or Two or more R groups on two or more atoms may optionally and independently, together with their intervening atoms, form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to those intervening atoms. A compound according to any one of the preceding claims, characterized in that.

45. R ４ is -L ｗ -R ｗｈ and provided that L ｗ is a covalent bond or an optionally substituted divalent C １－６ aliphatic or heteroaliphatic group having 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-; R ｗｈ is -T-H, T is O or S, Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ which is an aliphatic or heteroaliphatic group, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- Each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms. Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ , a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ , a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or Two R groups may optionally and independently form a covalent bond with each other, or Two or more R groups on the same atom may optionally and independently combine with the atom to form an optionally substituted 3- to 20-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the atom, or, Two or more R groups on two or more atoms may optionally and independently combine with their intervening atoms to form an optionally substituted 3- to 30-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the intervening atoms, A compound according to any one of the preceding claims, characterized in that.

46. L ｗ is a covalent bond, optionally substituted -CH ２ -, -CHD-, -CD ２ -, mono-substituted -CH ２ -, -CH(CH ３ )- 【Chemical Formula 62】 、 【Chemical Formula 63】 , -CHD-, mono-substituted -CD ２ , -C(O)-CH ２ , optionally substituted -C(S)-CH ２ , -C(N(R'))-CH ２ - (wherein, -CH ２ - is optionally substituted), optionally substituted -C(O)-CHD-, optionally substituted -C(S)-CHD-, -C(N(R'))-CHD- (wherein, -CHD- is optionally substituted), optionally substituted -C(O)-CD ２ , optionally substituted -C(S)-CD ２ , -C(N(R'))-CD ２ - (wherein, -CD ２ - is optionally substituted). A compound according to any one of the preceding claims, characterized in that.

47. T is O, A compound according to any one of the preceding claims, characterized in that.

48. T is S, A compound according to any one of claims 1 to 46, characterized in that.

49. R ｗ１ is -L-R'. A compound according to any one of the preceding claims, characterized in that.

50. R ｗ１ is H, optionally substituted C １－１０ aliphatic group, optionally substituted C １－１０ alkyl, methyl, ethyl, isopropyl, optionally substituted C ３－１０ cycloalkyl, cyclohexyl, optionally substituted C having 1 to 3 heteroatoms １－１０ heteroaliphatic group, optionally substituted C ６－１４ aryl, optionally substituted phenyl, 5- to 10-membered heteroaryl having 1 to 4 optionally substituted heteroatoms, 3- to 10-membered heterocyclyl having 1 to 4 optionally substituted heteroatoms, or a detectable moiety A compound according to any one of the preceding claims, characterized in that.

51. R ｗ２ is -L-R', R ｗ２ is H, an optionally substituted C1-10 aliphatic group, an optionally substituted C １－１０ alkyl, an optionally substituted C １－６ haloalkyl, methyl, ethyl, isopropyl, -C(CH ２ ) ２ -C≡C-CH ３ , -CH ２ -C≡CH, an optionally substituted C ３－１０ cycloalkyl, cyclopropyl, cyclohexyl, an optionally substituted adamantyl, 1-adamantyl, -CH ２ -CF ３ , an optionally substituted C １－１０ heteroaliphatic group having 1 to 3 heteroatoms, an optionally substituted C ６－１４ aryl, an optionally substituted phenyl, an optionally substituted 5- to 10-membered heteroaryl having 1 to 4 heteroatoms, an optionally substituted 3- to 10-membered heterocyclyl having 1 to 4 heteroatoms, or an optionally substituted oxetanyl. A compound according to any one of the preceding claims, characterized in that.

52. R ｗ１ and R ｗ２ together with their intervening atoms form an optionally substituted 5- to 14-membered ring having in addition to the intervening atoms 0 to 6 heteroatoms, or R ｗ１ and R ｗ２ together with their intervening atoms form an optionally substituted 5- to 14-membered partially unsaturated ring having 0 to 6 heteroatoms in addition to the intervening atoms A compound according to any one of claims 1 to 48, characterized in that.

53. -C(=NR ｗ１ )N(R ｗ２ )- is optionally substituted 【Chemical Formula 64】 wherein y is independently 0 to 4, 【Chemical Formula 65】 , y is independently 0, 1, 2, 3 or 4, 【Chemical Formula 66】 , y is independently 0, 1, 2, 3 or 4, and 【Chemical Formula 67】 is a single bond or a double bond, A compound according to any one of claims 1 to 48, characterized in that.

54. R ｗ３ is -L-R'. A compound according to any one of the preceding claims, characterized in that.

55. R ｗ３ is H, optionally substituted C １－１０ aliphatic group, optionally substituted C １－１０ alkyl, optionally substituted C １－６ haloalkyl, methyl, ethyl, isopropyl, optionally substituted C ３－１０ cycloalkyl, cyclopropyl, cyclohexyl, optionally substituted adamantyl, 1 - adamantyl, -CH ２ -CF ３ , optionally substituted C having 1 - 3 heteroatoms １－１０ heteroaliphatic group, optionally substituted C ６－１０ aryl, optionally substituted phenyl, 5 - 10 membered heteroaryl having 1 - 4 optionally substituted heteroatoms, 3 - 10 membered heterocyclyl having 1 - 4 optionally substituted heteroatoms, 3 - 10 membered saturated ring having 0 - 5 optionally substituted heteroatoms, 3 - 10 membered partially saturated ring having 0 - 5 optionally substituted heteroatoms, optionally substituted phenyl, optionally substituted 5 - 6 membered heteroaryl, 2 - pyridyl, 3 - pyridyl, or 4 - pyridyl, A compound according to any one of the preceding claims, characterized in that.

56. R ｗ２ and R ｗ３ together with the nitrogen atom to which they are attached form an optionally substituted 3- to 14-membered ring having, in addition to the nitrogen atom, 0 to 6 heteroatoms, R ｗ２ and R ｗ３ together with the nitrogen atom to which they are attached form an optionally substituted 3- to 10-membered aromatic ring having 0 to 5 heteroatoms in addition to the nitrogen atom, or R ｗ２ and R ｗ３ together with the nitrogen atom to which they are attached form an optionally substituted 3- to 8-membered monocyclic non-aromatic ring having 0 to 3 heteroatoms in addition to the nitrogen atom A compound according to any one of claims 1 to 50, characterized in that.

57. -N(R ｗ２ )(R ｗ３ ) is optionally substituted 【Chemical Formula 68】 wherein x and y are each independently 0 to 4, or -N(R ｗ２ )(R ｗ３ ) is optionally substituted 【Chemical Formula 69】 wherein x and y are each independently 0 to 4, or -N(R ｗ２ )(R ｗ３ ) is optionally substituted 【Chemical 70】 wherein x and y are each independently 0 to 4, or -N(R ｗ２ )(R ｗ３ ) is optionally substituted 【Chemical 71】 wherein y is 0 to 4; or -N(R ｗ２ )(R ｗ３ ) is optionally substituted 【Chemical Formula 72】 where x and y are each independently 0 to 4, and Q is optionally substituted S, Si, S(O) ２ is A compound according to any one of claims 1 to 50, characterized in that.

58. -N(R ｗ２ )(R ｗ３ ) is -NH ２ , 【Chemical Formula 73】 is, A compound according to any one of claims 1 to 50, characterized in that.

59. R ４ is 【Chemical 74】 is, A compound according to any one of claims 1 to 43, characterized in that.

60. A pharmaceutical composition comprising or delivering a compound according to any one of the preceding claims or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

61. A method for inhibiting the activity of a polypeptide comprising a nucleophilic moiety, the method comprising contacting the polypeptide with a compound or composition according to any one of the preceding claims (preferably, here, the nucleophilic moiety is —SH or —SeH or a salt form thereof, or the polypeptide is GPX4), or A method for inhibiting cell proliferation in a system, the method comprising administering to the system a compound or composition according to any one of the preceding claims, or A method for inducing cell death in a system, the method comprising administering to the system a compound or composition according to any one of the preceding claims, or A method for inducing ferroptosis in a system, the method comprising administering to the system a compound or composition according to any one of the preceding claims.

62. A method for preventing a condition, disorder or disease, the method comprising administering or delivering an effective amount of a compound or composition according to any one of the preceding claims to a subject susceptible thereto, or A method for preventing a condition, disorder or disease associated with a polypeptide comprising —SeH or a salt form thereof, the method comprising administering or delivering an effective amount of a compound or composition according to any one of the preceding claims to a subject susceptible thereto, or A method for treating a condition, disorder or disease associated with a polypeptide comprising —SeH or a salt form thereof, the method comprising administering or delivering an effective amount of a compound or composition according to any one of the preceding claims to a subject susceptible thereto.

63. A method for treating a condition, disorder or disease, the method comprising administering or delivering an effective amount of a compound or composition according to any one of the preceding claims to a subject susceptible thereto.

64. The method according to claim 62 or 63, wherein the condition, disorder or disease is cancer.

65. The cancer is adrenocortical cancer, anal cancer, biliary tract cancer, bladder cancer, bone cancer, brain cancer, breast cancer, cervical cancer, colon cancer, endometrial cancer, esophageal cancer, head and neck cancer, intestinal cancer, liver cancer, lung cancer, oral cancer, ovarian cancer, pancreatic cancer, kidney cancer, prostate cancer, salivary gland cancer, skin cancer, stomach cancer, testicular cancer, pharyngeal cancer, thyroid cancer, uterine cancer, vaginal cancer, sarcoma, or soft tissue cancer, or the cancer is osteosarcoma, glioma, astrocytoma, neuroblastoma, small intestine cancer, bronchial cancer, small cell lung cancer, non-small cell lung cancer, basal cell cancer, or melanoma, The method according to claim 64, characterized in that.

66. The cancer is a blood cancer, The method according to claim 65, characterized in that.

67. The blood cancer is acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML), lymphoma (e.g., Hodgkin lymphoma, non-Hodgkin lymphoma, Burkitt lymphoma), chronic lymphocytic leukemia (CLL), chronic myeloid leukemia (CML), hairy cell chronic myeloid leukemia (CML), or multiple myeloma, The method according to claim 66, characterized in that.

68. A compound containing an isourea moiety, or a salt thereof.

69. A compound containing an isothiourea moiety, or a salt thereof.

70. The compound inhibits the activity of a polypeptide containing a selenocysteine residue, The compound reacts with selenocysteine or a salt thereof, or a selenocysteine residue in a polypeptide, -SeH in selenocysteine or a salt form thereof substitutes for the isourea moiety, The compound can inhibit or prevent cell growth or proliferation, The compound can induce cell death, The compound can induce ferroptosis, The effect of the compound is reduced in the presence of a ferroptosis inhibitor, The IC of the compound observed in the presence of the ferroptosis inhibitor ５０ is about or at least about 2 to 5000 times, for example, about or at least about 10 to 1000, 50 to 1000, 100 to 1000, 2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 200, 500 or 1000 times that in the absence of the ferroptosis inhibitor, The IC of the said compound observed in the presence of a ferroptosis inhibitor ５０ is about or at least about 10 times that in the absence of a ferroptosis inhibitor, The IC of the compound observed in the presence of the ferroptosis inhibitor ５０ is about or at least about 20-fold that in the absence of the ferroptosis inhibitor, The IC of the said compound observed in the presence of a ferroptosis inhibitor ５０ is about or at least about 50 times that in the absence of a ferroptosis inhibitor, The IC of the compound observed in the presence of the ferroptosis inhibitor ５０ is about or at least about 100-fold that in the absence of the ferroptosis inhibitor, The IC of the compound observed in the presence of the ferroptosis inhibitor ５０ is about or at least about 1 to 100, such as about or at least about 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, or 100 μM, When the ferroptosis inhibitor is evaluated alone, the concentration of the ferroptosis inhibitor is about or at least about the EC50 of the ferroptosis inhibitor, The concentration of the ferroptosis inhibitor is about or at least about 0.1 - 100, for example, about or at least about 1 - 20, 2 - 10, 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 20, 30, 40, or 50 μM, The concentration of the ferroptosis inhibitor is about or at least about 1 μM, The concentration of the ferroptosis inhibitor is about or at least about 2 μM, the compound inhibits the activity of GPX4, the compound binds to GPX4, or The isourea or isothiourea moiety has the structure of R ｗ wherein R ｗ is -T-C(=NR ｗ１ )N(R ｗ２ )(R ｗ３ ) or a salt thereof, and R ｗ１ , R ｗ２ and R ｗ３ are each independently -L-R' or a detectable moiety. T is O or S, Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic group or heteroaliphatic group, and here, one or more methylene units are optionally and independently -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms and having 3 to 20 members, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ having 1 to 10 heteroatoms, a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups optionally and independently form a covalent bond with each other, or two or more R groups on the same atom optionally and independently together with the atom form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or two or more R groups on two or more atoms optionally and independently together with their intervening atoms form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to the intervening atoms, A compound according to any one of the preceding claims, characterized in that.

71. R ｗ A compound containing R ｗ is -T-C(=NR ｗ１ ), N(R ｗ２ )(R ｗ３ ), or a salt thereof, provided that R ｗ１ , R ｗ２ and R ｗ３ are each independently -L-R', or a detectable moiety Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic or heteroaliphatic group, and here, one or more methylene units are optionally and independently -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms and having 3 to 20 members, T is O or S, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ , a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ , a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or two R groups optionally and independently form a covalent bond with each other, or two or more R groups on the same atom optionally and independently together with the atom form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or two or more R groups on two or more atoms optionally and independently together with their intervening atoms form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 30 members and having 0 to 10 heteroatoms in addition to the intervening atoms, a compound, or R ｗ A compound containing R ｗ is -OC(=NR ｗ１ ), N(R ｗ２ )(R ｗ３ ), or a salt thereof, provided that R ｗ１ , R ｗ２ and R ｗ３ are each independently -L-R', or a detectable moiety Each L is independently a covalent bond or an optionally substituted divalent C having 1 to 6 heteroatoms １－１０ aliphatic or heteroaliphatic group, and here, one or more methylene units are optionally and independently -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O-substituted, each -Cy- is independently an optionally substituted monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms and having 3 to 20 members, Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ , a heteroaliphatic group of C having 1 to 10 heteroatoms, an aryl group of C １～２０ , a heteroaryl group of 5 to 20 members having 1 to 10 heteroatoms, a heterocyclyl of 3 to 20 members having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or ６～２０ ​ two R groups optionally and independently form a covalent bond with each other, or two or more R groups on the same atom optionally and independently together with the atom form an optionally substituted monocyclic, bicyclic or polycyclic ring having 3 to 20 members and having 0 to 10 heteroatoms in addition to the atom, or A compound in which two or more R groups on two or more atoms optionally and independently, together with their intervening atoms, form an optionally substituted 3- to 30-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the intervening atoms. Claim 72 L ｗ is a covalent bond or an optionally substituted divalent C １－６ aliphatic group or heteroaliphatic group having 1 to 6 heteroatoms, and wherein one or more methylene units are optionally and independently replaced by -C(R') ２ -, -Cy-, -O-, -S-, -N(R')-, -C(O)-, -C(S)-, -C(NR')-, -C(O)N(R')-, -C(S)N(R')-, -C(NR')N(R')-, -N(R')C(O)N(R')-, -N(R')C(O)O-, -S(O)-, -S(O) ２ -, -S(O) ２ N(R')-, -C(O)S-, or -C(O)O- Each -Cy- is independently an optionally substituted 3- to 20-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms. Each R' is independently R, -OR, -C(O)R, -C(O)OR, -C(O)N(R) ２ , -S(O)R, or -S(O)OR, and Each R is independently -H or an optionally substituted group selected from the group consisting of an aliphatic group of C １～２０ having 1 to 10 heteroatoms, a heteroaliphatic group of C １～２０ having 1 to 10 heteroatoms, an aryl group of C ６～２０ a 5- to 20-membered heteroaryl group having 1 to 10 heteroatoms, a 3- to 20-membered heterocyclyl having 1 to 10 heteroatoms, and combinations thereof, provided that these combinations each independently have 1 to 30 carbon atoms and 0 to 10 heteroatoms, or Two R groups optionally and independently form a covalent bond with each other, or Two or more R groups on the same atom optionally and independently, together with the atom, form an optionally substituted 3- to 20-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the atom, or Two or more R groups on two or more atoms optionally and independently, together with their intervening atoms, form an optionally substituted 3- to 30-membered monocyclic, bicyclic or polycyclic ring having 0 to 10 heteroatoms in addition to the intervening atoms. characterized in that -L ｗ -R ｗ The compound according to claim 71 or 72, comprising Claim 73 The compound is -C(=O)-L ｗ -R ｗ and includes A compound according to any one of claims 73 to 75, characterized in that. Claim 74 A compound shown in Table C1 or C2, or a pharmaceutically acceptable salt thereof.

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