N,N-Dimethyltryptamine and Related Hallucinogens and Their Uses

Abstract

Described herein are compounds that are derivatives of DMT or 5-MeO-DMT and can be metabolically converted to N,N-dimethyltryptamine or its analogs upon administration to a subject. In certain embodiments, the compounds described herein are useful for treating conditions associated with neurological disorders.

Description

[Technical Field]

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS This application claims the benefit of U.S. Provisional Patent Application No. 63 / 219,312, filed July 7, 2021, and U.S. Provisional Patent Application No. 63 / 276,516, filed November 5, 2021, the contents of each of which are incorporated herein by reference in their entirety. [Background technology]

[0002] Nearly one in five American adults suffers from a mental illness, and over 50% of Americans will be diagnosed with a mental disorder at some point in their lifetime. One in 25 Americans suffers from a serious mental illness such as major depression, schizophrenia, or bipolar disorder. Summary of the Invention

[0003] In one aspect, the disclosure provides a compound of formula (I), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 2 is -C(O)OR 3 , -C(O)R 4 , -CH(R 5 ) OR 6 , -C(O)OCH(R 5 )OC(O)R 6 , -C(O)OCH(R 5 )OC(O)OR 6 , -CH(R 5 )C(O)R 6 , -CH(R 5 )OC(O)R 6 , -CH(R 5 )OC(O)OR 6 , -S(O)2OR 7 , -P(O)OR 8 [N(R 9 )R 10], -P(O)[N(R 9 )R 10 ][N(R 11 )R 12 ], -C(O)N(R 9 )R 10 , -P(O)OR 11 (OR 12 ), -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 ], or -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 is independently hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A is replaced by R 9 and R 10 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A or substituted with R 9 and R 10 together with the atoms to which they are attached are unsubstituted or contain one or more R A forming a heterocyclylalkyl ring substituted with R 11 and R 12is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A or substituted with R 11 and R 12 together with the atoms to which they are attached are unsubstituted or contain one or more R A forming a heterocyclylalkyl ring substituted with Each R A are independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, an amino acid side chain, -OR 13 , -N(R 18 )R 19 , -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , -OP(O)OR 17 [N(R 18 )R 19 ], -C(O)N(R 18 )R 19 , -OC(O)N(R 18 )R 19 , or -OP(O)OR 20 (OR 21 ), wherein each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, amino acid side chain, aryl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 13 , R 14 , R 15 , R 16 , or R 17 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R B is replaced by R 18 and R 19 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R B or substituted with R 18 and R 19 together with the atoms to which they are attached are unsubstituted or contain one or more R B forming a heterocyclylalkyl ring substituted with R 20 and R 21 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R B or substituted with R 20 and R 21 together with the atoms to which they are attached are unsubstituted or contain one or more R B forming a heterocyclylalkyl ring substituted with Each R Bare independently halogen, amino, cyano, hydroxyl, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, arylalkyl, -C(O)CH3, -C(O)Ph, or heteroarylalkyl, wherein each cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl; R 1 is hydrogen, R 3 is not tert-butyl.

[0004] In some embodiments, a compound of Formula (I) having the structure of Formula (Ia), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is methoxy or hydrogen, and R 3 is alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl, each of which is independently unsubstituted or substituted with one or more R A is replaced by .

[0005] In some embodiments, the compound of Formula (I) has the structure of Formula (Ib): [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A2 , R A3 , and R A4 each independently represents hydrogen, or independently represents one or more of an alkyl, aryl, halogen, -OR 13 , -NR(R 18)R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is alkyl substituted with R A5 is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , or -OC(O)OR 16 wherein each heteroalkyl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0006] In some embodiments, a compound of Formula (I) having the structure of Formula (Ib-1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A2 , R A3 , R A4 , R A6 , and R A7 each independently represents hydrogen, or independently represents one or more of an alkyl, aryl, halogen, -OR 13 , -NR(R18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is alkyl substituted with R A5 is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , or -OC(O)OR 16 wherein each heteroalkyl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0007] In some embodiments, the compound of Formula (I) or (Ib) has the structure of Formula (Ib1), or a pharmaceutically acceptable salt thereof. [ka]

[0008] In some embodiments, a compound of Formula (I) having the structure of Formula (Ic), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 18 and R19 is independently hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each alkyl, cycloalkyl, and heteroalkyl is independently unsubstituted or substituted with one or more R B or substituted with R 18 and R 19 together with the atoms to which they are attached, are unsubstituted or contain one or more R B The heterocyclylalkyl ring is formed by substituted with

[0009] In some embodiments, a compound of Formula (I) having the structure of Formula (Id), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 5 is alkyl or cycloalkyl (each of which is independently unsubstituted or contains one or more R A substituted with ), or hydrogen, and R A6 is hydrogen, or is unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is alkyl substituted with

[0010] In some embodiments, a compound of Formula (I) having the structure of Formula (Ie), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 5is hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is independently unsubstituted or substituted with one or more R A is replaced by .

[0011] In some embodiments, a compound of Formula (I) having the structure of Formula (If), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is methoxy or hydrogen, and R 9 and R 10 is independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl, and each alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, and heterocyclylalkyl is independently unsubstituted or substituted with one or more R A or substituted with R 9 and R 10 together with the atoms to which they are attached, are unsubstituted or contain one or more R A The heterocyclylalkyl ring is formed by substituted with

[0012] In some embodiments, a compound of Formula (I) or (If) having the structure of Formula (If1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 10 is hydrogen, alkyl, heteroalkyl, cycloalkyl, or heterocyclylalkyl, and each of the alkyl, heteroalkyl, cycloalkyl, and heterocyclylalkyl is unsubstituted or contains one or more R A is replaced by X1 and X 2 each independently represents -CH2-, -O-, -NH-, -S-, -S(O)-, -S(O)2-, or -N(Y 1 )-, and each Y 1 is independently hydrogen, cycloalkyl, heteroalkyl, or alkyl.

[0013] In some embodiments, a compound of Formula (I) having the structure of Formula (Ig), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A2 , R A3 , and R A4 each independently represents hydrogen, or is unsubstituted or represents one or more of alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is alkyl substituted with R 10 is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of the alkyl, heteroalkyl, and cycloalkyl is unsubstituted or contains one or more R A is replaced by R A5 is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , or -OC(O)OR16 wherein each of the heteroalkyl, heterocyclylalkyl, and heteroaryl is unsubstituted or is selected from the group consisting of one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0014] In some embodiments, a compound of Formula (I) having the structure of Formula (Ih), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R 10 is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of the alkyl, heteroalkyl, and cycloalkyl is unsubstituted or contains one or more R A is replaced by R 18 and R 19 is independently hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each alkyl, cycloalkyl, or heterocyclylalkyl is independently unsubstituted or contains one or more R B or substituted with R 18 and R 19 together with the atoms to which they are attached, are unsubstituted or contain one or more R B The heterocyclylalkyl ring is formed by substituted with

[0015] In some embodiments, a compound of Formula (I) having the structure of Formula (Ii), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R 5 and R 10 is independently hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each alkyl, heteroalkyl, and cycloalkyl is independently unsubstituted or substituted with one or more R A is replaced by R A6 is independently hydrogen, alkyl, heteroalkyl, or cycloalkyl, each of which is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0016] In some embodiments, a compound of Formula (I) having the structure of Formula (Ij), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 5 and R 10 is hydrogen, alkyl, or heteroalkyl, and each of the alkyl and heteroalkyl is independently unsubstituted or contains one or more R A is replaced by .

[0017] In some embodiments, a compound of Formula (I) having the structure of Formula (Ik), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 4 is alkyl, heterocyclylalkyl, aryl, heteroaryl, or heteroalkyl, each of which is unsubstituted or contains one or more R A is replaced by .

[0018] In some embodiments, a compound of Formula (I) or (Ik) having the structure of Formula (Ik1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A2 , R A3 , and R A4 is independently hydrogen, an alkyl, or an amino acid side chain, and each alkyl or amino acid side chain is independently unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 10 is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of the alkyl, heteroalkyl, and cycloalkyl is unsubstituted or contains one or more R A is replaced by R A5 is heteroalkyl, heterocyclylalkyl, heteroaryl, -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13)C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , or -OC(O)OR 16 wherein each of the heteroalkyl, heterocyclylalkyl, and heteroaryl is unsubstituted or is selected from the group consisting of one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0019] In some embodiments, a compound of Formula (I) or (Ik) having the structure of Formula (Ik2), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 13 is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, or heterocyclylalkyl, and each of the alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, and heterocyclylalkyl is unsubstituted or contains one or more R B is replaced by p is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

[0020] In some embodiments, a compound of Formula (I) or (Ik) having the structure of Formula (Ik3), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, RA1 is an alkyl or amino acid side chain, each of which is unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R A5 is -N(R 18 )R 19 or -N(R 13 )C(O)R 14 is.

[0021] In some embodiments, a compound of Formula (I) having the structure of Formula (II), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl, each of which is unsubstituted or has one or more R A is replaced by R 6 is alkyl, cycloalkyl, heterocyclylalkyl, or heteroalkyl, each of which is unsubstituted or substituted with one or more R A is replaced by .

[0022] In some embodiments, a compound of Formula (I) having the structure of Formula (Im), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each of the alkyl, cycloalkyl, and heteroalkyl is unsubstituted or contains one or more R A is replaced by R 11 and R 12 is independently hydrogen, cycloalkyl, aryl, heteroaryl, or alkyl, and each of the alkyl, cycloalkyl, and heteroalkyl is independently unsubstituted or substituted with one or more R A is replaced by .

[0023] In some embodiments, a compound of Formula (I) or (Im) having the structure of Formula (Im1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A3 , and R 5 each is independently hydrogen, alkyl, or cycloalkyl; R A2 and R A4 each independently is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, —OC(O)R 15 , or -OC(O)OR 16 and Each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16, or -OC(O)N(R 18 )R 19 is replaced by .

[0024] In some embodiments, a compound of Formula (I), (Im), or (Im1) having the structure of Formula (Im1a), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A3 , and R 5 is independently hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is independently unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R B1 and R B2 Each of is independently hydrogen or alkyl that is unsubstituted or substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl.

[0025] In some embodiments, a compound of Formula (I) having the structure of Formula (In), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl; R 8 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl; R 9 and R 10 each is independently hydrogen or alkyl; Each cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0026] In some embodiments, a compound of Formula (I) or (In) having the structure of Formula (In1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 is hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is unsubstituted or is selected from alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 5 and R 8 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and the alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl are independently unsubstituted or substituted with one or more R A is replaced by R 13 is hydrogen, or unsubstituted, or contains one or more R B is alkyl substituted with

[0027] In some embodiments, a compound of Formula (I) having the structure of Formula (Io), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 11 and R 12 is independently selected from hydrogen, cycloalkyl, aryl, heteroaryl, or alkyl, and each cycloalkyl, aryl, heteroaryl, and alkyl is independently unsubstituted or contains one or more R A or substituted with R 11 and R 12 together with the atoms to which they are attached, are unsubstituted or contain one or more R A The heterocyclylalkyl ring is formed by substituted with

[0028] In some embodiments, a compound of Formula (I) or (Io) having the structure of Formula (Io1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 and R A3 each is independently hydrogen, alkyl, or cycloalkyl; R A2 and R A4 each independently represents alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, -OC(O)R 15 , or -OC(O)OR 16 and Each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0029] In some embodiments, a compound of Formula (I) or (Io) having the structure of Formula (Io2), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is methoxy or hydrogen, and R A1 is aryl or heteroaryl, each of which is unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0030] In some embodiments, a compound of Formula (I), (Io), or (Io1) having the structure of Formula (Io1a), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 and R A3is independently hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is independently unsubstituted or is substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R B1 and R B2 Each of is independently hydrogen or alkyl that is unsubstituted or substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl.

[0031] In some embodiments, a compound of Formula (I) having the structure of Formula (Ip), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 8 is alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl; R 9 and R 10 each is independently hydrogen or alkyl; Each alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0032] In some embodiments, a compound of Formula (I) or (Ip) having the structure of Formula (Ip1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 is hydrogen, alkyl, or cycloalkyl, each of which is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 8 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and each alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is unsubstituted or substituted with one or more R A is replaced by R 13 is hydrogen, or unsubstituted, or contains one or more R B is alkyl substituted with

[0033] In some embodiments, a compound of Formula (I) having the structure of Formula (Iq), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl; R 6 is alkyl, cycloalkyl, heteroalkyl, heterocyclylalkyl, aryl, or heteroaryl; Each alkyl, cycloalkyl, heteroaryl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0034] In some embodiments, a compound of Formula (I) or (Iq) having the structure of Formula (Iq1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is unsubstituted or has one or more R A is replaced by Q 1 teeth, [ka] and Y 1 , Y 2 , or Y 3 each independently represents -O-, -S-, -S(O)-, -S(O)2-, -N(R Y1 )-, or -NC(O)R Y2 and R Y1 and R Y2 Each of is independently hydrogen, alkyl, heteroalkyl, or heteroaryl.

[0035] In some embodiments, a compound of Formula (I) having the structure of Formula (Ir), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5is hydrogen, alkyl, or cycloalkyl; R 6 is alkyl, cycloalkyl, heteroalkyl, heterocyclylalkyl, aryl, or heteroaryl; Each alkyl, cycloalkyl, heteroaryl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0036] In some embodiments, a compound of Formula (I) or (Ir) having the structure of Formula (Ir1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is unsubstituted or has one or more R A is replaced by Q 1 teeth, [ka] and Y 1 , Y 2 , or Y 3 each independently represents -O-, -S-, -S(O)-, -S(O)2-, -N(R Y1 )-, or -NC(O)R Y2 and R Y1 and R Y2 Each of is independently hydrogen, alkyl, heteroalkyl, or heteroaryl.

[0037] In some embodiments, a compound of Formula (I) having the structure of Formula (Is), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 15 is alkyl, heteroalkyl, cycloalkyl, aryl, or heteroaryl, each of which is unsubstituted or contains one or more R B is replaced by .

[0038] In some embodiments, a compound of Formula (I) having the structure of Formula (It), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 13 is alkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, each of which is unsubstituted or contains one or more R B is replaced by .

[0039] In some embodiments, a compound of Formula (I) having the structure of Formula (Iu), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R A1 is hydrogen, alkyl, or cycloalkyl, each of which is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 20 and R 21 is independently hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and each alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more R B or substituted with R 20 and R 21 together with the atoms to which they are attached, are unsubstituted or contain one or more R B The heterocyclylalkyl ring is formed by substituted with

[0040] In some embodiments, a compound of Formula (I) having the structure of Formula (IV), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R 9 and R 10 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A or substituted with R 9 and R 10 together with the atoms to which they are attached, are unsubstituted or contain one or more R A forming a heterocyclylalkyl ring substituted with

[0041] R 11 and R 12is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A or substituted with R 11 and R 12 together with the atoms to which they are attached, are unsubstituted or contain one or more R A In some embodiments, a compound of Formula (I) having the structure of Formula (Iw), or a pharmaceutically acceptable salt thereof, [ka] During the ceremony, R 1 is hydrogen or methoxy, R A1 and R A2 is independently hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is independently unsubstituted or is substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R A3 -OR 13 , -N(R 18 )R 19 , -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , -OP(O)OR17 [N(R 18 )R 19 ], -C(O)N(R 18 )R 19 , -OC(O)N(R 18 )R 19 , or -OP(O)OR 20 (OR 21 ) and p is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

[0042] In another aspect, the present disclosure provides compounds of formula (I), (Ia), (Ib), (Ib-1), (Ib1), (Ic), (Id), (Ie), (If), (If1), (Ig), (Ih), (Ii), (Ij), (Ik), (Ik1), (Ik2), (Ik3), (Il), (Im), (Im1), (Im1a), (In), (In1), (Io), (Io1), (I (Io2), (Io1a), (Ip), (Ip1), (Iq), (Iq1), (Ir), (Ir1), (Is), (It), (Iu), (Iv), or (Iw), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, carrier, adjuvant, or vehicle.

[0043] In another aspect, the disclosure provides a method of treating a condition in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I), (Ia), (Ib), (Ib-1), (Ib1), (Ic), (Id), (Ie), (If), (If1), (Ig), (Ih), (Ii), (Ij), (Ik), (Ik1), (Ik2), (Ik3), (Il), (Im), (Im1), (Im1a), (In), (In1), (Io), (Io1), (Io2), (Io1a), (Ip), (Ip1), (Iq), (Iq1), (Ir), (Ir1), (Is), (It), (Iu), (Iv), or (Iw), or a pharmaceutically acceptable salt thereof. [Brief explanation of the drawings]

[0044] [Figure 1]1 shows the mean concentration-time profile of DMT following oral dosing of DMT to male SD rats (1 mg / kg for IV dosing and 10 mg / kg for oral dosing). [Figure 2] 1 shows the mean concentration-time profile of DMT following oral dosing of 5-MeO-DMT to male SD rats (1 mg / kg for IV dosing and 10 mg / kg for oral dosing). [Figure 3] FIG. 1 shows the time course of plasma concentrations of N,N-dimethyltryptamine (DMT) and the corresponding prodrug Compound 20 in Sprague-Dawley rats administered 1 mg / kg Compound 20 intravenously (IV) (Panel A) or 10 mg / kg Compound 20 orally (PO) (Panel B). [Figure 4] 1 shows the mean concentration-time profile of DMT following IV or oral dosing of Compound 20 to male SD rats (1 mg / kg for IV dosing and 10 mg / kg for oral dosing). [Figure 5] 1 shows the mean concentration-time profile of Compound 20 following IV or oral dosing of Compound 20 to male SD rats (1 mg / kg for IV dosing and 10 mg / kg for oral dosing). [Figure 6] FIG. 1 shows the time course of plasma concentrations of 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) and the corresponding prodrug Compound 19 in Sprague-Dawley rats administered 1 mg / kg Compound 19 intravenously (IV) (Panel A) or 10 mg / kg Compound 19 orally (PO) (Panel B). [Figure 7] 1 shows the mean concentration-time profile of 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) following IV or oral dosing of Compound 19 to male SD rats (1 mg / kg for IV dosing and 10 mg / kg for oral dosing). [Figure 8] 1 shows the mean total concentration of DMT following PO administration of 10 mg / kg of a DMT prodrug to male Sprague Dawley rats. [Figure 9]1 shows the mean total concentrations of DMT prodrugs following IV and PO administration of 1, 10 mg / kg, and 10 mg / kg to male Sprague Dawley rats. [Figure 10] 1 shows the mean total concentration of 5-MeO-DMT following PO administration of 10 mg / kg of the 5-MeO-DMT prodrug to male Sprague Dawley rats. [Figure 11] 1 shows the mean total concentrations of 5-MeO-DMT prodrug following IV and PO administration of 1, 10 mg / kg, and 10 mg / kg to male Sprague Dawley rats. [Figure 12] 1 shows the mean concentration-time profiles of DMT CP-2 and metabolite DMT after oral administration of DMT CP-2 (10 mg / Kg) to male SD rats. [Figure 13] 1 shows the mean concentration-time profiles of DMT CP-3 and metabolite DMT after oral administration of DMT CP-3 (10 mg / Kg) to male SD rats. [Figure 14] 1 shows the mean concentration-time profiles of DMT CP-4 and metabolite DMT after oral administration of DMT CP-4 (10 mg / Kg) to male SD rats. [Figure 15] 1 shows the mean concentration-time profiles of DMT CP-5 and metabolite DMT after oral administration of DMT CP-5 (10 mg / Kg) to male SD rats. [Figure 16] 1 shows the mean concentration-time profiles of DMT AP-1 and metabolite DMT after oral administration of DMT AP-1 (10 mg / Kg) to male SD rats. [Figure 17] 1 shows the mean concentration-time profiles of 5-MeO-DMT CP-2 and metabolite 5-MeO-DMT following oral administration of 5-MeO-DMT CP-2 (10 mg / Kg) to male SD rats. [Figure 18] 1 shows the mean concentration-time profiles of 5-MeO-DMT CP-3 and metabolite 5-MeO-DMT following oral administration of 5-MeO-DMT CP-3 (10 mg / Kg) to male SD rats. [Figure 19]1 shows the mean concentration-time profiles of 5-MeO-DMT CP-4 and metabolite 5-MeO-DMT following oral administration of 5-MeO-DMT CP-4 (10 mg / Kg) to male SD rats. [Figure 20] 1 shows the mean concentration-time profiles of 5-MeO-DMT CP-5 and metabolite 5-MeO-DMT following oral administration of 5-MeO-DMT CP-5 (10 mg / Kg) to male SD rats. [Figure 21] 1 shows the mean concentration-time profiles of 5-MeO-DMT AP-1 and metabolite 5-MeO-DMT following oral administration of 5-MeO-DMT AP-1 (10 mg / Kg) to male SD rats. [Figure 22] 1 shows the mean concentration-time profiles of DMT benzamide and metabolite DMT following oral administration of DMT benzamide (10 mg / Kg) to male SD rats. [Figure 23] 1 shows the mean concentration-time profiles of the 5-MeO-DMT prodrug and metabolite 5-MeO-DMT following oral administration of the 5-MeO-DMT prodrug (10 mg / Kg) to male SD rats. [Figure 24] 1 shows the mean concentration-time profiles of the 5-MeO-DMT prodrug and metabolite 5-MeO-DMT following oral administration of the 5-MeO-DMT prodrug (10 mg / Kg) to male SD rats. [Figure 25] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of 5-MeO-DMT methylpivaloylcarbamate (10 mg / Kg) to male SD rats. [Figure 26] 1 shows the mean concentration-time profile of the metabolite DMT following oral administration of DMT methoxyethylcarbamate formate (10 mg / Kg) to male SD rats. [Figure 27] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of 5-MeO-DMT methoxyethylcarbamate (10 mg / Kg) to male SD rats. [Figure 28]1 shows the mean concentration-time profile of the metabolite DMT after oral administration of DMT trimethylolpropaneamide (10 mg / Kg) to male SD rats. [Figure 29] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT after oral administration of 5-MeO-DMT trimethylolpropaneamide (10 mg / Kg) to male SD rats. [Figure 30] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of 5-MeO-DMT 4-piperidinopiperidine urea formate (10 mg / Kg) to male SD rats. [Figure 31] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the 5-MeO-DMT N,N-dimethylurea formate prodrug of 5-MeO-DMT (10 mg / Kg) to male SD rats. [Figure 32] 1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug DMT lysine trihydrochloride (10 mg / Kg) to male SD rats. [Figure 33] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT lysine trihydrochloride (10 mg / Kg) to male SD rats. [Figure 34] 1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug di-DMT urea (symmetric urea) diformate salt (10 mg / Kg) to male SD rats. [Figure 35] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug di-5-MeO-DMT urea (symmetric urea) diformate salt (10 mg / Kg) to male SD rats. [Figure 36] 1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug DMT valine dihydrochloride (10 mg / Kg) to male SD rats. [Figure 37] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT valine dihydrochloride (10 mg / Kg) to male SD rats. [Figure 38] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT N,N-dimethylglycine formate (10 mg / Kg) to male SD rats. [Figure 39] 1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug Phe-N-Me-Gly DMT dihydrochloride (DMT dipeptide) (10 mg / Kg) to male SD rats. [Figure 40] 1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug DMT alanine dihydrochloride (10 mg / Kg) to male SD rats. [Figure 41] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT alanine dihydrochloride (10 mg / Kg) to male SD rats. [Figure 42] 1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug DMT tetramethylphosphorodiamide (10 mg / Kg) to male SD rats. [Figure 43] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT tetramethylphosphorodiamide (10 mg / Kg) to male SD rats. [Figure 44] 1 shows the mean concentration-time profile of the metabolite DMT following oral administration of the prodrug DMT phenylalanine dihydrochloride (10 mg / Kg) to male SD rats. [Figure 45] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT alanine dihydrochloride (10 mg / Kg) to male SD rats. [Figure 46] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT 2,2-dimethylpropyl pivalate carbamate formate (10 mg / Kg) to male SD rats. [Figure 47]1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug DMT N,N-dimethylglycine hydrochloride (10 mg / Kg) to male SD rats. [Figure 48] 1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug DMT methyl pivalate (10 mg / Kg) to male SD rats. [Figure 49] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT methylpivalate (10 mg / Kg) to male SD rats. [Figure 50] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT-3,3-dimethylsuccinate hydrochloride (10 mg / Kg) to male SD rats. [Figure 51] 1 shows the mean concentration-time profile of the metabolite DMT following oral administration of the prodrug DMT 2,2-dimethylpropyl pivalate carbamate formate (10 mg / Kg) to male SD rats. [Figure 52] 1 shows the mean concentration-time profile of the metabolite DMT after oral administration of the prodrug DMT methyl alcohol (10 mg / Kg) to male SD rats. [Figure 53] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT methyl alcohol (10 mg / Kg) to male SD rats. [Figure 54] 1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT carboxy-isopropylvalinate ditrifluoroacetate (10 mg / Kg) to male SD rats. [Figure 55] 1 shows the mean concentration-time profile of the metabolite DMT following oral administration of the prodrug DMT methylsuccinate (10 mg / Kg) to male SD rats. [Figure 56]1 shows the mean concentration-time profile of the metabolite 5-MeO-DMT following oral administration of the prodrug 5-MeO-DMT methylsuccinate (10 mg / Kg) to male SD rats. [Figure 57] 1 shows the mean concentration-time profile of the metabolite DMT following oral administration of the prodrug DMT methyl pivaloylcarbamate formate (10 mg / Kg) to male SD rats. [Figure 58] 1 shows the mean concentration-time profile of the metabolite DMT following oral administration of the glutarate prodrug of DMT (10 mg / Kg) to male SD rats. DETAILED DESCRIPTION OF THE INVENTION

[0045] Described herein is a compound that can be metabolically converted into N,N-dimethyltryptamine or its analog when administered to a subject.The compounds disclosed herein can be useful for treating neurological disorders such as psychiatric disorders, substance abuse disorders, or conditions that benefit from increasing neuroplasticity.

[0046] Definition. The compounds herein may include all stereoisomers, enantiomers, diastereomers, mixtures, racemates, atropisomers, and tautomers thereof.

[0047] Unless otherwise specified, any compound disclosed herein can be substituted. Non-limiting examples of optional substituents include hydroxyl groups, sulfhydryl groups, halogens, amino groups, nitro groups, nitroso groups, cyano groups, azide groups, sulfoxide groups, sulfone groups, sulfonamide groups, carboxyl groups, carboxylic aldehyde groups, imine groups, alkyl groups, haloalkyl groups, alkenyl groups, haloalkenyl groups, alkynyl groups, haloalkynyl groups, alkoxy groups, aryl groups, aryloxy groups, aralkyl groups, arylalkoxy groups, heterocyclylalkyl groups, heteroaryl groups, cycloalkyl groups, acyl groups, acyloxy groups, carbamate groups, amide groups, urea groups, epoxy groups, and ester groups.

[0048] Non-limiting examples of alkyl groups include linear, branched, and cyclic alkyl and alkylene groups. Alkyl groups include, for example, substituted or unsubstituted C1, C2, C3, C4, C5, C6, C7, C8, C9, C10, C11, C12, C13, C14, C15, C16, C17, C18, C19, C20, C21, C22, C23, C24, C25, C26, C27, C28, C29, C30, C31, C32, C33, C34, C35, C36, C37, C38, C39, C40, C41, C42, C43, C44, C45, C46, ​​C47, C48, C49, C50, C51, C52, C53, C54, C55, C56, C57 10 , C 11 , C 12 , C 13 , C 14 , C 15 , C 16 , C 17 , C 18 , C 19 , C 20 , C 21 , C 22 , C 23 , C 24 , C 25 , C 26 , C 27 , C 28 , C 29 , C 30 , C 31 , C 32 , C 33 , C 34 , C 35 , C 36 , C 37 , C 38 , C 39 , C 40 , C 41 , C 42 , C 43 , C 44 , C 45 , C 46 , C 47 , C 48 , C 49 , or C 50 It can be a group.

[0049] Alkyl groups can include branched and unbranched alkyl groups. Non-limiting examples of straight chain alkyl groups include methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, octyl, nonyl, and decyl.

[0050] Branched alkyl groups include any straight chain alkyl group substituted with any number of alkyl groups. Non-limiting examples of branched alkyl groups include isopropyl, isobutyl, sec-butyl, and t-butyl.

[0051] Non-limiting examples of substituted alkyl groups include hydroxymethyl, chloromethyl, trifluoromethyl, aminomethyl, 1-chloroethyl, 2-hydroxyethyl, 1,2-difluoroethyl, and 3-carboxypropyl.

[0052] Non-limiting examples of cycloalkyl groups include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl groups. Cycloalkyl groups also include fused, bridged, and spiro-bicyclic rings, as well as higher fused, bridged, and spiro systems. Cycloalkyl groups can be substituted with any number of linear, branched, or cyclic alkyl groups. Non-limiting examples of cyclic alkyl groups include cyclopropyl, 2-methylcycloprop-1-yl, cycloprop-2-en-1-yl, cyclobutyl, 2,3-dihydroxycyclobut-1-yl, cyclobut-2-en-1-yl, cyclopentyl, cyclopent-2-en-1-yl, cyclopenta-2,4-dien-1-yl, cyclohexyl, cyclohex-2-en-1-yl, cycloheptyl, cyclooctanyl, 2,5-dimethylcyclopent-1-yl, 3,5-dichlorocyclohex-1-yl, 4,5-dimethylcyclopent-1-yl, 4,5-dimethylcyclopent-1-yl, 4,5-dimethylcyclohex ... -hydroxycyclohex-1-yl, 3,3,5-trimethylcyclohex-1-yl, octahydropentenyl, octahydro-1H-indenyl, 3a,4,5,6,7,7a-hexahydro-3H-inden-4-yl, decahydroazulenyl, bicyclo-[2.1.1]hexanyl, bicyclo[2.2.1]heptanyl, bicyclo[3.1.1]heptanyl, 1,3-dimethyl[2.2.1]heptan-2-yl, bicyclo[2.2.2]octanyl, and bicyclo[3.3.3]undecanyl.

[0053] Non-limiting examples of alkenyl groups include straight-chain, branched, and cyclic alkenyl groups. One or more olefins of an alkenyl group can be, for example, E, Z, cis, trans, terminal, or exo-methylene. Alkenyl groups can be, for example, substituted or unsubstituted C2, C3, C4, C5, C6, C7, C8, C9, C10, C11, C12, C13, C14, C15, C16, C17, C18, C19, C20, C21, C22, C23, C24, C25, C26, C27, C28, C29, C30, C31, C32, C33, C34, C35, C36, C37, C38, C39, C40, C41, C42, C43, C44, C45, C46, ​​C47, C4 10 , C 11 , C 12 , C 13 , C 14 , C 15 , C 16 , C 17 , C 18 , C 19 , C 20 , C 21 , C 22 , C 23 , C 24 , C 25 , C 26 , C 27 , C 28 , C 29 , C 30 , C 31 , C 32 , C 33 , C 34 , C 35 , C 36 , C 37 , C 38 , C 39 , C 40 , C 41 , C 42 , C 43 , C 44 , C 45 , C 46 , C 47 , C 48 , C 49 , or C 50 Non-limiting examples of alkenyl and alkenylene groups include ethenyl, prop-1-en-1-yl, isopropenyl, but-1-en-4-yl, 2-chloroethenyl, 4-hydroxybuten-1-yl, 7-hydroxy-7-methyloct-4-en-2-yl, and 7-hydroxy-7-methylocta-3,5-dien-2-yl.

[0054] Non-limiting examples of alkynyl groups include straight-chain, branched, and cyclic alkynyl groups. The triple bond of an alkynyl group can be internal or terminal. An alkynyl or alkynylene group can be, for example, a substituted or unsubstituted C2, C3, C4, C5, C6, C7, C8, C9, C10, C11, C12, C13, C14, C15, C16, C17, C18, C19, C20, C21, C22, C23, C24, C25, C26, C27, C28, C29, C30, C31, C32, C33, C34, C35, C36, C37, C38, C39, C40, C41, C42, C43, C44, C45, C46, ​​C47, C48, C49, C50, 10 , C 11 , C 12 , C 13 , C 14 , C 15 , C 16 , C 17 , C 18 , C 19 , C 20 , C 21 , C 22 , C 23 , C 24 , C 25 , C 26 , C 27 , C 28 , C 29 , C 30 , C 31 , C 32 , C 33 , C 34 , C 35 , C 36 , C 37 , C 38 , C 39 , C 40 , C 41 , C 42 , C 43 , C 44 , C 45 , C 46 , C 47 , C 48 , C 49 , or C 50 Non-limiting examples of alkynyl groups include ethynyl, prop-2-yn-1-yl, prop-1-yn-1-yl, and 2-methyl-hex-4-yn-1-yl; 5-hydroxy-5-methylhex-3-yn-1-yl, 6-hydroxy-6-methylhept-3-yn-2-yl, and 5-hydroxy-5-ethylhept-3-yn-1-yl.

[0055] A haloalkyl group can be any alkyl group substituted with any number of halogen atoms, such as fluorine, chlorine, bromine, and iodine atoms. A halo-alkenyl group can be any alkenyl group substituted with any number of halogen atoms. A halo-alkynyl group can be any alkynyl group substituted with any number of halogen atoms.

[0056] An alkoxy group can be, for example, an oxygen atom substituted with any alkyl, alkenyl, or alkynyl group. Ether or ether groups include alkoxy groups. Non-limiting examples of alkoxy groups include methoxy, ethoxy, propoxy, isopropoxy, and isobutoxy.

[0057] A heterocycle can be any ring containing a non-carbon ring atom, such as N, O, S, P, Si, B, or any other heteroatom. A heterocycle can be substituted with any number of substituents, such as alkyl groups and halogen atoms. A heterocycle can be aromatic (heteroaryl) or non-aromatic. Non-limiting examples of heterocycles include pyrrole, pyrrolidine, pyridine, piperidine, succinamide, maleimide, morpholine, imidazole, thiophene, furan, tetrahydrofuran, pyran, and tetrahydropyran.

[0058] Non-limiting examples of heterocyclic rings include heterocyclic units having a single ring containing one or more heteroatoms, non-limiting examples of which include diazirinyl, aziridinyl, azetidinyl, pyrazolidinyl, imidazolidinyl, oxazolidinyl, isoxazolinyl, thiazolidinyl, isothiazolinyl, oxathiazolidinonyl, oxazolidinonyl, hydantoinyl, tetrahydrofuranyl, pyrrolidinyl, morpholinyl, piperazinyl, piperidinyl, dihydropyranyl, tetrahydropyranyl, piperidin-2-onyl, 2,3,4,5-tetrahydro-1H- azepinyl, 2,3-dihydro-1H-indole, and 1,2,3,4-tetrahydroquinoline), and ii) heterocyclic units having two or more rings, one of which is a heterocyclic ring (non-limiting examples of which include hexahydro-1H-pyrrolidinyl, 3a,4,5,6,7,7a-hexahydro-1H-benzo[d]imidazolyl, 3a,4,5,6,7,7a-hexahydro-1H-indolyl, 1,2,3,4-tetrahydroquinolinyl, and decahydro-1H-cycloocta[b]pyrrolyl).

[0059] Non-limiting examples of heteroaryls include: i) heteroaryl rings containing a single ring (non-limiting examples of which include 1,2,3,4-tetrazolyl, [1,2,3]triazolyl, [1,2,4]triazolyl, triazinyl, thiazolyl, 1H-imidazolyl, oxazolyl, isoxazolyl, isothiazolyl, furanyl, thiophenyl, pyrimidinyl, 2-phenylpyrimidinyl, pyridinyl, 3-methylpyridinyl, and 4-dimethylaminopyridinyl); and ii) heteroaryl rings containing two or more rings. (one of which is a heteroaryl ring) (non-limiting examples of which include 7H-purinyl, 9H-purinyl, 6-amino-9H-purinyl, 5H-pyrrolo[3,2-d]pyrimidinyl, 7H-pyrrolo[2,3-d]pyrimidinyl, pyrido[2,3-d]pyrimidinyl, 4,5,6,7-tetrahydro-1-H-indolyl, quinoxalinyl, quinazolinyl, quinolinyl, 8-hydroxy-quinolinyl, and isoquinolinyl).

[0060] "Alkyl" refers to an optionally substituted straight-chain or optionally substituted branched-chain saturated hydrocarbon having 1 to about 10 carbon atoms, or 1 to 6 carbon atoms, and the sp of the alkyl residue 3 The -hybridization carbon is attached to the rest of the molecule by a single bond. Examples include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, 2-methyl-1-propyl, 2-methyl-2-propyl, 2-methyl-1-butyl, 3-methyl-1-butyl, 2-methyl-3-butyl, 2,2-dimethyl-1-propyl, 2-methyl-1-pentyl, 3-methyl-1-pentyl, 4-methyl-1-pentyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl, 2,2-dimethyl-1-butyl, 3,3-dimethyl-1-butyl, 2-ethyl-1-butyl, butyl, isobutyl, sec-butyl, t-butyl, n-pentyl, isopentyl, neopentyl, tert-amyl, and hexyl, as well as longer alkyl groups such as heptyl, octyl, and the like. Whenever a numerical range appears herein, such as "C1-C6 alkyl," means that the alkyl group consists of 1 carbon atom, 2 carbon atoms, 3 carbon atoms, 4 carbon atoms, 5 carbon atoms, or 6 carbon atoms, but this definition also encompasses occurrences of the term "alkyl" where no numerical range is specified. In some embodiments, alkyl refers to any of C1-C6 alkyl groups. 10The alkyl group may be alkyl, C1-C9 alkyl, C1-C8 alkyl, C1-C7 alkyl, C1-C6 alkyl, C1-C5 alkyl, C1-C4 alkyl, C1-C3 alkyl, C1-C2 alkyl, or C1 alkyl. Unless stated otherwise in the specification, an alkyl group is optionally substituted with, for example, oxo, halogen, amino, nitrile, nitro, hydroxyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, an alkyl is optionally substituted with oxo, halogen, -CN, -CF3, -OH, -OMe, -NH2, or -NO2. In some embodiments, an alkyl is optionally substituted with oxo, halogen, -CN, -CF3, -OH, or -OMe. In some embodiments, an alkyl is optionally substituted with halogen.

[0061] "Alkenyl" refers to an optionally substituted straight chain or an optionally substituted branched chain hydrocarbon having one or more carbon-carbon double bonds and having from 2 to about 10 carbon atoms, more preferably from 2 to about 6 carbon atoms, and the sp of the alkenyl residue 2 The -hybridization carbon is connected to the rest of the molecule by a single bond. The group may be in either the cis or trans conformation about the double bond(s) and should be understood to include both isomers. Examples include, but are not limited to, ethenyl (-CH=CH), 1-propenyl (-CHCH=CH), isopropenyl [-C(CH)=CH], butenyl, 1,3-butadienyl, and the like. Whenever appearing herein, a numerical range such as "C2-C6 alkenyl" means that the alkenyl group can consist of 2 carbon atoms, 3 carbon atoms, 4 carbon atoms, 5 carbon atoms, or 6 carbon atoms, although this definition also encompasses occurrences of the term "alkenyl" where no numerical range is specified. In some embodiments, alkenyl refers to a C2-C6 alkenyl. 10Alkenyl is C2-C9 alkenyl, C2-C8 alkenyl, C2-C7 alkenyl, C2-C6 alkenyl, C2-C5 alkenyl, C2-C4 alkenyl, C2-C3 alkenyl, or C2 alkenyl. Unless stated otherwise in the specification, alkenyl groups are optionally substituted with, for example, oxo, halogen, amino, nitrile, nitro, hydroxyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, alkenyl is optionally substituted with oxo, halogen, -CN, -CF3, -OH, -OMe, -NH2, or -NO2. In some embodiments, alkenyl is optionally substituted with oxo, halogen, -CN, -CF3, -OH, or -OMe. In some embodiments, alkenyl is optionally substituted with halogen.

[0062] "Alkynyl" refers to an optionally substituted straight-chain or optionally substituted branched-chain hydrocarbon having one or more carbon-carbon triple bonds and having from 2 to about 10 carbon atoms, more preferably from 2 to about 6 carbon atoms. Examples include, but are not limited to, ethynyl, 2-propynyl, 2-butynyl, 1,3-butadinyl, and the like. Whenever it appears herein, a numerical range such as "C2-C6 alkynyl" means that the alkynyl group can consist of 2 carbon atoms, 3 carbon atoms, 4 carbon atoms, 5 carbon atoms, or 6 carbon atoms, although this definition also encompasses occurrences of the term "alkynyl" where no numerical range is specified. In some embodiments, alkynyl refers to any of the C2-C6 alkynyl groups. 10alkynyl, C2-C9 alkynyl, C2-C8 alkynyl, C2-C7 alkynyl, C2-C6 alkynyl, C2-C5 alkynyl, C2-C4 alkynyl, C2-C3 alkynyl, or C2 alkynyl. Unless stated otherwise in the specification, alkynyl groups are optionally substituted with, for example, oxo, halogen, amino, nitrile, nitro, hydroxyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, alkynyl is optionally substituted with oxo, halogen, -CN, -CF3, -OH, -OMe, -NH2, or -NO2. In some embodiments, alkynyl is optionally substituted with oxo, halogen, -CN, -CF3, -OH, or -OMe. In some embodiments, alkynyl is optionally substituted with halogen.

[0063] "Alkoxy" means a group of the formula -OR a where R a is an alkyl radical as defined herein. Unless stated otherwise in the specification, an alkoxy group can be optionally substituted with, for example, oxo, halogen, amino, nitrile, nitro, hydroxyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, an alkoxy is optionally substituted with oxo, halogen, -CN, -CF3, -OH, -OMe, -NH2, or -NO2. In some embodiments, an alkoxy is optionally substituted with oxo, halogen, -CN, -CF3, -OH, or -OMe. In some embodiments, an alkoxy is optionally substituted with halogen.

[0064] "Aminoalkyl" refers to an alkyl radical, as defined above, substituted with one or more amines. In some embodiments, the alkyl is substituted with one amine. In some embodiments, the alkyl is substituted with one, two, or three amines. Hydroxyalkyl includes, for example, aminomethyl, aminoethyl, aminopropyl, aminobutyl, or aminopentyl. In some embodiments, the hydroxyalkyl is aminomethyl.

[0065] "Aryl" refers to a radical derived from a hydrocarbon ring system containing hydrogen, 6 to 30 carbon atoms, and at least one aromatic ring. The aryl radical can be a monocyclic, bicyclic, tricyclic, or tetracyclic ring system, which can include fused (when fused to a cycloalkyl or heterocyclylalkyl ring, the aryl is attached through an aromatic ring atom) or bridged ring systems. In some embodiments, the aryl is a 6- to 10-membered aryl. In some embodiments, the aryl is a 6-membered aryl. Aryl radicals include, but are not limited to, aryl radicals derived from the hydrocarbon ring systems of anthrylene, naphthylene, phenanthrylene, anthracene, azulene, benzene, chrysene, fluoranthene, fluorene, as-indacene, s-indacene, indane, indene, naphthalene, phenalene, phenanthrene, pleiadene, pyrene, and triphenylene. In some embodiments, the aryl is phenyl. Unless stated otherwise in the specification, aryl can be optionally substituted with, for example, halogen, amino, nitrile, nitro, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, aryl is optionally substituted with halogen, methyl, ethyl, -CN, -CF3, -OH, -OMe, -NH2, or -NO2. In some embodiments, aryl is optionally substituted with halogen, methyl, ethyl, -CN, -CF3, -OH, or -OMe. In some embodiments, aryl is optionally substituted with halogen.

[0066] "Cycloalkyl" refers to a stable, partially or fully saturated monocyclic or polycyclic carbocyclic ring, which may include fused (when fused to an aryl or heteroaryl ring, the cycloalkyl is attached through a non-aromatic ring atom), bridged, or spiro ring systems. Representative cycloalkyls include those having 3 to 15 carbon atoms (C3-C4). 15 cycloalkyl), 3 to 10 carbon atoms (C3-C 10Examples of cycloalkyl include, but are not limited to, cycloalkyls having 3 to 8 carbon atoms (C3-C8 cycloalkyl), 3 to 6 carbon atoms (C3-C6 cycloalkyl), 3 to 5 carbon atoms (C3-C5 cycloalkyl), or 3 to 4 carbon atoms (C3-C4 cycloalkyl). In some embodiments, cycloalkyls are 3 to 6-membered cycloalkyls. In some embodiments, cycloalkyls are 5 to 6-membered cycloalkyls. Monocyclic cycloalkyls include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. Examples of polycyclic cycloalkyl or carbocycle include adamantyl, norbornyl, decalinyl, bicyclo[3.3.0]octane, bicyclo[4.3.0]nonane, cis-decalin, trans-decalin, bicyclo[2.1.1]hexane, bicyclo[2.2.1]heptane, bicyclo[2.2.2]octane, bicyclo[3.2.2]nonane, and bicyclo[3.3.2]decane, and 7,7-dimethyl-bicyclo[2.2.1]heptanyl. Examples of partially saturated cycloalkyl include cyclopentenyl, cyclohexenyl, cycloheptenyl, and cyclooctenyl. Unless otherwise specified herein, cycloalkyl is optionally substituted with, for example, oxo, halogen, amino, nitrile, nitro, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, cycloalkyl is optionally substituted with oxo, halogen, methyl, ethyl, -CN, -CF3, -OH, -OMe, -NH2, or -NO2. In some embodiments, cycloalkyl is optionally substituted with oxo, halogen, methyl, ethyl, -CN, -CF3, -OH, or -OMe. In some embodiments, cycloalkyl is optionally substituted with halogen.

[0067] "Deuterated alkyl" refers to an alkyl radical, as defined above, that is substituted with one or more deuterium atoms. In some embodiments, the alkyl is substituted with one deuterium atom. In some embodiments, the alkyl is substituted with one, two, or three deuterium atoms. In some embodiments, the alkyl is substituted with one, two, three, four, five, or six deuterium atoms. Deuterated alkyls include, for example, CD3, CHD, CHD, CHCD, CDCD, CHDCD, CHCHD, or CHCHD. In some embodiments, the deuterated alkyl is CD3.

[0068] "Haloalkyl" refers to an alkyl radical, as defined above, substituted with one or more halogens. In some embodiments, the alkyl is substituted with one, two, or three halogens. In some embodiments, the alkyl is substituted with one, two, three, four, five, or six halogens. Haloalkyl includes, for example, trifluoromethyl, difluoromethyl, fluoromethyl, trichloromethyl, 2,2,2-trifluoroethyl, 1,2-difluoroethyl, 3-bromo-2-fluoropropyl, 1,2-dibromoethyl, and the like. In some embodiments, the haloalkyl is trifluoromethyl.

[0069] "Halo" or "halogen" refers to bromo, chloro, fluoro, or iodo. In some embodiments, halogen is fluoro or chloro. In some embodiments, halogen is fluoro.

[0070] "Heteroalkyl" refers to an alkyl group in which one or more skeletal atoms of the alkyl are selected from an atom other than carbon, e.g., oxygen, nitrogen (e.g., -NH-, -N(alkyl)-), sulfur, or a combination thereof. The heteroalkyl is attached to the remainder of the molecule at a carbon atom of the heteroalkyl. In one embodiment, the heteroalkyl is a C1-C6 heteroalkyl, where the heteroalkyl is composed of 1 to 6 carbon atoms and one or more atoms other than carbon, e.g., oxygen, nitrogen (e.g., -NH-, -N(alkyl)-), sulfur, or a combination thereof, and the heteroalkyl is attached to the remainder of the molecule at a carbon atom of the heteroalkyl. Examples of such heteroalkyls are, for example, -CHOCH3, -CHCHOCH3, -CHCHOCH2CH2OCH3, or -CH(CH3)OCH3. Unless stated otherwise in the specification, heteroalkyl is optionally substituted with, for example, oxo, halogen, amino, nitrile, nitro, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, heteroalkyl is optionally substituted with oxo, halogen, methyl, ethyl, -CN, -CF3, -OH, -OMe, -NH2, or -NO2. In some embodiments, heteroalkyl is optionally substituted with oxo, halogen, methyl, ethyl, -CN, -CF3, -OH, or -OMe. In some embodiments, heteroalkyl is optionally substituted with halogen.

[0071] "Hydroxyalkyl" refers to an alkyl radical, as defined above, substituted with one or more hydroxyls. In some embodiments, the alkyl is substituted with one hydroxyl. In some embodiments, the alkyl is substituted with one, two, or three hydroxyls. Hydroxyalkyl includes, for example, hydroxymethyl, hydroxyethyl, hydroxypropyl, hydroxybutyl, or hydroxypentyl. In some embodiments, the hydroxyalkyl is hydroxymethyl.

[0072] "Heterocyclylalkyl" refers to a stable 3- to 24-membered partially or fully saturated ring radical containing 2 to 23 carbon atoms and 1 to 8 heteroatoms selected from the group consisting of nitrogen, oxygen, phosphorus, and sulfur. Unless stated otherwise in the specification, a heterocyclylalkyl radical can be a monocyclic, bicyclic, tricyclic, or tetracyclic ring system, which can include fused (when fused to an aryl or heteroaryl ring, the heterocyclylalkyl is attached through a non-aromatic ring atom) or bridged ring systems, and the nitrogen, carbon, or sulfur atoms in the heterocyclylalkyl radical can be optionally oxidized, and the nitrogen atom can be optionally quaternized.

[0073] Representative heterocyclylalkyls include those containing 2 to 15 carbon atoms (C2-C 15 heterocyclylalkyl), 2 to 10 carbon atoms (C2-C 10Examples of heterocyclylalkyl include, but are not limited to, heterocyclylalkyls having 2 to 8 carbon atoms (C2-C8 heterocyclylalkyl), 2 to 6 carbon atoms (C2-C6 heterocyclylalkyl), 2 to 5 carbon atoms (C2-C5 heterocyclylalkyl), or 2 to 4 carbon atoms (C2-C4 heterocyclylalkyl). In some embodiments, the heterocyclylalkyl is a 3- to 6-membered heterocyclylalkyl. In some embodiments, the cycloalkyl is a 5- to 6-membered heterocyclylalkyl. Examples of such heterocyclylalkyl radicals include aziridinyl, azetidinyl, dioxolanyl, thienyl[1,3]dithianyl, decahydroisoquinolyl, imidazolinyl, imidazolidinyl, isothiazolidinyl, isoxazolidinyl, morpholinyl, octahydroindolyl, octahydroisoindolyl, 2-oxopiperazinyl, 2-oxopiperidinyl, 2-oxopyrrolidinyl, oxazolidinyl, piperidinyl, piperazinyl, 4-piperidonyl, pyrrolidinyl, Examples of heterocyclylalkyl include, but are not limited to, pyrazolidinyl, quinuclidinyl, thiazolidinyl, tetrahydrofuryl, trithianyl, tetrahydropyranyl, thiomorpholinyl, thiamorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxo-thiomorpholinyl, 1,3-dihydroisobenzofuran-1-yl, 3-oxo-1,3-dihydroisobenzofuran-1-yl, methyl-2-oxo-1,3-dioxol-4-yl, and 2-oxo-1,3-dioxol-4-yl. The term heterocyclylalkyl also includes all ring forms of carbohydrates, including, but not limited to, monosaccharides, disaccharides, and oligosaccharides. When referring to the number of carbon atoms of a heterocyclylalkyl, it is understood that the number of carbon atoms of the heterocyclylalkyl is not the same as the total number of atoms (including heteroatoms) that make up the heterocyclylalkyl (i.e., the skeletal atoms of the heterocyclylalkyl ring).Unless stated otherwise in the specification, heterocyclylalkyl is optionally substituted with, for example, oxo, halogen, amino, nitrile, nitro, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, heterocyclylalkyl is optionally substituted with oxo, halogen, methyl, ethyl, -CN, -CF3, -OH, -OMe, -NH2, or -NO2. In some embodiments, heterocyclylalkyl is optionally substituted with oxo, halogen, methyl, ethyl, -CN, -CF3, -OH, or -OMe. In some embodiments, heterocyclylalkyl is optionally substituted with halogen.

[0074] "Heteroaryl" refers to a 5- to 14-membered ring system containing a hydrogen atom; 1 to 13 carbon atoms; 1 to 6 heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur; and at least one aromatic ring. The heteroaryl radical can be a monocyclic, bicyclic, tricyclic, or tetracyclic ring system, which can include fused (when fused to a cycloalkyl or heterocyclylalkyl ring, the heteroaryl is attached through an aromatic ring atom) or bridged ring systems, and the nitrogen, carbon, or sulfur atoms in the heteroaryl radical can be optionally oxidized, and the nitrogen atom can be optionally quaternized. In some embodiments, the heteroaryl is a 5- to 10-membered heteroaryl. In some embodiments, the heteroaryl is a 5- to 6-membered heteroaryl.Examples include azepinyl, acridinyl, benzimidazolyl, benzothiazolyl, benzindolyl, benzodioxolyl, benzofuranyl, benzoxazolyl, benzothiazolyl, benzothiadiazolyl, benzo[b][1,4]dioxepinyl, 1,4-benzodioxanyl, benzonaphthofuranyl, benzoxazolyl, benzodioxolyl, benzodioxinyl, benzopyranyl, benzopyranonyl, benzofuranyl, benzofuranonyl, benzothienyl (benzothiophenyl), benzotriazolyl, benzo[4,6]imidazo[1,2-a]pyridinyl, carbazolyl, cinnolinyl, dibenzofuranyl, dibenzothiophenyl, furanyl, furanonyl, isothiazolyl, imidazolyl, indazolyl, indolyl, indazolyl, isoindolyl, indophenyl, and indophenyl. Examples include, but are not limited to, dolinyl, isoindolinyl, isoquinolyl, indolizinyl, isoxazolyl, naphthyridinyl, oxadiazolyl, 2-oxoazepinyl, oxazolyl, oxiranyl, 1-oxidopyridinyl, 1-oxidopyrimidinyl, 1-oxidopyrazinyl, 1-oxidopyridazinyl, 1-phenyl-1H-pyrrolyl, phenazinyl, phenothiazinyl, phenoxazinyl, phthalazinyl, pteridinyl, purinyl, pyrrolyl, pyrazolyl, pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, quinazolinyl, quinoxalinyl, quinolinyl, quinuclidinyl, isoquinolinyl, tetrahydroquinolinyl, thiazolyl, thiadiazolyl, triazolyl, tetrazolyl, triazinyl, and thiophenyl (i.e., thienyl). Unless stated otherwise in the specification, heteroaryl is optionally substituted with, for example, halogen, amino, nitrile, nitro, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, aryl, cycloalkyl, heterocyclylalkyl, heteroaryl, etc. In some embodiments, heteroaryl is optionally substituted with halogen, methyl, ethyl, -CN, -CF, -OH, -OMe, -NH, or -NO. In some embodiments, heteroaryl is optionally substituted with halogen, methyl, ethyl, -CN, -CF, -OH, or -OMe.In some embodiments, the heteroaryl is optionally substituted with halogen.

[0075] Any compound herein can be purified. Compounds herein can be at least 1% pure, at least 2% pure, at least 3% pure, at least 4% pure, at least 5% pure, at least 6% pure, at least 7% pure, at least 8% pure, at least 9% pure, at least 10% pure, at least 11% pure, at least 12% pure, at least 13% pure, at least 14% pure, at least 15% pure, at least 16% pure, at least 17% pure, at least 18% pure, at least 19% pure, at least 20% pure, at least 21% pure, at least 22% pure, at least 23% pure, at least 24% pure, at least 25% pure, at least 26% pure, at least 27% pure, at least 28% pure, at least 29% pure, at least 30% pure, at least 31% pure, at least 32% pure, at least 33% pure, at least 34% pure, at least 35% pure, at least 36% pure, at least 37% pure, at least 38% pure, at least 39% pure, at least 40% pure, at least 41% pure, at least 42% pure, at least 43% pure, at least 44% pure, at least 45% pure, at least 46% pure, at least 47% pure, at least 48% pure, at least 49% pure, at least 50% pure, at least 51% pure, at least 52% pure, at least 53% pure, at least 54% pure, at least 55% pure, at least 56% pure, at least 57% pure, at least 58% pure, at least 59% pure, at least 60% pure, at least 61% pure, at least 62% pure, at least 63% pure, at least 6 Pure, at least 23% pure, at least 24% pure, at least 25% pure, at least 26% pure, at least 27% pure, at least 28% pure, at least 29% pure, at least 30% pure, at least 31% pure, at least 32% pure, at least 33% pure, at least 34% pure, at least 35% pure, at least 36% pure, at least 37% pure, at least 38% pure, at least 39% pure, at least 40% pure, at least 41% pure, at least 42% pure, at least 43% pure, at least 44% pure Pure, at least 45% pure, at least 46% pure, at least 47% pure, at least 48% pure, at least 49% pure, at least 50% pure, at least 51% pure, at least 52% pure, at least 53% pure, at least 54% pure, at least 55% pure, at least 56% pure, at least 57% pure, at least 58% pure, at least 59% pure, at least 60% pure, at least 61% pure, at least 62% pure, at least 63% pure, at least 64% pure, at least 65% pure, at least 66% pure , at least 67% pure, at least 68% pure, at least 69% pure, at least 70% pure, at least 71% pure, at least 72% pure, at least 73% pure, at least 74% pure, at least 75% pure, at least 76% pure, at least 77% pure, at least 78% pure, at least 79% pure, at least 80% pure, at least 81% pure, at least 82% pure, at least 83% pure, at least 84% pure, at least 85% pure, at least 86% pure, at least 87% pure, at least 88% pure,It can be at least 89% pure, at least 90% pure, at least 91% pure, at least 92% pure, at least 93% pure, at least 94% pure, at least 95% pure, at least 96% pure, at least 97% pure, at least 98% pure, at least 99% pure, at least 99.1% pure, at least 99.2% pure, at least 99.3% pure, at least 99.4% pure, at least 99.5% pure, at least 99.6% pure, at least 99.7% pure, at least 99.8% pure, or at least 99.9% pure.

[0076] Pharmaceutically acceptable salts. The present disclosure provides the use of pharmaceutically acceptable salts of any compound described herein. Pharmaceutically acceptable salts include, for example, acid addition salts and base addition salts. The acid added to the compound to form the acid addition salt can be an organic acid or an inorganic acid. The base added to the compound to form the base addition salt can be an organic base or an inorganic base. In some embodiments, the pharmaceutically acceptable salt is a metal salt. In some embodiments, the pharmaceutically acceptable salt is an ammonium salt.

[0077] Metal salts can be formed by the addition of an inorganic base to a compound of the present disclosure. Inorganic bases consist of a metal cation paired with a basic counterion, such as hydroxide, carbonate, bicarbonate, or phosphate. The metal can be an alkali metal, alkaline earth metal, transition metal, or main group metal. In some embodiments, the metal is lithium, sodium, potassium, cesium, cerium, magnesium, manganese, iron, calcium, strontium, cobalt, titanium, aluminum, copper, cadmium, or zinc.

[0078] In some embodiments, the metal salt is a lithium salt, a sodium salt, a potassium salt, a cesium salt, a cerium salt, a magnesium salt, a manganese salt, an iron salt, a calcium salt, a strontium salt, a cobalt salt, a titanium salt, an aluminum salt, a copper salt, a cadmium salt, or a zinc salt.

[0079] Ammonium salts can be generated by adding ammonia or an organic amine to a compound of the present disclosure. In some embodiments, the organic amine is trimethylamine, triethylamine, diisopropylamine, ethanolamine, diethanolamine, triethanolamine, morpholine, N-methylmorpholine, piperidine, N-methylpiperidine, N-ethylpiperidine, dibenzylamine, piperazine, pyridine, pyrazole, pyrazolidine, pyrazoline, pyridazine, pyrimidine, imidazole, or pyrazine.

[0080] In some embodiments, the ammonium salt is a triethylamine salt, a trimethylamine salt, a diisopropylamine salt, an ethanolamine salt, a diethanolamine salt, a triethanolamine salt, a morpholine salt, an N-methylmorpholine salt, a piperidine salt, an N-methylpiperidine salt, an N-ethylpiperidine salt, a dibenzylamine salt, a piperazine salt, a pyridine salt, a pyrazole salt, a pyridazine salt, a pyrimidine salt, an imidazole salt, or a pyrazine salt.

[0081] Acid addition salts can be formed by the addition of an acid to a compound of the present disclosure. In some embodiments, the acid is organic. In some embodiments, the acid is inorganic. In some embodiments, the acid is hydrochloric acid, hydrobromic acid, hydroiodic acid, nitric acid, nitrous acid, sulfuric acid, sulfurous acid, phosphoric acid, isonicotinic acid, lactic acid, salicylic acid, tartaric acid, ascorbic acid, gentisic acid, gluconic acid, glucuronic acid, saccharic acid, formic acid, benzoic acid, glutamic acid, pantothenic acid, acetic acid, propionic acid, butyric acid, fumaric acid, succinic acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, citric acid, oxalic acid, or maleic acid.

[0082] In some embodiments, the salt is hydrochloride, hydrobromide, hydroiodide, nitrate, nitrite, sulfate, sulfite, phosphate, isonicotinate, lactate, salicylate, tartrate, ascorbate, gentisate, gluconate, glucuronate, saccharate, formate, benzoate, glutamate, pantothenate, acetate, propionate, butyrate, fumarate, succinate, methanesulfonate, ethanesulfonate, benzenesulfonate, p-toluenesulfonate, citrate, oxalate, or maleate.

[0083] Pharmaceutical compositions. According to another embodiment, the present disclosure provides a composition comprising a compound of the present disclosure and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The amount of the compound in the composition is an amount effective to treat the relevant disease, disorder, or condition in a patient in need thereof ("effective amount"). In some embodiments, the composition of the present disclosure is formulated for oral administration to a patient.

[0084] The term "pharmaceutically acceptable carrier, adjuvant, or vehicle" refers to a non-toxic carrier, adjuvant, or vehicle that does not destroy the pharmacological activity of the agent with which it is formulated. Pharmaceutically acceptable carriers, adjuvants, or vehicles that may be used in the compositions of the present disclosure include, but are not limited to, ion exchangers, alumina, stearates such as aluminum stearate, lecithin, serum proteins such as human serum albumin, buffer substances such as phosphates, saturated vegetable fatty acids such as glycine, sorbic acid, potassium sorbate, and protamine sulfate, water, partial glyceride mixtures of salts or electrolytes, disodium hydrogen phosphate, potassium hydrogen phosphate, sodium chloride, zinc salts, colloidal silica, magnesium trisilicate, polyvinylpyrrolidone, cellulose-based substances, polyethylene glycol, sodium carboxymethylcellulose, polyacrylates, waxes, polyethylene-polyoxypropylene-block polymers, polyethylene glycol, and wool fat.

[0085] The compositions of the present disclosure may be administered orally, parenterally, enterally, intravesically, intraperitoneally, by inhalation spray, topically, rectally, nasally, buccally, vaginally, or via an implanted reservoir. As used herein, the term "parenteral" includes subcutaneous, intravenous, intramuscular, intra-articular, intrasynovial, intrasternal, intrathecal, intrahepatic, intralesional, and intracranial injection or infusion techniques. In some embodiments, the compositions are administered orally, intraperitoneally, or intravenously. In some embodiments, the compositions are transmucosal formulations. Sterile injectable forms of the compositions of the present disclosure may be aqueous or oily suspensions. These suspensions may be formulated according to techniques known in the art using suitable dispersing or wetting agents and suspending agents. The sterile injectable formulation may also be a sterile injectable solution or suspension in a parenterally acceptable non-toxic diluent or solvent, such as a solution in 1,3-butanediol. Among the acceptable vehicles and solvents that may be employed are water, Ringer's solution, and isotonic sodium chloride solution. In addition, sterile, fixed oils are conventionally employed as a solvent or suspending medium.

[0086] Any sterile fixed oil, including synthetic mono- or diglycerides, may be used to aid in the delivery of the composition.Fatty acids such as oleic acid and its glyceride derivatives are useful for the preparation of injectables, as well as natural pharmaceutically acceptable oils such as olive oil or castor oil, especially in their polyoxyethylated versions.These oil solutions or suspensions may also contain long-chain alcohol diluents or dispersants, such as carboxymethylcellulose or similar dispersants, which are commonly used in the formulation of pharmaceutically acceptable dosage forms, including emulsions or suspensions.Other commonly used surfactants, such as Tween, Span, and other emulsifiers or bioavailability enhancers, commonly used in the manufacture of pharmaceutically acceptable solid, liquid, or other dosage forms, may also be used for formulation purposes.

[0087] Pharmaceutically acceptable compositions can be orally administered in any orally acceptable dosage form, including but not limited to capsules, tablets, aqueous suspensions or solutions.For tablets for oral use, commonly used carriers include lactose and cornstarch.Lubricants such as magnesium stearate can also be added.For oral administration in capsule form, useful diluents include lactose and dry cornstarch.When aqueous suspensions are required for oral use, active ingredients are combined with emulsifiers and suspending agents.If desired, certain sweeteners, flavorings or coloring agents can also be added.

[0088] Alternatively, the pharmaceutically acceptable composition can be administered in the form of suppositories for rectal administration. These can be prepared by mixing the agent with a suitable non-irritating excipient that is solid at room temperature but liquid at rectal temperature, thereby melting in the rectum and releasing the drug. Such materials include cocoa butter, beeswax, and polyethylene glycol.

[0089] In some embodiments, the pharmaceutically acceptable composition is formulated for oral administration. Such formulations may be administered with or without food. In some embodiments, the pharmaceutically acceptable composition is administered without food. In other embodiments, the pharmaceutically acceptable composition is administered with food.

[0090] It should also be understood that the specific dosage and treatment regimen for any particular patient will depend on a variety of factors, including the activity of the specific compound employed, the patient's age, body weight, general health, sex, diet, time of administration, rate of excretion, drug combination, and the judgment of the treating physician, and the severity of the particular disease being treated.

[0091] Liquid dosage forms for oral administration include, but are not limited to, pharmaceutically acceptable emulsions, microemulsions, solutions, suspensions, syrups, and elixirs.In addition to the active compound, liquid dosage forms may contain inert diluents commonly used in the art, such as water or other solvents, solubilizers, and emulsifiers such as ethyl alcohol, isopropyl alcohol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butylene glycol, dimethylformamide, oils (especially cottonseed oil, peanut oil, corn oil, germ oil, olive oil, castor oil, and sesame oil), glycerol, tetrahydrofurfuryl alcohol, polyethylene glycol, and fatty acid ester sorbitan, and mixtures thereof.In addition to inert diluents, oral compositions may also contain adjuvants such as wetting agents, emulsifiers and suspending agents, sweeteners, flavorings, and fragrances.

[0092] Injectable preparations, for example, sterile injectable aqueous or oleaginous suspensions, can be formulated according to known techniques using suitable dispersing or wetting agents and suspending agents. Sterile injectable preparations can also be sterile injectable solutions, suspensions, or emulsions in parenterally acceptable non-toxic diluents or solvents, such as solutions in 1,3-butanediol. Acceptable vehicles and solvents that may be used include water, Ringer's solution, USP, and isotonic sodium chloride solution. Additionally, sterile fixed oils are conventionally used as solvents or suspending media. For this purpose, any brand of fixed oil can be used, including synthetic mono- or diglycerides. Additionally, fatty acids such as oleic acid can be used in the preparation of injectables.

[0093] Injectable formulations can be sterilized, for example, by filtration through a bacterial-retaining filter, or by incorporating sterilizing agents in the form of sterile solid compositions which can be dissolved or dispersed in sterile water or other sterile injectable medium before use.

[0094] To prolong the effect of the compounds of the present disclosure, it may be desirable to slow the absorption of the compounds from subcutaneous or intramuscular injection. This can be accomplished by using a liquid suspension of crystalline or amorphous material with poor water solubility. Therefore, the rate of absorption of a composition will depend on its dissolution rate, which may vary depending on crystal size and crystalline form. Alternatively, delayed absorption of a parenterally administered compound form can be achieved by dissolving or suspending the compound in an oil vehicle. Injectable depot forms are made by forming microencapsulated matrices of the compound in biodegradable polymers such as polylactide-polyglycolide. The release rate of the compound can be controlled depending on the ratio of compound to polymer and the nature of the particular polymer used. Examples of other biodegradable polymers include poly(orthoesters) and poly(anhydrides). Depot injectable formulations can also be prepared by entrapping the compound in liposomes or microemulsions that are compatible with body tissues.

[0095] Compositions for rectal or vaginal administration are preferably suppositories which can be prepared by mixing a compound of the present disclosure with a suitable non-irritating excipient or carrier, such as cocoa butter, polyethylene glycol, or a suppository wax, which is solid at ordinary temperatures but liquid at body temperature and therefore will melt in the rectum or vaginal cavity and release the active compound.

[0096] Solid dosage forms for oral administration include capsules, tablets, pills, powders, and granules. In such solid dosage forms, the active compound is mixed with at least one inert pharmaceutically acceptable excipient or carrier such as sodium citrate or dicalcium phosphate, and / or a) fillers or extenders such as starches, lactose, sucrose, glucose, mannitol, and silicic acid; b) binders such as, for example, carboxymethylcellulose, alginates, gelatin, polyvinylpyrrolidone, sucrose, and acacia; c) humectants such as glycerol; d) disintegrating agents such as agar-agar, calcium carbonate, potato or tapioca starch, alginic acid, certain silicates, and sodium carbonate; e) solution retardants such as paraffin; f) absorption accelerators such as quaternary ammonium compounds; g) wetting agents such as, for example, cetyl alcohol and glycerol monostearate; h) absorbents such as kaolin and bentonite clay; and i) lubricants such as talc, calcium stearate, magnesium stearate, solid polyethylene glycols, sodium lauryl sulfate, and mixtures thereof. In the case of capsules, tablets and pills, the dosage forms may also comprise buffering agents.

[0097] Solid compositions of a similar type may also be used as fillers in soft and hard-filled gelatin capsules using such excipients as lactose or milk sugar, high molecular weight polyethylene glycols, and the like. Solid dosage forms of tablets, dragees, capsules, pills, and granules may be prepared with coatings and shells, such as enteric coatings and other coatings well known in the pharmaceutical formulation art. They may optionally contain opacifying agents, or may be of a composition that releases the active ingredient(s) only in a certain part of the intestinal tract, optionally in a delayed manner. Examples of embedding compositions that may be used include polymeric substances and waxes. Solid compositions of a similar type may also be used as fillers in soft and hard-filled gelatin capsules using such excipients as lactose or milk sugar, high molecular weight polyethylene glycols, and the like.

[0098] The therapeutic agent may also be in microencapsulated form with one or more of the excipients described above. Solid dosage forms such as tablets, dragees, capsules, pills, and granules may be prepared with coatings and shells, such as enteric coatings, release-controlling coatings, and other coatings well known in the pharmaceutical formulation art. In such solid dosage forms, the active compound may be mixed with at least one inert diluent, such as sucrose, lactose, or starch. According to common practice, such dosage forms may also contain additional substances other than inert diluents, such as tableting lubricants and other tableting aids, such as magnesium stearate and microcrystalline cellulose. In the case of capsules, tablets, and pills, the dosage forms may also contain buffering agents. They may optionally contain opacifying agents, or may be of a composition that preferably releases the active ingredient(s) only in a certain part of the intestinal tract, optionally in a delayed manner. Examples of embedding compositions that may be used include polymeric substances and waxes.

[0099] Dosage forms for topical or transdermal administration of the compounds of the present disclosure include ointments, pastes, creams, lotions, gels, powders, solutions, sprays, inhalants, or patches. The active ingredient is mixed under sterile conditions with a pharmaceutically acceptable carrier and any necessary preservatives or buffers, as needed. Ophthalmic formulations, ear drops, and eye drops are also contemplated within the scope of the present disclosure. Furthermore, the present disclosure contemplates the use of transdermal patches, which have the added advantage of providing controlled delivery of the compound to the body. Such dosage forms can be made by dissolving or dispensing the compound in an appropriate medium. Absorption enhancers can also be used to increase the flux of the compound across the skin. The rate can be controlled by either providing a rate-controlling membrane or by dispersing the compound in a polymer matrix or gel.

[0100] Compounds of the present disclosure. Described herein are compounds that can be metabolically converted into N,N-dimethyltryptamine or its analogs when administered to a subject. In certain embodiments, the compounds described herein are useful in treating any brain disease-related condition.

[0101] In some embodiments, the compounds described herein are prodrugs of dimethyltryptamine (DMT) or 5-MeO-DMT. In some embodiments, the compounds described herein are hallucinogens with improved pharmacokinetic properties (e.g., longer half-life, longer tmax, and / or longer trlast) compared to DMT or 5-MeO-DMT.

[0102] In one aspect, the disclosure provides a compound of formula (I), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 2 is -C(O)OR 3 , -C(O)R 4 , -CH(R 5 ) OR 6 , -C(O)OCH(R 5 )OC(O)R 6 , -C(O)OCH(R 5 )OC(O)OR 6 , -CH(R 5 )C(O)R 6 , -CH(R 5 )OC(O)R 6 , -CH(R 5 )OC(O)OR 6 , -S(O)2OR 7 , -P(O)OR 8 [N(R 9 )R 10 ], -P(O)[N(R 9 )R 10 ][N(R 11 )R 12], -C(O)N(R 9 )R 10 , -P(O)OR 11 (OR 12 ), -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 ], or -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 is independently hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A is substituted with R 9 and R 10 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more A or substituted with R 9 and R 10 together with the atoms to which they are attached are unsubstituted or contain one or more R A forming a heterocyclylalkyl ring substituted with R 11 and R 12 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A or substituted with R 11 and R12 together with the atoms to which they are attached are unsubstituted or contain one or more R A forming a heterocyclylalkyl ring substituted with Each R A are independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, an amino acid side chain, -OR 13 , -N(R 18 )R 19 , -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , -OP(O)OR 17 [N(R 18 )R 19 ], -C(O)N(R 18 )R 19 , -OC(O)N(R 18 )R 19 , or -OP(O)OR 20 (OR 21 ), wherein each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, amino acid side chain, aryl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 13 , R 14 , R 15 , R 16 , or R 17is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R B is replaced by R 18 and R 19 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R B or substituted with R 18 and R 19 together with the atoms to which they are attached are unsubstituted or contain one or more R B forming a heterocyclylalkyl ring substituted with R 20 and R 21 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R B or substituted with R 20 and R 21 together with the atoms to which they are attached are unsubstituted or contain one or more R B forming a heterocyclylalkyl ring substituted with Each R Bis independently halogen, amino, cyano, hydroxyl, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, arylalkyl, —C(O)CH3, —C(O)Ph, or heteroarylalkyl, and each cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl.

[0103] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is R 2 is -C(O)OR 3 , -C(O)R 4 , -CH(R 5 ) OR 6 , -C(O)OCH(R 5 )OC(O)R 6 , -C(O)OCH(R 5 )OC(O)OR 6 , -CH(R 5 )C(O)R 6 , -S(O)2OR 7 , -P(O)OR 8 [N(R 9 )R 10 ], --C(O)N(R 9 )R 10 , -P(O)OR 11 (OR 12 ), -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 ], or -CH(R 5 )OP(O)OR 11 (OR 12 )

[0104] In some embodiments, a compound of formula (I), or a pharmaceutically acceptable salt thereof: R 3 , R 4 , R 6 , R 7 , and R 8each is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl; Each R 5 are independently hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl; Each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0105] In some embodiments, a compound of Formula (I), or a pharmaceutically acceptable salt thereof, wherein R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A is replaced by .

[0106] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR3 and R 3 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is ethyl.

[0107] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is -N(R 13 )C(O)OR 14 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 13 is hydrogen or alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 14 is alkyl, aryl, or heteroaryl.

[0108] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is heteroalkyl substituted with alkyl.

[0109] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is N(R 18 )R 19 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 18 and R 19 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 18 and R 19 and together with the atom to which they are attached form a heterocyclylalkyl ring. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 18 and R 19 and together with the atom to which they are attached form a heterocyclylalkyl ring. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 18 and R 19together with the atoms to which they are attached form an unsubstituted heterocyclylalkyl ring.

[0110] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is C(O)R 14 is alkyl substituted with R 14 is one or more R B In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is C(O)R 14 is alkyl substituted with R 14 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is C(O)R 14 is alkyl substituted with R 14 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is C(O)R 14 is alkyl substituted with R 14 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)OR 3 and R 3 is C(O)R 14 is alkyl substituted with R14 is an unsubstituted heterocyclylalkyl.

[0111] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)R 4 and R 4 is heterocyclylalkyl.

[0112] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -C(O)N(R 9 )R 10 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 4 and R 5 taken together with the atoms to which they are attached may be unsubstituted or may contain one or more R A In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 4 and R 5 together with the atoms to which they are attached form one or more R A The heterocyclylalkyl ring is formed by substituted with

[0113] In some embodiments, the compound of Formula (I) has the structure of Formula (Ia), or a pharmaceutically acceptable salt thereof. [ka] In the formula, R 1 is methoxy or hydrogen, and R 3 is alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl, each of which is independently unsubstituted or substituted with one or more R A In some embodiments, the compound of formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 is unsubstituted alkyl or unsubstituted heteroalkyl. In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is methoxy and R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is methoxy and R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen and R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen and R 3 is an unsubstituted alkyl.

[0114] In some embodiments, a compound of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, isobutyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 is methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl. In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound of formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen and R 3 In some embodiments, the compound of formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is methoxy and R 3 In some embodiments, the compound of formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 In some embodiments, the compound is of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 3 teeth, [ka] In some embodiments, the compound is of formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is methoxy and R 3 teeth, [ka] In some embodiments, the compound is of formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen and R 3 teeth, [ka] is.

[0115] In some embodiments, a compound of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0116] In some embodiments, a compound of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0117] In some embodiments, a compound of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0118] In some embodiments, a compound of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0119] In some embodiments, a compound of Formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen, R 3 In some embodiments, the compound is of formula (I) or (Ia), or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen and R 3 is alkyl, R 3 is attached to the atom to which it is bonded via a primary or secondary carbon.

[0120] In some embodiments, the compound of Formula (I) has the structure of Formula (Ib), or a pharmaceutically acceptable salt thereof. [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A2 , R A3 , and R A4 each independently represents hydrogen, or independently represents one or more of an alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is alkyl substituted with

[0121] RA5 is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , or -OC(O)OR 16 wherein each heteroalkyl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 In some embodiments, the compound of formula (Ib), or a pharmaceutically acceptable salt thereof, is substituted with R A1 , R A2 , R A3 , and R A4 One of the R is alkyl and the other is not alkyl. A1 , R A2 , R A3 , and R A4 In some embodiments, the compound is of formula (Ib), or a pharmaceutically acceptable salt thereof, wherein R A1 , R A2 , R A3 , and R A4 Two of the R are alkyl and two are not alkyl. A1 , R A2 , R A3 , and R A4 and each of R is hydrogen. In some embodiments, the compound of formula (Ib), or a pharmaceutically acceptable salt thereof, A1 , R A2 , R A3 , and R A4In some embodiments, the compound is of formula (Ib), or a pharmaceutically acceptable salt thereof, wherein R A1 , R A2 , R A3 , and R A4 One of the R is alkyl and the other is not alkyl. A1 , R A2 , R A3 , and R A4 is hydrogen and alkyl is methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Ib), or a pharmaceutically acceptable salt thereof, wherein R A1 , R A2 , R A3 , and R A4 Two of the R are alkyl and two are not alkyl. A1 , R A2 , R A3 , and R A4 is hydrogen and each alkyl is independently methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of Formula (Ib), or a pharmaceutically acceptable salt thereof, wherein R A5 In some embodiments, the compound is of formula (Ib), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 In some embodiments, the compound is of formula (Ib), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 In some embodiments, the compound is of formula (Ib), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 is methyl, ethyl, isopropyl, n-propyl, tert-butyl, isobutyl, or n-butyl. In some embodiments, the compound is of formula (Ib), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15and R 15 is isobutyl.

[0122] In some embodiments, a compound of Formula (I) having the structure of Formula (Ib-1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A2 , R A3 , R A4 , R A6 , and R A7 each independently represents hydrogen, or independently represents one or more of an alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is alkyl substituted with R A5 is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , or -OC(O)OR 16 wherein each heteroalkyl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R18 )R 19 is replaced by .

[0123] In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A1 , R A2 , R A3 , R A4 , R A6 , and R A7 One of the R is alkyl and the other is not alkyl. A1 , R A2 , R A3 , R A4 , R A6 , and R A7 In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A1 , R A2 , R A3 , R A4 , R A6 , and R A7 Two of the R are alkyl and two are not alkyl. A1 , R A2 , R A3 , R A4 , R A6 , and R A7 In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A1 , R A2 , R A3 , R A4 , R A6 , and R A7 and each of R is hydrogen. In some embodiments, the compound of formula (Ib-1), or a pharmaceutically acceptable salt thereof, A1 , R A2 , R A3 , R A4 , R A6 , and R A7 One of the R is alkyl and the other is not alkyl. A1 , R A2 , R A3 , R A4 , R A6 , and R A7is hydrogen, and alkyl is methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A3 and R A4 are each independently alkyl, and R A1 , R A2 , R A6 , and R A7 In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A1 , R A2 , R A3 , R A4 , R A6 , and R A7 Two of the R are alkyl and two are not alkyl. A1 , R A2 , R A3 , R A4 , R A6 , and R A7 is hydrogen and each alkyl is independently methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A5 In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 is methyl, ethyl, isopropyl, n-propyl, tert-butyl, isobutyl, or n-butyl. In some embodiments, the compound is of formula (Ib-1), or a pharmaceutically acceptable salt thereof, wherein RA5 is -OC(O)R 15 and R 15 is isobutyl.

[0124] In some embodiments, a compound of Formula (I) or (Ib-1), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0125] In some embodiments, a compound of Formula (I) or (Ib) has the structure of Formula (Ib1), or a pharmaceutically acceptable salt thereof. [ka]

[0126] In some embodiments, the compound is a compound of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5is methoxy, ethoxy, cyclopropyloxy, methylamino, or dimethylamino. In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 teeth, [ka] is.

[0127] In some embodiments, the compound is a compound of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 is.

[0128] In some embodiments, the compound is a compound of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 is alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl.

[0129] In some embodiments, the compound is a compound of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)OR 14 In some embodiments, the compound is of formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)OR 14 and R 13 is hydrogen or alkyl. In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)OR 14 and R 13 In some embodiments, the compound is of formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)OR 14 and R 13 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)OR 14 and R 13 is unsubstituted alkyl. In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)OR 14 and R 14 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl.

[0130] In some embodiments, the compound is a compound of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13)C(O)R 14 In some embodiments, the compound is of formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 13 is hydrogen or alkyl. In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 13 In some embodiments, the compound is of formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 13 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 13 is unsubstituted alkyl. In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 14 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 14 In some embodiments, the compound is of Formula (Ib) or (Ib1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -N(R 13 )C(O)R 14and R 14 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl.

[0131] In some embodiments, a compound of Formula (I), (Ib), or (Ib1), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0132] In some embodiments, a compound of Formula (I), (Ib), or (Ib1), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0133] In some embodiments, a compound of Formula (I), (Ib), or (Ib1), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0134] In some embodiments, a compound of Formula (I) having the structure of Formula (Ic), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 18 and R 19 is independently hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each alkyl, cycloalkyl, and heteroalkyl is independently unsubstituted or substituted with one or more R B or substituted with R 18 and R 19together with the atoms to which they are attached, are unsubstituted or contain one or more R B The heterocyclylalkyl ring is formed by substituted with

[0135] In some embodiments, a compound of Formula (I) or (Ic), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 is independently methyl, ethyl, n-propyl, isopropyl, cyclopropyl, tert-butyl, -CHCHOMe, or -CHCHSOMe. In some embodiments, a compound of Formula (I) or (Ic), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 is hydrogen and R 19 is methyl, ethyl, n-propyl, isopropyl, cyclopropyl, tert-butyl, -CH2CH2OMe, or -CH2CH2SO2Me. In some embodiments, a compound of Formula (I) or (Ic), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 Each of is methyl, ethyl, n-propyl, isopropyl, cyclopropyl, tert-butyl, —CH2CH2OMe, or —CH2CH2SO2Me.

[0136] In some embodiments, the compound is a compound of Formula (I) or (Ic), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 and together with the atom to which they are attached form a substituted or unsubstituted heterocyclylalkyl ring. In some embodiments, the compound is of Formula (I) or (Ic), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 together with the atoms to which they are attached form an azetidine ring, a pyrrolidine ring, or a piperidine ring, each of which is substituted or unsubstituted.

[0137] In some embodiments, a compound of Formula (I) or (Ic), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0138] In some embodiments, a compound of Formula (I) or (Ic), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0139] In some embodiments, a compound of Formula (I) having the structure of Formula (Id), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R 5 is hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is independently unsubstituted or substituted with one or more R A is replaced by R A6 is hydrogen, or is unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is alkyl substituted with

[0140] In some embodiments, the compound is a compound of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5In some embodiments, the compound is of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is unsubstituted alkyl. In some embodiments, the compound is of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen, methyl, ethyl, or isopropyl. In some embodiments, the compound is of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein R A6 In some embodiments, the compound is of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein R A6 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, or benzyl. In some embodiments, the compound is of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is unsubstituted alkyl, and R A6 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, or benzyl. In some embodiments, the compound is of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R A6 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, or benzyl.

[0141] In some embodiments, the compound is of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0142] In some embodiments, the compound is of formula (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0143] In some embodiments, a compound of Formula (I) having the structure of Formula (Ie), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 5 is hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is independently unsubstituted or substituted with one or more R A is replaced by .

[0144] In some embodiments, a compound of formula (I) or (Ie), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (Id), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (Ie), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (Ie), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is methyl, ethyl, or isopropyl.

[0145] In some embodiments, a compound of Formula (I) or (Ie), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0146] In some embodiments, a compound of Formula (I) having the structure of Formula (If), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 9 and R 10 is independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl, and each alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, and heterocyclylalkyl is independently unsubstituted or substituted with one or more R A or substituted with R 9 and R 10 together with the atoms to which they are attached, are unsubstituted or contain one or more R A The heterocyclylalkyl ring is formed by substituted with

[0147] In some embodiments, a compound of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 9 and R 10In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 is independently methyl, ethyl, n-propyl, isopropyl, n-butyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, tert-butyl, n-pentyl, n-heptyl, n-octyl, n-nonyl, or 3-methyl-1-butyl. In some embodiments, a compound of Formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 is independently CH2CHF2, CH2CF3, or CH2cPr. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10is independently 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 9 and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 9 and R 10 Each of is methyl.

[0148] In some embodiments, a compound of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy or hydrogen, and R 9 is hydrogen and R 10is alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 9 is hydrogen and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 9 is hydrogen and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 is unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 9 is hydrogen and R 10 is unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 9 is hydrogen and R 10 is unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 is methyl, ethyl, n-propyl, isopropyl, n-butyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, tert-butyl, n-pentyl, n-heptyl, n-octyl, n-nonyl, or 3-methyl-1-butyl. In some embodiments, a compound of Formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 is —CH2CHF2, —CH2CF3, or —CH2cPr. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl. In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 9 is hydrogen and R 10 In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 9 is hydrogen and R 10In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 teeth, [ka] In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 9 is hydrogen and R 10 teeth, [ka] In some embodiments, the compound is of formula (I) or (If), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 9 is hydrogen and R 10 teeth, [ka] is.

[0149] In some embodiments, a compound of Formula (I) or (If), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0150] In some embodiments, a compound of Formula (I) or (If) having the structure of Formula (If1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R10 is hydrogen, alkyl, heteroalkyl, cycloalkyl, or heterocyclylalkyl, and each of the alkyl, heteroalkyl, cycloalkyl, and heterocyclylalkyl is unsubstituted or contains one or more R A is replaced by X 1 and X 2 each independently represents -CH2-, -O-, -NH-, -S-, -S(O)-, -S(O)2-, or -N(Y 1 )-, and each Y 1 is independently hydrogen, cycloalkyl, heteroalkyl, or alkyl.

[0151] In some embodiments, the compound is a compound of formula (If1), or a pharmaceutically acceptable salt or solvate thereof, wherein each Y 1 is independently hydrogen, methyl, ethyl, n-propyl, isopropyl, cyclopropyl, or CH2CH2OMe. In some embodiments, the compound of formula (If1), or a pharmaceutically acceptable salt or solvate thereof, wherein X 1 is -CH2- and X 2 is -N(Y 1 In some embodiments, the compound is of formula (If1), or a pharmaceutically acceptable salt or solvate thereof, wherein X 2 is -CH2- and X 1 is -N(Y 1 In some embodiments, the compound is of formula (If1), or a pharmaceutically acceptable salt or solvate thereof, wherein X 1 is -CH2- and X 2 is -N(Y 1 )- and Y 1 is hydrogen, methyl, ethyl, n-propyl, isopropyl, cyclopropyl, or —CHCHOMe. In some embodiments, the compound of formula (If1), or a pharmaceutically acceptable salt or solvate thereof, wherein X 2 is -CH2- and X 1 is -N(Y 1 )- and Y1 is hydrogen, methyl, ethyl, n-propyl, isopropyl, cyclopropyl, or —CHCHOMe. In some embodiments, the compound is of formula (If1), or a pharmaceutically acceptable salt or solvate thereof, wherein X 1 and X 2 In some embodiments, the compound is of formula (If1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is hydrogen.

[0152] In some embodiments, a compound of Formula (I) having the structure of Formula (Ig), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A2 , R A3 , and R A4 each independently represents hydrogen, or is unsubstituted or represents one or more of alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is alkyl substituted with R 10 is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of the alkyl, heteroalkyl, and cycloalkyl is unsubstituted or contains one or more R A is replaced by R A5 is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR 13 , -N(R 13 )C(O)OR 14, -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , or -OC(O)OR 16 wherein each of the heteroalkyl, heterocyclylalkyl, and heteroaryl is unsubstituted or is selected from the group consisting of one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0153] In some embodiments, the compound is a compound of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein one R A1 , R A2 , R A3 , and R A4 is alkyl and is not alkyl R A1 , R A2 , R A3 , and R A4 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A2 , R A3 , and R A4 Two of the R are alkyl and two are not alkyl. A1 , R A2 , R A3 , and R A4 and each of R is hydrogen. In some embodiments, the compound of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, A1 , R A2 , R A3 , and R A4 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt thereof, wherein one R A1 , R A2 , RA3 , and R A4 is alkyl and is not alkyl R A1 , R A2 , R A3 , and R A4 is hydrogen and each alkyl is independently methyl, ethyl, tert-butyl, or isopropyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A2 , R A3 , and R A4 Two of the R are alkyl and two are not alkyl. A1 , R A2 , R A3 , and R A4 is hydrogen, and each alkyl is independently methyl, ethyl, tert-butyl, or isopropyl.

[0154] In some embodiments, the compound is a compound of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is unsubstituted heterocyclylalkyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is methoxy, ethoxy, cyclopropyloxy, methylamino, or dimethylamino. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 teeth, [ka] is.

[0155] In some embodiments, the compound is a compound of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is hydrogen, methyl, ethyl, n-propyl, or isopropyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is -CH2CH2OMe or -CH2CH2SO2Me.

[0156] In some embodiments, the compound is a compound of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 is alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt thereof, wherein R A5is -OC(O)R 15 and R 15 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl.

[0157] In some embodiments, the compound is a compound of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is N(R 13 )C(O)OR 14 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is N(R 13 )C(O)OR 14 and R 13 is hydrogen or alkyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is N(R 13 )C(O)OR 14 and R 13 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is N(R 13 )C(O)OR 14 and R 13 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)OR 14 and R 13 is unsubstituted alkyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)OR 14 and R 14 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl.

[0158] In some embodiments, the compound is a compound of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 13 is hydrogen or alkyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 13 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 13 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 13 is unsubstituted alkyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 14 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 14is unsubstituted alkyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 14 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 14 In some embodiments, the compound is of formula (Ig), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 and R 14 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl.

[0159] In some embodiments, a compound of Formula (I) or (Ig), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0160] In some embodiments, a compound of Formula (I) or (Ig), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0161] In some embodiments, a compound of Formula (I) or (Ig), or a pharmaceutically acceptable salt thereof, wherein the compound is: [ka]

[0162] In some embodiments, a compound of Formula (I) having the structure of Formula (Ih), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R 10 is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of the alkyl, heteroalkyl, and cycloalkyl is unsubstituted or contains one or more R A is replaced by R 18 and R 19 is independently hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each alkyl, cycloalkyl, or heterocyclylalkyl is independently unsubstituted or contains one or more R B or substituted with R 18 and R 19 together with the atoms to which they are attached, are unsubstituted or contain one or more R B The heterocyclylalkyl ring is formed by substituted with

[0163] In some embodiments, the compound is a compound of formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 In some embodiments, the compound is of formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is hydrogen, methyl, ethyl, n-propyl, or isopropyl. In some embodiments, the compound is of formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is CH2CH2OMe or CH2CH2SO2Me.

[0164] In some embodiments, a compound of formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 is independently methyl, ethyl, n-propyl, isopropyl, cyclopropyl, tert-butyl, CH2CH2OMe, or CH2CH2SO2Me. In some embodiments, the compound of Formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 is hydrogen and R 19 is methyl, ethyl, n-propyl, isopropyl, cyclopropyl, tert-butyl, CH2CH2OMe, or CH2CH2SO2Me. In some embodiments, the compound of Formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 Each of is methyl, ethyl, n-propyl, isopropyl, cyclopropyl, tert-butyl, CH2CH2OMe, or CH2CH2SO2Me.

[0165] In some embodiments, the compound is a compound of formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 together with the atom to which they are attached form a heterocyclylalkyl ring. In some embodiments, the compound is of formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 are taken together with the atoms to which they are attached to form an azetidine ring, a morpholine ring, a pyrrolidine ring, or a piperidine ring, each of which is substituted or unsubstituted. In some embodiments, the compound is of formula (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein R 18 and R 19 together with the atoms to which they are attached form an azetidine ring, a morpholine ring, a pyrrolidine ring, or a piperidine ring.

[0166] In some embodiments, a compound of Formula (I) or (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0167] In some embodiments, a compound of Formula (I) or (Ih), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0168] In some embodiments, a compound of Formula (I) having the structure of Formula (Ii), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R 5 and R 10 is independently hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each alkyl, heteroalkyl, and cycloalkyl is independently unsubstituted or substituted with one or more R A is replaced by R A6 is independently hydrogen, alkyl, heteroalkyl, or cycloalkyl, each of which is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0169] In some embodiments, the compound is a compound of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is unsubstituted alkyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is methyl, ethyl, or isopropyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen, methyl, ethyl, or isopropyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R A6 In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R A6 In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R A6 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, or benzyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R A6 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, or benzyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R A6 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, or benzyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is unsubstituted alkyl, and R A6is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, or benzyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R A6 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, or benzyl.

[0170] In some embodiments, the compound is a compound of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is hydrogen, methyl, ethyl, n-propyl, or isopropyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is CH2CH2OMe or CH2CH2SO2Me.

[0171] In some embodiments, the compound is a compound of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 , R 10 , and R A6 and each is independently hydrogen, alkyl, heteroalkyl, or cycloalkyl. In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 , R 10 , and R A6 is independently hydrogen, alkyl, or cycloalkyl. In some embodiments, the compound of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 , R 10 , and R A6In some embodiments, the compound is of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 , R 10 , and R A6 Each of is independently hydrogen, methyl, ethyl, n-propyl, or isopropyl.

[0172] In some embodiments, the compound of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, is: [ka]

[0173] In some embodiments, the compound of formula (Ii), or a pharmaceutically acceptable salt or solvate thereof, is: [ka]

[0174] In some embodiments, a compound of Formula (I) having the structure of Formula (Ij), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 5 and R 10 is hydrogen, alkyl, or heteroalkyl, and each of the alkyl and heteroalkyl is independently unsubstituted or contains one or more R A is replaced by .

[0175] In some embodiments, the compound is a compound of formula (Ij), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (Ij), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5In some embodiments, the compound is of formula (Ij), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (Ij), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is methyl, ethyl, or isopropyl.

[0176] In some embodiments, the compound is a compound of formula (Ij), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 In some embodiments, the compound is of formula (Ij), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is hydrogen, methyl, ethyl, n-propyl, or isopropyl. In some embodiments, the compound is of formula (Ij), or a pharmaceutically acceptable salt or solvate thereof, wherein R 10 is CH2CH2OMe or CH2CH2SO2Me.

[0177] In some embodiments, a compound of Formula (I) or (Ij), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0178] In some embodiments, a compound of Formula (I) having the structure of Formula (Ik), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 4 is alkyl, heterocyclylalkyl, aryl, heteroaryl, or heteroalkyl, each of which is unsubstituted or contains one or more R A is replaced by .

[0179] In some embodiments, the compound is a compound of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 4 is heterocyclylalkyl.

[0180] In some embodiments, the compound is a compound of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 is unsubstituted alkyl. In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, 3-methyl-1-butyl, n-pentyl, n-hexyl, n-heptyl, n-octyl, or n-nonyl. In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 is cyclopropyl, cyclobutyl, cyclohexyl, cycloheptyl, or cyclooctyl. In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 3-pyrimidyl, or 6-pyrimidyl.

[0181] In some embodiments, a compound of Formula (I) or (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0182] In some embodiments, the compound is of Formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0183] In some embodiments, a compound of Formula (I) or (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0184] In some embodiments, a compound of Formula (I) or (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0185] In some embodiments, the compound is a compound of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] is.

[0186] In some embodiments, the compound is of Formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0187] In some embodiments, the compound is a compound of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R 14 is alkyl, cycloalkyl, or aryl, each of which is independently unsubstituted or substituted with one or more R B In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R 14 is methyl, ethyl, n-propyl, isopropyl, or CH2CH2OMe. In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R 14 is phenyl.

[0188] In some embodiments, a compound of Formula (I) or (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0189] In some embodiments, the compound is a compound of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R A7 is hydrogen, or is unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R A7 In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R A7 is unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R A7 is unsubstituted alkyl. In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R A7 is methyl, ethyl, n-propyl, isopropyl, or n-butyl. In some embodiments, the compound is of formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 teeth, [ka] and R A7 is benzyl.

[0190] In some embodiments, the compound is of Formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0191] In some embodiments, the compound is of Formula (Ik), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0192] In some embodiments, a compound of Formula (I) or (Ik) having the structure of Formula (Ik1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A2 , R A3 , and R A4 is independently hydrogen, an alkyl, or an amino acid side chain, and each alkyl or amino acid side chain is independently unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 10 is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of the alkyl, heteroalkyl, and cycloalkyl is unsubstituted or contains one or more R A is replaced by R A5 is heteroalkyl, heterocyclylalkyl, heteroaryl, -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , or -OC(O)OR 16 wherein each of the heteroalkyl, heterocyclylalkyl, and heteroaryl is unsubstituted or is selected from the group consisting of one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0193] In some embodiments, a compound of Formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A2 , R A3 , and R A4 and each of R is hydrogen. In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A2 , R A3 , and R A4 is hydrogen or alkyl. In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A2 , R A3 , and R A4 In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is heteroalkyl or heterocyclylalkyl. In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 In some embodiments, the compound of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A2 , R A3 , and R A4 is hydrogen, and R A5 In some embodiments, the compound of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , RA2 , R A3 , and R A4 is hydrogen, and R A5 In some embodiments, the compound of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A2 , R A3 , and R A4 is hydrogen, and R A5 In some embodiments, the compound of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A2 , R A3 , and R A4 is hydrogen, and R A5 is methylsulfonyl.

[0194] In some embodiments, the compound is a compound of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 is alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl. In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 is unsubstituted alkyl. In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R15 and R 15 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 is unsubstituted aryl. In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -OC(O)R 15 and R 15 In some embodiments, the compound is of formula (Ik1), or a pharmaceutically acceptable salt thereof, wherein R A5 is -OC(O)R 15 and R 15 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl.

[0195] In some embodiments, a compound of Formula (I) or (Ik) having the structure of Formula (Ik2), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 13 is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, or heterocyclylalkyl, and each of the alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, and heterocyclylalkyl is unsubstituted or contains one or more R Bis replaced by p is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

[0196] In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl. In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is hydrogen or alkyl. In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt thereof, wherein R 13 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, n-pentyl, or 3-methyl-1-butyl. In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is hydrogen or methyl. In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is unsubstituted aryl. In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl. In some embodiments, a compound of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein p is 1, 2, 3, 4, or 5. In some embodiments, a compound of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein p is 1. In some embodiments, a compound of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein p is 2. In some embodiments, a compound of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein p is 3. In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein p is 4. In some embodiments, the compound is of Formula (I), (Ik), or (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein p is 5.

[0197] In some embodiments, the compound is of Formula (Ik1), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0198] In some embodiments, the compound is of Formula (Ik2), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0199] In some embodiments, a compound of Formula (I) or (Ik) having the structure of Formula (Ik3), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 is an alkyl or amino acid side chain, each of which is unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R A5 is -N(R 18 )R 19 or -N(R 13 )C(O)R 14 is.

[0200] In some embodiments, the compound is a compound of formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 18 )R 19 In some embodiments, the compound is of formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 is -N(R 18 )R 19 and R 18 and R 19 In some embodiments, the compound is of formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 18 )R 19 and R 19 is alkyl, cycloalkyl, or aryl. In some embodiments, the compound is of formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 18 )R 19 and R 18 is hydrogen and R 19 is alkyl, cycloalkyl, or aryl. In some embodiments, the compound is of formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 18 )R 19 and R 18 is hydrogen and R 19 is unsubstituted alkyl, unsubstituted cycloalkyl, or unsubstituted aryl. In some embodiments, the compound is of formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 18 )R 19 and R 18 is hydrogen and R 19 is methyl, ethyl, isopropyl, tert-butyl, or phenyl.

[0201] In some embodiments, the compound is a compound of formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein R A5 is -N(R 13 )C(O)R 14 is.

[0202] In some embodiments, the compound is of Formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka] In some embodiments, the compound is of Formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0203] In some embodiments, the compound is of Formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka] In some embodiments, the compound is of Formula (Ik3), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0204] In some embodiments, a compound of Formula (I) having the structure of Formula (II), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5is hydrogen, alkyl, or cycloalkyl, each of which is unsubstituted or has one or more R A is replaced by R 6 is alkyl, cycloalkyl, heterocyclylalkyl, or heteroalkyl, each of which is unsubstituted or substituted with one or more R A is replaced by .

[0205] In some embodiments, the compound is a compound of formula (I) or (II), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is methyl, ethyl, isopropyl, tert-butyl, 2-dimethylaminoethyl, or cyclopropyl. In some embodiments, the compound of Formula (I) or (II), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 5 is hydrogen and R 6 is methyl, ethyl, isopropyl, tert-butyl, 2-dimethylaminoethyl, or cyclopropyl. In some embodiments, the compound of Formula (I) or (II), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 5 is hydrogen and R 6 is methyl, ethyl, isopropyl, tert-butyl, 2-dimethylaminoethyl, or cyclopropyl. In some embodiments, the compound is of formula (I) or (II), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 5 is hydrogen and R 6 In some embodiments, the compound of formula (I) or (II), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5In some embodiments, the compound is of formula (I) or (II), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 5 is hydrogen and R 6 is tert-butyl.

[0206] In some embodiments, a compound of Formula (I) or (II), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0207] In some embodiments, a compound of Formula (I) having the structure of Formula (Im), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each of the alkyl, cycloalkyl, and heteroalkyl is unsubstituted or contains one or more R A is replaced by R 11 and R 12 is independently hydrogen, cycloalkyl, aryl, heteroaryl, or alkyl, and each of the alkyl, cycloalkyl, and heteroalkyl is independently unsubstituted or substituted with one or more R A is replaced by .

[0208] In some embodiments, the compound is a compound of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 is hydrogen and R 12 is cycloalkyl, aryl, heteroaryl, or alkyl. In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 is hydrogen and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 is hydrogen and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen or alkyl. In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen, unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted heteroalkyl, or alkyl substituted with heteroaryl. In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 is hydrogen and R 12 is cycloalkyl, aryl, heteroaryl, or alkyl. In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11is hydrogen and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the is -OC(O)R 15 In some embodiments, the compound of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the is -OC(O)R 15 and each R 15 is alkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the is -OC(O)R 15 and each R 15 is an unsubstituted alkyl, an unsubstituted cycloalkyl, an unsubstituted heterocyclylalkyl, an unsubstituted aryl, or an unsubstituted heteroaryl. In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the is -OC(O)R 15 and each R 15 is heterocyclylalkyl substituted with alkyl or arylalkyl.

[0209] In some embodiments, the compound is a compound of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 4 is hydrogen and R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 5 is hydrogen and R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 5 is hydrogen and R 11 and R12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 5 is hydrogen and R 11 and R 12 Each of is tert-butyl.

[0210] In some embodiments, the compound is a compound of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the [ka] In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl. In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of formula (I) or (Im), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of is benzyl.

[0211] In some embodiments, a compound of Formula (I) or (Im) having the structure of Formula (Im1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A3 , and R 6 each is independently hydrogen, alkyl, or cycloalkyl; R A2 and R A4 each independently is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, —OC(O)R 15 , or -OC(O)OR 16 and Each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19is replaced by .

[0212] In some embodiments, the compound is a compound of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 and R A3 Each of is hydrogen.

[0213] In some embodiments, a compound of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 4 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein each R 15 is alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 is alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, 3-methyl-1-butyl, cyclopropyl, or cyclobutyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5 is hydrogen, and each R 15 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, 3-methyl-1-butyl, cyclopropyl, or cyclobutyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5 is hydrogen, and each R 15 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5 is hydrogen, and each R 15 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 , R A3 , and R 5 is hydrogen, and each R 15is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl.

[0214] In some embodiments, a compound of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 is alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, 3-methyl-1-butyl, cyclopropyl, or cyclobutyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is hydrogen, and each R 16 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, 3-methyl-1-butyl, cyclopropyl, or cyclobutyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is hydrogen, and each R 16 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 is phenyl or 4-nitrophenyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein each R A2 and R A4 is -OC(O)OR 16 and R A1 , R A3 , and R 5 is hydrogen, and each R 16In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is hydrogen, and each R 16 In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and each R A1 , R A3 , and R 5 is hydrogen, and each R 16 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl.

[0215] In some embodiments, a compound of Formula (I), (Im), or (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0216] In some embodiments, a compound of Formula (I), (Im), or (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0217] In some embodiments, a compound of Formula (I), (Im), or (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0218] In some embodiments, a compound of Formula (I), (Im), or (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0219] In some embodiments, a compound of Formula (I), (Im), or (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0220] In some embodiments, a compound of Formula (I), (Im), or (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0221] In some embodiments, a compound of Formula (I), (Im), or (Im1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0222] In some embodiments, a compound of Formula (I), (Im), or (Im1) having the structure of Formula (Im1a), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 , R A3 , and R 5 is independently hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is independently unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R B1 and R B2Each of is independently hydrogen or alkyl that is unsubstituted or substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl.

[0223] In some embodiments, the compound is a compound of formula (Im1a), or a pharmaceutically acceptable salt or solvate thereof, wherein R B1 and R B2 is independently hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, pentan-3-yl, or benzyl. In some embodiments, the compound is of formula (Im1a), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Im1a), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A3 , and R 5 In some embodiments, the compound is of formula (Im1a), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 , R A3 , and R 5 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl; B1 and R B2 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, pentan-3-yl, or benzyl.

[0224] In some embodiments, a compound of Formula (I), (Im), (Im1), or (Im1a), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0225] In some embodiments, a compound of Formula (I), (Im), (Im1), or (Im1a), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0226] In some embodiments, a compound of Formula (I) having the structure of Formula (In), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl; R 8 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl; R 9 and R 10 each is independently hydrogen or alkyl; Each cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0227] In some embodiments, the compound is a compound of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5is hydrogen or unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen, methyl, ethyl, or tert-butyl. In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl. In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is unsubstituted alkyl or unsubstituted cycloalkyl. In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. In some embodiments, the compound is of Formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 In some embodiments, the compound is of formula (I) or (In), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 is alkyl.

[0228] In some embodiments, a compound of Formula (I) or (In) having the structure of Formula (In1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 is hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is unsubstituted or is selected from alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 5 and R 8 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and the alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl are independently unsubstituted or substituted with one or more R A is replaced by R13 is hydrogen, or unsubstituted, or contains one or more R B is alkyl substituted with

[0229] In some embodiments, the compound is a compound of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 and R A1 In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 and R A1 In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 and R A1 In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 and R A1 In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is unsubstituted alkyl or unsubstituted cycloalkyl. In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is unsubstituted alkyl. In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or —CHCH(Et) . In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 and R A1 is hydrogen or alkyl, and R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or —CHCH(Et) . In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 and R A1 is hydrogen or unsubstituted alkyl, and R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or —CHCH(Et) . In some embodiments, the compound is of formula (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 and RA1 is hydrogen and R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or —CHCH(Et)

[0230] In some embodiments, a compound of Formula (I), (In), or (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0231] In some embodiments, a compound of Formula (I), (In), or (In1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0232] In some embodiments, a compound of Formula (I) having the structure of Formula (Io), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 11 and R 12 is independently selected from hydrogen, cycloalkyl, aryl, heteroaryl, or alkyl, and each cycloalkyl, aryl, heteroaryl, and alkyl is independently unsubstituted or contains one or more R A or substituted with R 11 and R 12 together with the atoms to which they are attached, are unsubstituted or contain one or more R A The heterocyclylalkyl ring is formed by substituted with

[0233] In some embodiments, a compound of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 is independently selected from cycloalkyl, aryl, heteroaryl, or alkyl, or R 11 and R 12 and together with the atom to which they are attached form a heterocyclylalkyl ring. In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 is hydrogen and R 12 is alkyl, cycloalkyl, aryl, heteroaryl, or alkyl. In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the is -OC(O)R 15In some embodiments, the compound of formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the is -OC(O)R 15 and each R 15 is alkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl. In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the is -OC(O)R 15 and each R 15 is an unsubstituted alkyl, an unsubstituted cycloalkyl, an unsubstituted heterocyclylalkyl, an unsubstituted aryl, or an unsubstituted heteroaryl. In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the is -OC(O)R 15 and each R 15 is heterocyclylalkyl substituted with alkyl or arylalkyl.

[0234] In some embodiments, a compound of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 11 and R 12 Each of is tert-butyl.

[0235] In some embodiments, a compound of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of the [ka] In some embodiments, the compound is of formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl. In some embodiments, the compound is of Formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 In some embodiments, the compound is of formula (I) or (Io), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12 Each of is benzyl.

[0236] In some embodiments, a compound of Formula (I) or (Io) having the structure of Formula (Io1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 and R A3 each is independently hydrogen, alkyl, or cycloalkyl; R A2 and R A4 each independently represents an alkyl, heteroalkyl, or cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, -OC(O)R 15 , or -OC(O)OR 16 and Each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0237] In some embodiments, a compound of Formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 and R A3 Each of is hydrogen.

[0238] In some embodiments, a compound of Formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 is alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, 3-methyl-1-butyl, cyclopropyl, or cyclobutyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3 is hydrogen, and each R 15 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, 3-methyl-1-butyl, cyclopropyl, or cyclobutyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and RA3 is hydrogen, and each R 15 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3 is hydrogen, and each R 15 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 15 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)R 15 and R A1 and R A3 is hydrogen, and each R 15 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl.

[0239] In some embodiments, a compound of Formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 is alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, 3-methyl-1-butyl, cyclopropyl, or cyclobutyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 and R A3 is hydrogen, and each R 16is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, 3-methyl-1-butyl, cyclopropyl, or cyclobutyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein each R A2 and R A4 is -OC(O)OR 16 and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 is phenyl or 4-nitrophenyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein each R A2 and R A4 is -OC(O)OR 16 and R A1 and R A3 is hydrogen, and each R 16 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and each R A1 and R A3 are independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 and R A3 is hydrogen, and each R 16 In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16and R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl, and each R 16 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A2 and R A4 Each of the is -OC(O)OR 16 and R A1 and R A3 is hydrogen, and each R 16 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl.

[0240] In some embodiments, a compound of Formula (I), (Io), or (Io1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0241] In some embodiments, the compound is of Formula (I), (Io), or (Io1), or a pharmaceutically acceptable salt or solvate thereof. [ka]

[0242] In some embodiments, a compound of Formula (I) or (Io) having the structure of Formula (Io2), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is methoxy or hydrogen, and R A1is aryl or heteroaryl, each of which is unsubstituted or contains one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by .

[0243] In some embodiments, the compound is a compound of formula (Io2), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 In some embodiments, the compound is of formula (Io2), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 is aryl substituted with halogen. In some embodiments, the compound is of formula (Io2), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 teeth, [ka] and Z 1 , Z 2 , and Z 3 is independently hydrogen or halogen. In some embodiments, the compound is of formula (Io2), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 teeth, [ka] and Z 1 , Z 2 , and Z 3 is independently hydrogen, fluoro, chloro, bromo, or iodo. In some embodiments, the compound is of formula (Io2), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 teeth, [ka] is.

[0244] In some embodiments, the compound is of Formula (Io2), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0245] In some embodiments, the compound is of Formula (Io2), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0246] In some embodiments, a compound of Formula (I), (Io), or (Io1) having the structure of Formula (Io1a), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R A1 and R A3 is independently hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is independently unsubstituted or is one or more of alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R B1 and R B2Each of is independently hydrogen or alkyl that is unsubstituted or substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl.

[0247] In some embodiments, the compound is a compound of Formula (Io1a), or a pharmaceutically acceptable salt or solvate thereof, wherein R B1 and R B2 is independently hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, pentan-3-yl, or benzyl. In some embodiments, the compound of Formula (Io1a), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of Formula (Io1a), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 and R A3 and each is independently hydrogen. In some embodiments, the compound is of formula (Io1a), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 and R A3 is independently hydrogen, methyl, ethyl, isopropyl, or tert-butyl; B1 and R B2 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, pentan-3-yl, or benzyl.

[0248] In some embodiments, the compound is of Formula (Io1a), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0249] In some embodiments, the compound is of Formula (Io1a), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0250] In some embodiments, a compound of Formula (I) having the structure of Formula (Ip), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 8 is alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl; R 9 and R 10 each is independently hydrogen or alkyl; Each alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0251] In some embodiments, the compound is a compound of Formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is unsubstituted alkyl or unsubstituted cycloalkyl. In some embodiments, the compound is of formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. In some embodiments, the compound is of Formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 In some embodiments, the compound is of formula (I) or (Ip), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 is hydrogen and R 10 is alkyl.

[0252] In some embodiments, a compound of Formula (I) or (Ip) having the structure of Formula (Ip1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, RA1 is hydrogen, alkyl, or cycloalkyl, each of which is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 8 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and each alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is unsubstituted or substituted with one or more R A is replaced by R 13 is hydrogen, or unsubstituted, or contains one or more R B is alkyl substituted with

[0253] In some embodiments, the compound is a compound of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 is hydrogen or alkyl. In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 is hydrogen or unsubstituted alkyl. In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 is hydrogen, methyl, ethyl, or tert-butyl. In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8is alkyl or cycloalkyl. In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is unsubstituted alkyl or unsubstituted cycloalkyl. In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 8 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is unsubstituted alkyl. In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or —CHCH(Et) . In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1is hydrogen or unsubstituted alkyl, and R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or —CHCH(Et) . In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 is hydrogen and R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or —CHCH(Et)

[0254] In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0255] In some embodiments, the compound is of formula (Ip1), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0256] In some embodiments, a compound of Formula (I) having the structure of Formula (Iq), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl; R 6 is alkyl, cycloalkyl, heteroalkyl, heterocyclylalkyl, aryl, or heteroaryl; Each alkyl, cycloalkyl, heteroaryl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0257] In some embodiments, the compound is a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen or alkyl. In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen or unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is alkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6is an unsubstituted alkyl, an unsubstituted cycloalkyl, an unsubstituted heterocyclylalkyl, an unsubstituted aryl, or an unsubstituted heteroaryl. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is methyl, isopropyl, tert-butyl, or —CH(Et)2.

[0258] In some embodiments, the compound is a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is alkyl, and R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 6 is unsubstituted alkyl. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is unsubstituted alkyl, and R 6 is unsubstituted alkyl. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R6 is methyl, ethyl, isopropyl, tert-butyl, or cyclopropyl. In some embodiments, the compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 6 is methyl, ethyl, isopropyl, tert-butyl, or cyclopropyl. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 5 is hydrogen and R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 5 is hydrogen and R 6 is tert-butyl.

[0259] In some embodiments, the compound is a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is unsubstituted alkyl. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6is methyl, ethyl, n-propyl, tert-butyl, 3-methyl-1-butyl, n-pentyl, n-hexyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl.

[0260] In some embodiments, the compound is a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is CH2CH2OMe or CH2CH2SO2Me. In some embodiments, a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is -(CH2) r COH, where r is 1, 2, 3, 4, 5, or 6. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6is -(CH2) s CO2R 13 and s is 1, 2, 3, 4, 5, or 6. In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is -(CH2) s CO2R 13 and R 13 In some embodiments, the compound is of formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is -(CH2) s CO2R 13 and R 13 is unsubstituted alkyl. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is -(CH2) s CO2R 13 and R 13 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or —CH(Et) 2 .

[0261] In some embodiments, the compound is a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is -CH(R A1 )NH2 and R A1 is hydrogen, alkyl, heteroalkyl, or an amino acid side chain. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is -CH(R A1 )NH2 and R A1 is an amino acid side chain. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is -CH(R A1 )NH2 and R A1is methyl, ethyl, n-propyl, isopropyl, tert-butyl, CH(Me)Et, CHCH(Me) or CHCHSMe. In some embodiments, the compound is of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is -CH(R A1 )NH2 and R A1 is benzyl.

[0262] In some embodiments, a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0263] In some embodiments, a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0264] In some embodiments, a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0265] In some embodiments, a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0266] In some embodiments, a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0267] In some embodiments, a compound of Formula (I) or (Iq), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0268] In some embodiments, a compound of Formula (I) or (Iq) having the structure of Formula (Iq1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is unsubstituted or has one or more R A is replaced by Q 1 teeth, [ka] and Y 1 , Y 2 , or Y 3 each independently represents -O-, -S-, -S(O)-, -S(O)2-, -N(R Y1 )-, or -NC(O)R Y2 and R Y1 and R Y2 Each of is independently hydrogen, alkyl, heteroalkyl, or heteroaryl.

[0269] In some embodiments, a compound of Formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 In some embodiments, the compound of formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, is 1 , Y 2 , or Y 3 Each of -N(R Y1 )- and R Y1 In some embodiments, the compound is of formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 is independently methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, CH(Et)2, CH2CH2OMe, CH2CH2SO2Me, or CH2CF3. In some embodiments, the compound of Formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 and each is phenyl. In some embodiments, the compound of formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 and each is benzyl. In some embodiments, the compound of formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 is independently 2-pyridyl, 3-pyridyl, or 4-pyridyl.

[0270] In some embodiments, a compound of Formula (Iq) or (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0271] In some embodiments, a compound of Formula (Iq) or (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0272] In some embodiments, a compound of Formula (Iq) or (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0273] In some embodiments, a compound of Formula (Iq) or (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0274] In some embodiments, a compound of Formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2, or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 each of which independently [ka] and R Z1 is hydrogen or alkyl. In some embodiments, the compound is of formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 each of which independently [ka] and R Z1 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or CH(Et)2. In some embodiments, the compound of Formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 each of which independently [ka] and R Z1 is benzyl.

[0275] In some embodiments, the compound is of Formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0276] In some embodiments, the compound is of Formula (Iq1), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0277] In some embodiments, a compound of Formula (I) having the structure of Formula (Ir), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl; R 6 is alkyl, cycloalkyl, heteroalkyl, heterocyclylalkyl, aryl, or heteroaryl; Each alkyl, cycloalkyl, heteroaryl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A is replaced by .

[0278] In some embodiments, the compound is a compound of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen or alkyl. In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen or unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is alkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is an unsubstituted alkyl, an unsubstituted cycloalkyl, an unsubstituted heterocyclylalkyl, an unsubstituted aryl, or an unsubstituted heteroaryl. In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5is methyl, ethyl, isopropyl, tert-butyl, or —CH(Et)2.

[0279] In some embodiments, the compound is a compound of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is alkyl, and R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen and R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is unsubstituted alkyl, and R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is unsubstituted alkyl, and R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is methyl, ethyl, n-propyl, isopropyl, tert-butyl, 3-methyl-1-butyl, n-pentyl, n-hexyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. In some embodiments, the compound is of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 In some embodiments, the compound is of formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein R 6 teeth, [ka] is.

[0280] In some embodiments, a compound of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0281] In some embodiments, a compound of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0282] In some embodiments, a compound of Formula (I) or (Ir) having the structure of Formula (Ir1), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is methoxy or hydrogen, R 5 is hydrogen, alkyl, or cycloalkyl, and each of the alkyl and cycloalkyl is unsubstituted or has one or more R A is replaced by Q 1 teeth, [ka] and Y 1 , Y 2 , or Y 3 each independently represents -O-, -S-, -S(O)-, -S(O)2-, -N(R Y1 )-, or -NC(O)R Y2 and R Y1 and R Y2 Each of is independently hydrogen, alkyl, heteroalkyl, or heteroaryl.

[0283] In some embodiments, the compound of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, is 1 , Y 2 , or Y 3 Each of -N(R Y1 In some embodiments, the compound of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, is 1 , Y 2 , or Y 3 Each of -N(R Y1 )- and R Y1In some embodiments, the compound is of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 is independently methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, CH(Et)2, CH2CH2OMe, CH2CH2SO2Me, or CH2CF3. In some embodiments, the compound of Formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 and each is phenyl. In some embodiments, the compound of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 and each is benzyl. In some embodiments, the compound is of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 is independently 2-pyridyl, 3-pyridyl, or 4-pyridyl.

[0284] In some embodiments, a compound of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0285] In some embodiments, a compound of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0286] In some embodiments, a compound of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0287] In some embodiments, a compound of Formula (I) or (Ir), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0288] In some embodiments, the compound of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, is 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 each of which independently [ka] and R Z1is hydrogen or alkyl. In some embodiments, the compound is of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 each of which independently [ka] and R Z1 is methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, or CH(Et)2. In some embodiments, the compound of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, wherein Y 1 , Y 2 , or Y 3 Each of -N(R Y1 )-or-NC(O)R Y2 and R Y1 and R Y2 each of which independently [ka] is.

[0289] In some embodiments, the compound is of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0290] In some embodiments, the compound is of formula (Ir1), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0291] In some embodiments, a compound of Formula (I) having the structure of Formula (Is), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 15 is alkyl, heteroalkyl, cycloalkyl, aryl, or heteroaryl, each of which is unsubstituted or contains one or more R B is replaced by .

[0292] In some embodiments, the compound is a compound of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 In some embodiments, the compound of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 is unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 is methyl, ethyl, n-propyl, isopropyl, n-butyl, or tert-butyl. In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 In some embodiments, the compound of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15is —CH[CH(Me)2]NH2. In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 is -(CH2) q COH, where q is 1, 2, 3, 4, 5, or 6. In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl. In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 is methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 15 In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is hydrogen and R 15 In some embodiments, the compound is of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is methoxy and R 15 is methyl.

[0293] In some embodiments, a compound of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0294] In some embodiments, a compound of formula (I) or (Is), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0295] In some embodiments, a compound of Formula (I) having the structure of Formula (It), or a pharmaceutically acceptable salt thereof: [ka] In the formula, R 1 is hydrogen or methoxy, and R 13 is alkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, each of which is unsubstituted or contains one or more R B is replaced by .

[0296] In some embodiments, a compound of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is methyl, ethyl, isopropyl, tert-butyl, n-butyl, n-pentyl, n-hexyl, n-heptyl, or n-octyl. In some embodiments, the compound is of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is -CH2CH2OMe, CH2CH2SO2Me, or CH2CH2NMe2. In some embodiments, a compound of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is (CH2) u COH, and u is 1, 2, 3, 4, 5, or 6. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, or 6-pyrimidyl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 In some embodiments, the compound is of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13is oxetan-3-yl or azetidin-3-yl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] is.

[0297] In some embodiments, a compound of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] and R B1 is hydrogen or alkyl, and Z 1 is -O-, -S-, -S(O)-, -S(O)2-, or -N(R C1 )- and R C1 is hydrogen, alkyl, acetyl, or benzoyl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] and R C1 In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] and R C1 is methyl, acetyl, or benzoyl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] is.

[0298] In some embodiments, a compound of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] and Y 1 , Y 2 , or Y 3 each independently represents -O-, -S-, -S(O)-, -S(O)2-, or -N(R B2 )- and each R B2 is independently hydrogen, alkyl, acetyl, or benzoyl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] and R B2 In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] and R B2 is unsubstituted alkyl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] and each R B2is independently methyl, acetyl, or benzoyl. In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 teeth, [ka] is.

[0299] In some embodiments, a compound of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is -CH2CH2R B3 and R B3 In some embodiments, the compound is of formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is -CH2CH2R B3 and R B3 In some embodiments, the compound is of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13 is -CH2CH2R B3 and R B3 teeth, [ka] is.

[0300] In some embodiments, a compound of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0301] In some embodiments, a compound of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0302] In some embodiments, a compound of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0303] In some embodiments, a compound of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0304] In some embodiments, a compound of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0305] In some embodiments, a compound of Formula (I) or (It), or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: [ka]

[0306] In some embodiments, a compound of Formula (I) having the structure of Formula (Iu), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R A1 is hydrogen, alkyl, or cycloalkyl, each of which is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R 20 and R 21 is independently hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and each of the alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or contains one or more R B or substituted with R 20 and R 21 together with the atoms to which they are attached, are unsubstituted or contain one or more R B The heterocyclylalkyl ring is formed by substituted with

[0307] In some embodiments, the compound is a compound of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 is methyl, ethyl, isopropyl, or tert-butyl. In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R A1 is methyl, ethyl, isopropyl, —CH(Et)2, or tert-butyl.

[0308] In some embodiments, the compound is a compound of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 and each is independently unsubstituted alkyl. In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt thereof, wherein R 20 and R 21 is independently methyl, ethyl, n-propyl, isopropyl, tert-butyl, 3-methyl-1-butyl, n-pentyl, or n-hexyl. In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 each of which independently [ka] In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R20 and R 21 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 and each of R is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl. In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 is independently 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, or 4-pyrimidyl. In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 is hydrogen and R 21 is alkyl, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen and is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl.

[0309] In some embodiments, the compound is a compound of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 and each independently is alkyl or cycloalkyl. In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 is independently unsubstituted alkyl, and R A1In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 is independently unsubstituted alkyl, and R 1 In some embodiments, the compound of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 is tert-butyl, and R A1 is hydrogen and R 1 In some embodiments, the compound of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein R 20 and R 21 is tert-butyl, and R A1 is hydrogen and R 1 is hydrogen.

[0310] In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0311] In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0312] In some embodiments, a compound of Formula (I) having the structure of Formula (IV), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R 9 and R 10 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A or substituted with R 9 and R 10 together with the atoms to which they are attached, are unsubstituted or contain one or more R A forming a heterocyclylalkyl ring substituted with R 11 and R 12 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or contains one or more R A or substituted with R 11 and R 12 together with the atoms to which they are attached, are unsubstituted or contain one or more R A The heterocyclylalkyl ring is formed by substituted with

[0313] In some embodiments, the compound is a compound of formula (IV), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 and R 10 is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A In some embodiments, the compound is of formula (IV), or a pharmaceutically acceptable salt or solvate thereof, wherein R 11 and R 12is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A In some embodiments, the compound is of formula (IV), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 , R 10 , R 11 , and R 12 is independently alkyl, cycloalkyl, or hydrogen, and each alkyl and cycloalkyl is independently unsubstituted or contains one or more R A In some embodiments, the compound is of formula (IV), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 , R 10 , R 11 , and R 12 is independently hydrogen, methyl, ethyl, isopropyl, n-propyl, isobutyl, tert-butyl, or n-butyl. In some embodiments, the compound of formula (IV), or a pharmaceutically acceptable salt or solvate thereof, wherein R 9 , R 10 , R 11 , and R 12 Each of is methyl.

[0314] In some embodiments, the compound is of Formula (Iv), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0315] In some embodiments, a compound of Formula (I) having the structure of Formula (Iw), or a pharmaceutically acceptable salt thereof: [ka] During the ceremony, R 1 is hydrogen or methoxy, R A1 and R A2 is independently hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is independently unsubstituted or is one or more of alkyl, aryl, halogen, -OR 13 , -NR(R 18 )R 19 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , or -OC(O)N(R 18 )R 19 is replaced by R A3 -OR 13 , -N(R 18 )R 19 , -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , -C(O)R 14 , -OC(O)R 15 , -OC(O)OR 16 , -OP(O)OR 17 [N(R 18 )R 19 ], -C(O)N(R 18 )R 19 , -OC(O)N(R 18 )R 19 , or -OP(O)OR 20 (OR 21 ) and p is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

[0316] In some embodiments, the compound of Formula (Iw) or a pharmaceutically acceptable salt or solvate thereof, wherein each R A1 and R A2is independently hydrogen, alkyl, or cycloalkyl. In some embodiments, the compound is of Formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein each R A1 and R A2 is independently hydrogen, unsubstituted alkyl, or unsubstituted cycloalkyl. In some embodiments, the compound is of Formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein each R A1 and R A2 are independently hydrogen.

[0317] In some embodiments, the compound is a compound of formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein R A3 is -C(O)OR 13 , -N(R 13 )C(O)OR 14 , -N(R 13 )C(O)R 14 , or -C(O)R 14 In some embodiments, the compound is of formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein R A3 is -C(O)OR 13 In some embodiments, the compound is of formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein R A3 is -C(O)OR 13 and R 13 is hydrogen, or unsubstituted, or contains one or more R B In some embodiments, the compound is of formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein R A3 is -C(O)OR 13 and R 13 is hydrogen, or unsubstituted alkyl. In some embodiments, the compound is of formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein R A3 is -C(O)OR 13 and R 13is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or tert-butyl. In some embodiments, the compound is of formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein R A3 is -C(O)OR 13 and R 13 is hydrogen or tert-butyl.

[0318] In some embodiments, the compound has formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein p is 1, 2, 3, 4, or 5. In some embodiments, the compound has formula (Iw), or a pharmaceutically acceptable salt or solvate thereof, wherein p is 2, 3, 4, or 5.

[0319] In some embodiments, the compound is of Formula (Iv), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka] [ka]

[0320] In some embodiments, R is a compound of Formula (I), (Ia), (Ib), (Ib-1), (Ib1), (Ic), (Id), (Ie), (If), (If1), (Ig), (Ih), (Ii), (Ij), (Ik), (Ik1), (Ik2), (Ik3), (Il), (Im), (Im1), (Im1a), (In), (In1), (Io), (Io1), (Io2), (Io1a), (Ip), (Ip1), (Iq), (Iq1), (Ir), (Ir1), (Is), (It), (Iu), (Iv), or (Iw), or a pharmaceutically acceptable salt thereof; 1In some embodiments, a compound of Formula (I), (Ia), (Ib), (Ib-1), (Ib1), (Ic), (Id), (Ie), (If), (If1), (Ig), (Ih), (Ii), (Ij), (Ik), (Ik1), (Ik2), (Ik3), (Il), (Im), (Im1), (Im1a), (In), (In1), (Io), (Io1), (Io2), (Io1a), (Ip), (Ip1), (Iq), (Iq1), (Ir), (Ir1), (Is), (It), (Iu), (Iv), or (Iw), or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen.

[0321] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 is hydrogen or alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 is hydrogen or unsubstituted alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 4 is an unsubstituted alkyl.

[0322] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is hydrogen or alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5is hydrogen or unsubstituted alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 5 is an unsubstituted alkyl.

[0323] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 and R 5 is hydrogen or alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 where R 5 is hydrogen or unsubstituted alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH2OC(O)R 6 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 where R 6 is alkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5)OC(O)R 6 and R 6 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 and R 6 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 where R 6 is unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted heterocyclylalkyl, unsubstituted aryl, or unsubstituted heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 and R 6 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 and R 6 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)R 6 and R 6 is heterocyclylalkyl substituted with arylalkyl.

[0324] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH2OC(O)OR 6 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6 and R 5 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6 where R 5 is hydrogen or unsubstituted alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6 and R 6 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6 and R 6 is alkyl, heteroalkyl, cycloalkyl, or heterocyclylalkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6 and R 6 is heterocyclylalkyl substituted with alkyl, heteroalkyl, or arylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6and R 6 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6 and R 6 is an unsubstituted alkyl, an unsubstituted heteroalkyl, an unsubstituted cycloalkyl, or an unsubstituted heterocyclylalkyl. In some embodiments, a compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6 and R 6 is heterocyclylalkyl substituted with alkyl, heteroalkyl, or arylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OCH(R 5 )OC(O)OR 6 and R 6 is unsubstituted heterocyclylalkyl.

[0325] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 and R 10 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 and R 10and each is independently unsubstituted alkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(H)R 10 and R 10 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(H)R 10 and R 10 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 where R 9 and R 10 Each of the groups independently represents -N(R 18 )R 19 or -C(O)OR 13 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is unsubstituted alkyl, and R 10 is -N(R 18 )R 19 or -C(O)OR 13 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(H)R 10 and R 10 is -N(R 18 )R 19 or -C(O)OR 13 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R9 is alkyl, and R 10 is -N(R 18 )R 19 is alkyl substituted with R 18 and R 19 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is alkyl, and R 10 is -N(R 18 )R 19 is alkyl substituted with R 18 and R 19 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is unsubstituted alkyl, and R 10 is -N(R 18 )R 19 is alkyl substituted with R 18 and R 19 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(H)R 10 and R 10 is -N(R 18 )R 19 is alkyl substituted with R 18 and R 19 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is alkyl, and R 10 is -C(O)OR 13is alkyl substituted with R 13 is alkyl or hydrogen. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is alkyl, and R 10 is -C(O)OR 13 is alkyl substituted with R 13 is unsubstituted alkyl, or hydrogen. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(H)R 10 and R 10 is -C(O)OR 13 is alkyl substituted with R 13 is unsubstituted alkyl, or hydrogen. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 and R 10 is independently alkyl substituted with —C(O)OH. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is alkyl, and R 10 is alkyl substituted with —C(O)OH. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is C(O)N(H)R 10 and R 10 is alkyl substituted with —C(O)OH.

[0326] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, unsubstituted aryl, unsubstituted heteroaryl, unsubstituted alkyl, or unsubstituted heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with cycloalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with unsubstituted heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with unsubstituted heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with unsubstituted cycloalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is substituted with cycloalkyl substituted with alkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is —OC(O)R 15 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is —OC(O)R 15 is substituted with R 15 is hydrogen, alkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9is hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl, each of which is —OC(O)R 15 is substituted with R 15 is hydrogen, unsubstituted alkyl, unsubstituted aryl, or unsubstituted heteroaryl.

[0327] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, alkyl, cycloalkyl, or heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, unsubstituted alkyl, unsubstituted cycloalkyl, or unsubstituted heteroalkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 is alkyl or heteroalkyl, each of which is —N(R 13 )C(O)R 14 is substituted with R 13 and R 14 is independently hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10and R 10 is alkyl or heteroalkyl, each of which is —C(O)N(R 18 )R 19 is substituted with R 18 and R 19 is independently hydrogen, aryl, heteroaryl, alkyl, or heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 is alkyl or heteroalkyl, each of which is —N(R 13 )C(O)R 14 is substituted with R 13 and R 14 and each is independently hydrogen, unsubstituted aryl, unsubstituted heteroaryl, unsubstituted alkyl, or unsubstituted heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 is alkyl or heteroalkyl, each of which is —C(O)N(R 18 )R 19 is substituted with R 18 and R 19 Each of is independently hydrogen, unsubstituted aryl, unsubstituted heteroaryl, unsubstituted alkyl, or unsubstituted heteroalkyl.

[0328] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, alkyl, cycloalkyl, or heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2is -C(O)N(R 9 )R 10 and R 9 is hydrogen, unsubstituted alkyl, unsubstituted cycloalkyl, or unsubstituted heteroalkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 is -N(R 18 )R 19 is a cycloalkyl substituted with R 18 and R 19 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 is -N(R 18 )R 19 is a cycloalkyl substituted with R 18 and R 19 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 is -N(R 18 )R 19 is a cycloalkyl substituted with R 18 and R 19 together with the atoms to which they are attached form an unsubstituted heterocyclylalkyl ring.

[0329] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9is hydrogen, alkyl, cycloalkyl, or heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 9 is hydrogen, unsubstituted alkyl, unsubstituted cycloalkyl, or unsubstituted heteroalkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 is -OC(O)N(R 18 )R 19 is alkyl substituted with R 18 and R 19 are taken together with the atoms to which they are attached to form a heteroaryl ring or a heterocyclylalkyl ring, each of which is substituted with alkyl, heteroalkyl, or cycloalkyl. In some embodiments, the compounds are of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)N(R 9 )R 10 and R 10 is -OC(O)R 15 is alkyl substituted with R 15 is heterocyclylalkyl substituted with alkyl or arylalkyl.

[0330] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is alkyl, heteroalkyl, heterocyclylalkyl, or cycloalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4is unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted heterocyclylalkyl, or unsubstituted cycloalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is heterocyclylalkyl substituted with aryl or arylalkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is aryl, heterocyclylalkyl, or heterocyclylalkyl substituted with arylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is heterocyclylalkyl substituted with heterocyclylalkyl.

[0331] In some embodiments, the compound is of formula (Iu), or a pharmaceutically acceptable salt or solvate thereof, wherein: [ka]

[0332] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -C(O)OR 13 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -C(O)OR 13 is alkyl substituted with R13 is hydrogen, alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -C(O)OR 13 is alkyl substituted with R 13 is hydrogen, unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted aryl, or unsubstituted heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -OC(O)R 15 is alkyl substituted with R 15 is alkyl, cycloalkyl, heteroaryl, or heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -OC(O)R 15 is alkyl substituted with R 15 is alkyl, cycloalkyl, heteroaryl, or heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -OC(O)R 15 is alkyl substituted with R 15 is unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted heteroaryl, or unsubstituted heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -OC(O)R 15 is alkyl substituted with R15 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -N(R 13 )C(O)R 14 is alkyl substituted with R 13 is alkyl, cycloalkyl, or hydrogen, and R 14 is alkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is -N(R 13 )C(O)R 14 is alkyl substituted with R 13 is unsubstituted alkyl, unsubstituted cycloalkyl, or hydrogen, and R 14 is unsubstituted alkyl, unsubstituted aryl, or unsubstituted heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is an alkyl substituted with an aryl, the aryl being alkyl or -OC(O)OR 16 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is an alkyl substituted with an aryl, the aryl being alkyl or -OC(O)OR 16 is substituted with R 16is alkyl, heteroalkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is an alkyl substituted with an aryl, the aryl being alkyl or -OC(O)OR 16 is substituted with R 16 is unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted cycloalkyl, unsubstituted aryl, or unsubstituted heteroaryl.

[0333] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is C(O)R 14 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is C(O)R 14 heterocyclylalkyl substituted with R 14 is alkyl, heteroalkyl, cycloalkyl, or aryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)R 4 and R 4 is C(O)R 14 heterocyclylalkyl substituted with R 14 is unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted cycloalkyl, or unsubstituted aryl.

[0334] In some embodiments, the compound is of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 2 is -P(O)OR 11 (OR12 ) or CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 is hydrogen and R 12 is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, and the alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl is unsubstituted or is substituted with one or more R A In some embodiments, the compound is of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) or CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 is hydrogen and R 12 is unsubstituted or contains one or more R A is alkyl substituted with

[0335] In some embodiments, a compound of Formula (I) or (Iu), or a pharmaceutically acceptable salt thereof, wherein R 20 is hydrogen and R 21 is alkyl, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and the alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl is unsubstituted or contains one or more R B or substituted with R 20 and R 21 together with the atoms to which they are attached, are unsubstituted or contain one or more R B In some embodiments, the compound of formula (I) or (Iu), or a pharmaceutically acceptable salt thereof, wherein R 20 is hydrogen and R 21 is unsubstituted or contains one or more RB is alkyl substituted with

[0336] In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -CH(R 5 )OC(O)OR 6 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -CH(R 5 )OC(O)OR 6 and R 5 and R 6 is independently hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R A In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -CH(R 5 )OC(O)OR 6 and R 5 and R 6 Each of is independently hydrogen, or unsubstituted or one or more R A In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -CH(R 5 )OC(O)OR 6 and R 5 is hydrogen and R 6 is hydrogen, or unsubstituted, or contains one or more R A In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -CH(R 5 )OC(O)OR 6 and R 5 is hydrogen and R 6is methyl, ethyl, n-propyl, isopropyl, isobutyl, tert-butyl, or n-butyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 2 is -CH(R 5 )OC(O)OR 6 and R 5 is hydrogen and R 6 is ethyl.

[0337] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 5 is hydrogen, alkyl, cycloalkyl, or heteroalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 5 is hydrogen, unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted heteroalkyl, or alkyl substituted with heteroaryl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 and R 12In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 and R 12 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 and R 12 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 and R 12 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the is -OC(O)R 15 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 and R12 Each of the is -OC(O)R 15 and each R 15 is alkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the is -OC(O)R 15 and each R 15 is unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted heterocyclylalkyl, unsubstituted aryl, or unsubstituted heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the is -OC(O)R 15 and each R 15 is heterocyclylalkyl substituted with alkyl or arylalkyl.

[0338] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 ] and R 5is hydrogen, alkyl, cycloalkyl, heteroalkyl, or alkyl substituted with heteroaryl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 ] and R 4 is hydrogen, unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted heteroalkyl, or alkyl substituted with heteroaryl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 ] and R 8 is alkyl, cycloalkyl, aryl, heteroaryl, alkyl, or alkyl substituted with aryl or heteroaryl; R 9 is hydrogen and R 12 is -C(O)OR 13 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 ] and R 8 is unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted aryl, unsubstituted heteroaryl, unsubstituted alkyl, or alkyl substituted with aryl or heteroaryl; R 9 is hydrogen and R 12 is -C(O)OR 13 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 13In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -CH(R 5 )OP(O)OR 8 [N(R 9 )R 10 ] and R 12 is -C(O)OR 13 is alkyl substituted with R 13 is an unsubstituted alkyl.

[0339] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the formulas is -C(O)OR 13 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 13is alkyl, cycloalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 13 is unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted aryl, or unsubstituted heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the is -OC(O)R 15 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the is -OC(O)R 15 is alkyl substituted with R 15 is alkyl, cycloalkyl, heteroaryl, or heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the is -OC(O)R 15 is alkyl substituted with R 15 is unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted heteroaryl, or unsubstituted heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12Each of the is -OC(O)R 15 is alkyl substituted with R 15 is heterocyclylalkyl substituted with alkyl or arylalkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the is -OC(O)OR 16 is alkyl substituted with R 16 is alkyl, cycloalkyl, heteroaryl, or heterocyclylalkyl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 Each of the is -OC(O)OR 16 is alkyl substituted with R 16 is unsubstituted alkyl, unsubstituted cycloalkyl, unsubstituted heteroaryl, or unsubstituted heterocyclylalkyl.

[0340] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 together with the atom to which they are attached form a heterocyclylalkyl ring. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12and R are taken together with the atoms to which they are attached to form an unsubstituted heterocyclylalkyl ring. In some embodiments, the compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 and together with the atom to which they are attached form an aryl-substituted heterocyclylalkyl ring. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 and R are taken together with the atoms to which they are attached to form a heterocyclylalkyl ring substituted with an unsubstituted aryl. In some embodiments, the compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 11 (OR 12 ) and R 11 and R 12 together with the atoms to which they are attached form a heterocyclylalkyl ring substituted with an aryl, wherein the aryl is substituted with a halogen.

[0341] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 8 [N(R 9 )R 10 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 8 [N(R 9 )R 10 ] and R 8is alkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 8 [N(R 9 )R 10 ] and R 8 is unsubstituted alkyl, unsubstituted aryl, or unsubstituted heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 8 [N(R 9 )R 10 ] and R 9 and R 10 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 8 [N(R 9 )R 10 ] and R 8 is unsubstituted alkyl, unsubstituted aryl, or unsubstituted heteroaryl, and R 9 is hydrogen and R 10 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 8 [N(R 9 )R 10 ] and R 8 is unsubstituted alkyl, unsubstituted aryl, or unsubstituted heteroaryl, and R 9 is hydrogen and R 10 is -C(O)R 14 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -P(O)OR 8 [N(R 9 )R 10 ] and R 10 is -C(O)R14 is alkyl substituted with R 14 is hydrogen or alkyl. In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 14 is an unsubstituted alkyl.

[0342] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -S(O)2OR 7 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -S(O)2OR 7 and R 7 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -S(O)2OR 7 and R 7 is -C(O)R 14 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 7 is -C(O)R 14 is alkyl substituted with R 14 is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -S(O)2OR 7 and R 7 is -C(O)R 14 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 7 is -C(O)R 14 is alkyl substituted with R 14In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -S(O)2OR 7 and R 7 is -C(O)R 14 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 7 is -C(O)R 14 is alkyl substituted with R 14 is heterocyclylalkyl substituted with alkyl, —C(O)CH 3 , or C(O)Ph.

[0343] In some embodiments, R is a compound of Formula (I), (Ia), (Ib), (Ib-1), (Ib1), (Ic), (Id), (Ie), (If), (If1), (Ig), (Ih), (Ii), (Ij), (Ik), (Ik1), (Ik2), (Ik3), (Il), (Im), (Im1), (Im1a), (In), (In1), (Io), (Io1), (Io2), (Io1a), (Ip), (Ip1), (Iq), (Iq1), (Ir), (Ir1), (Is), (It), (Iu), (Iv), or (Iw), or a pharmaceutically acceptable salt thereof; 1 is hydrogen. In some embodiments, a compound of Formula (I), (Ia), (Ib), (Ib-1), (Ib1), (Ic), (Id), (Ie), (If), (If1), (Ig), (Ih), (Ii), (Ij), (Ik), (Ik1), (Ik2), (Ik3), (Il), (Im), (Im1), (Im1a), (In), (In1), (Io), (Io1), (Io2), (Io1a), (Ip), (Ip1), (Iq), (Iq1), (Ir), (Ir1), (Is), (It), (Iu), (Iv), or (Iw), or a pharmaceutically acceptable salt thereof, wherein R 1 is methoxy.

[0344] In some embodiments, the compound is a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OR 3 and R 3 is OP(O)OR 20 (OR 21 In some embodiments, the compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OR 3 and R 3 is -OP(O)OR 20 (OR 21 ) and R 20 and R 21 and each is independently alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl. In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OR 3 and R 3 is -OP(O)OR 20 (OR 21 ) and R 20 and R 21 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OR 3 and R 3 is -OP(O)OR 20 (OR 21 ) and R 20 and R 21 In some embodiments, the compound is of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 2 is -C(O)OR 3 and R 3 is -OP(O)OR20 (OR 21 ) and R 20 and R 21 Each of is independently unsubstituted alkyl.

[0345] In another aspect, the present disclosure provides compounds of formula (I), (Ia), (Ib), (Ib-1), (Ib1), (Ic), (Id), (Ie), (If), (If1), (Ig), (Ih), (Ii), (Ij), (Ik), (Ik1), (Ik2), (Ik3), (Il), (Im), (Im1), (Im1a), (In), (In1), (Io), (Io1), (I (Io2), (Io1a), (Ip), (Ip1), (Iq), (Iq1), (Ir), (Ir1), (Is), (It), (Iu), (Iv), or (Iw), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, carrier, adjuvant, or vehicle.

[0346] The pharmaceutical compositions of the present disclosure can include racemic, scalemic, or diasteromeric enriched mixtures of any compound described herein that contains a stereocenter.

[0347] Selected compounds of the present disclosure with their corresponding Simplified Molecular Input Line Entry System (SMILES) strings are provided in Table 1. [Table 1-1] [Table 1-2] [Table 1-3] [Table 1-4] [Table 1-5] [Table 1-6] Table 1-7 Table 1-8 Table 1-9 Table 1-10 Table 1-11 Table 1-12 Table 1-13 Table 1-14 Table 1-15 Table 1-16 Table 1-17 Table 1-18 Table 1-19 Table 1-20 Table 1-21 Table 1-22 Table 1-23 Table 1-24 Table 1-25 Table 1-26 Table 1-27 Table 1-28 Table 1-29 Table 1-30 Table 1-31 Table 1-32 Table 1-33 Table 1-34 Table 1-35 Table 1-36 Table 1-37 Table 1-38 Table 1-39 Table 1-40 [Table 1-41] [Table 1-42] [Table 1-43] [Table 1-44] [Table 1-45] [Table 1-46] [Table 1-47] [Table 1-48] [Table 1-49] [Table 1-50] [Table 1-51] [Table 1-52] [Table 1-53]

[0348] In some embodiments, the compound described herein is a compound selected from Table 1.

[0349] In some embodiments, the compound described herein is a compound selected from Table 1A below. [Table 2-1] Table 2-2 Table 2-3 Table 2-4 Table 2-5 Table 2-6 Table 2-7 Table 2-8 Table 2-9 Table 2-10 Table 2-11 Table 2-12 Table 2-13 Table 2-14 Table 2-15 Table 2-16 Table 2-17

[0350] Treatment methods. In yet another aspect, the disclosure provides a method of treating or preventing a disease, disorder, or condition in which increased levels of a tryptamine hallucinogen such as DMT are beneficial, comprising administering to a subject in need thereof an effective amount of a compound of Formula (I), (Ia), (Ib), (Ib-1), (Ib1), (Ic), (Id), (Ie), (If), (If1), (Ig), (Ih), (Ii), (Ij), (Ik), (Ik1) ), (Ik2), (Ik3), (Il), (Im), (Im1), (Im1a), (In), (In1), (Io), (Io1), (Io2), (Io1a), (Ip), (Ip1), (Iq), (Iq1), (Ir), (Ir1), (Is), (It), (Iu), (Iv), or (Iw), or a pharmaceutically acceptable salt thereof. In some embodiments, the condition comprises post-traumatic stress disorder, major depression, schizophrenia, Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Parkinson's disease dementia, dementia, Lewy body dementia, multiple system atrophy, or substance abuse. In some embodiments, the condition comprises a musculoskeletal pain disorder, including fibromyalgia, muscle pain, joint stiffness, osteoarthritis, rheumatoid arthritis, and muscle spasms. In some embodiments, the present disclosure provides a method for treating disorders of female reproductive health, including premenstrual arrhythmia (PMDD), premenstrual syndrome (PMS), postpartum depression, and menopause. The compounds of the present invention can also be used to treat any brain disorder.

[0351] In some embodiments, the compounds disclosed herein are 5-HT 2A In some embodiments, the compounds disclosed herein have activity as 5-HT 2A Elicit biological responses by activating receptors (e.g., 5-HT 2A Allosteric regulation or modulation of biological targets that activate receptors). 5-HT 2A 5-HT agonism correlates with the promotion of neuroplasticity. 2A The antagonist is 5-HT 2AIn some embodiments, the compounds disclosed herein inhibit the neuritogenesis and spinogenesis effects of hallucinogenic compounds with agonistic activity, such as DMT, LSD, and DOI. 2A In some embodiments, the compounds disclosed herein are selective 5-HT modulators and promote neuroplasticity (e.g., cortical structural plasticity). 2A The compound is a modulator and promotes neuroplasticity (e.g., cortical structural plasticity). Promotion of neuroplasticity can include, for example, increased dendritic spine growth, increased synaptic protein synthesis, enhanced synaptic response, increased dendritic spine complexity, increased dendritic branching content, increased spine production, increased neuritogenesis, or any combination thereof. In some embodiments, increased neuroplasticity includes increased cortical structural plasticity in the anterior part of the brain.

[0352] In some embodiments, 5-HT 2A modulators (e.g., 5-HT 2A In some embodiments, the non-hallucinogenic 5-HT agonist is non-hallucinogenic. 2A modulators (e.g., 5-HT 2A agonists) are used to treat neurological disorders in which modulators induce dissociative side effects. In some embodiments, the hallucinogenic potency of the compounds described herein is assessed in vitro. In some embodiments, the hallucinogenic potency of the compounds described herein assessed in vitro is compared to the hallucinogenic potency of a hallucinogenic homolog assessed in vitro. In some embodiments, the compounds described herein induce less hallucinogenic potency in vitro than the hallucinogenic homolog.

[0353] In some embodiments, a modulator of serotonin receptor 2A (5-HT 2A Modulators, e.g., 5-HT 2A Serotonin receptor modulators, such as 5-HT agonists, are used to treat brain disorders. In some embodiments, the compounds of the present disclosure inhibit 5-HT 2Aalone as an agonist or as a 5-HT 2A They function in combination with a second therapeutic agent that is also a modulator. In such cases, the second therapeutic agent can be an agonist or antagonist. In some cases, they may be used to modulate 5-HT receptors, such as those with potential hallucinogenic effects. 2A To mitigate the undesirable effects of 5-HT agonism 2A It may be useful to administer an antagonist in combination with the compounds of the present disclosure. Serotonin receptor modulators useful as second therapeutic agents for the combination therapies described herein are known to those of skill in the art and i...

Claims

1. A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein 【Chemical 1】 In the formula R １ is methoxy or hydrogen, and R ２ is -C(O)OR ３ 、 -C(O)R ４ 、 -CH(R ５ )OR ６ 、 -C(O)OCH(R ５ )OC(O)R ６ 、 -C(O)OCH(R ５ )OC(O)OR ６ 、 -CH(R ５ )C(O)R ６ 、 -CH(R ５ )OC(O)R ６ 、 -CH(R ５ )OC(O)OR ６ 、 -S(O) ２ OR ７ 、 -P(O)OR ８ [N(R ９ )R １０ 、 -P(O)[N(R ９ )R １０ [N(R １１ )R １２ 、 -C(O)N(R ９ )R １０ 、 -P(O)OR １１ (OR １２ )、 -CH(R ５ )OP(O)OR ８ [N(R ９ )R １０ 、 or -CH(R ５ )OP(O)OR １１ (OR １２ ) and R ３ 、R ４ 、R ５ 、R ６ 、R ７ 、and R ８ each of which is, independently, hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is, independently, unsubstituted or substituted with one or more R Ａ ; R ９ and R １０ each independently is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R Ａ or R ９ and R １０ together with the atoms to which they are attached form an unsubstituted or one or more R Ａ substituted heterocyclylalkyl ring, R １１ and R １２ each independently is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R Ａ or R １１ and R １２ together with the atom to which they are attached form an unsubstituted or substituted with one or more R Ａ heterocyclylalkyl ring, Each R Ａ is, independently, alkyl, heteroalkyl, cycloalkyl, heteroscyclylalkyl, aryl, heteroaryl, an amino acid side chain, -OR １３ , -N(R １８ )R １９ , -C(O)OR １３ , -N(R １３ )C(O)OR １４ , -N(R １３ )C(O)R １４ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , -OP(O)OR １７ [N(R １８ )R １９ , -C(O)N(R １８ )R １９ , -OC(O)N(R １８ )R １９ , or -OP(O)OR ２０ (OR ２１ ), and each alkyl, heteroalkyl, cycloalkyl, heteroscyclylalkyl, amino acid side chain, aryl, and heteroaryl is, independently, unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ )R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ )R １９ . R １３ , R １４ , R １５ , R １６ , or R １７ each of which is independently alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R Ｂ and is substituted with R １８ and R １９ each is, independently, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is, independently, unsubstituted or substituted with one or more R Ｂ or R １８ and R １９ together with the atom to which they are attached form an unsubstituted or substituted with one or more R Ｂ heterocyclylalkyl ring, R ２０ and R ２１ each independently is alkyl, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R Ｂ or R ２０ and R ２１ together with the atom to which they are attached form an unsubstituted or one or more R Ｂ substituted heterocyclylalkyl ring, Each R Ｂ is independently halogen, amino, cyano, hydroxyl, alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, arylalkyl, -C(O)CH ３ , -C(O)Ph, or heteroarylalkyl, and each cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl, R １ wherein R is hydrogen, ３ said compound or a pharmaceutically acceptable salt thereof, provided that R is not tert-butyl.

2. Having the structure of formula (Ia) 【Chemical 2】 wherein R １ is methoxy or hydrogen, and R ３ is alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl, each of which is independently unsubstituted or substituted with one or more R Ａ , the compound according to claim 1, or a pharmaceutically acceptable salt thereof.

3. a) Having the structure of formula (Ib), wherein 【Chemical Formula 4】 In the formula R １ is methoxy or hydrogen, and R Ａ１ 、 R Ａ２ 、 R Ａ３ 、 and R Ａ４ each independently is hydrogen or independently is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ ), R １９ and is alkyl substituted therewith, R Ａ５ is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR １３ , -N(R １３ )C(O)OR １４ , -N(R １３ )C(O)R １４ , -C(O)R １４ , -OC(O)R １５ , or -OC(O)OR １６ and each heteroalkyl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ )R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ )R １９ ), Optionally having the structure of formula (Ib1) 【Chemical Formula 5】 Or b) Having the structure of formula (Ic) 【Chemical Formula 7】 wherein R １ is hydrogen or methoxy, and each of R １８ and R １９ is independently hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each alkyl, cycloalkyl, and heteroalkyl is independently unsubstituted or substituted with one or more R Ｂ , or R １８ and R １９ together with the atom to which they are attached form an unsubstituted or substituted with one or more R Ｂ heterocyclic alkyl ring, The compound according to claim 1 or 2, or a pharmaceutically acceptable salt thereof.

4. a) Having the structure of formula (Id) 【Chemical 8】 wherein R １ is hydrogen or methoxy, and R ５ is alkyl or cycloalkyl (each of which is independently unsubstituted or substituted with one or more R Ａ ), or hydrogen, and R Ａ６ is hydrogen, or unsubstituted, or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ )R １９ and is alkyl substituted with Or b) Having the structure of formula (Ie) 【Chemical Formula 9】 wherein R １ is hydrogen or methoxy, and R ５ is hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is independently unsubstituted or substituted with one or more R Ａ . The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

5. Having the structure of formula (If), optionally 【Chemical Formula 10】 wherein R １ is methoxy or hydrogen, and each of R ９ and R １０ is independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, or heterocyclylalkyl, and each alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, and heterocyclylalkyl is independently unsubstituted or substituted with one or more R Ａ , or R ９ and R １０ together with the atom to which they are attached form a heterocyclylalkyl ring that is unsubstituted or substituted with one or more R Ａ ​ a) Having the structure of formula (If1), wherein In the formula 【Chemical Formula 12】 b) Having the structure of formula (Ig), wherein R １ is methoxy or hydrogen, and R １０ is hydrogen, alkyl, heteroalkyl, cycloalkyl, or heterocyclylalkyl, and each of alkyl, heteroalkyl, cycloalkyl, and heterocyclylalkyl is unsubstituted or substituted with one or more R Ａ groups, X １ and X ２ each independently is -CH ２ -, -O-, -NH-, -S-, -S(O)-, -S(O) ２ -, or -N(Y １ )- selected from, each Y １ is independently hydrogen, cycloalkyl, heteroalkyl, or alkyl In the formula 【Chemical 13】 c) Having the structure of formula (Ih), wherein R １ is methoxy or hydrogen, and R Ａ１ 、 R Ａ２ 、 R Ａ３ 、 and R Ａ４ each is, independently, hydrogen, or unsubstituted, or one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ ), R １９ and is alkyl substituted with R １０ is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of alkyl, heteroalkyl, and cycloalkyl is unsubstituted or substituted with one or more R Ａ groups, R Ａ５ is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR １３ , -N(R １３ )C(O)OR １４ , -N(R １３ )C(O)R １４ , -C(O)R １４ , -OC(O)R １５ , or -OC(O)OR １６ wherein each of heteroalkyl, heterocyclylalkyl, and heteroaryl is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ )R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ )R １９ ), In the formula 【Chemical Formula 15】 d) Having the structure of formula (Ii), wherein R １ is hydrogen or methoxy, R １０ is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of alkyl, heteroalkyl, and cycloalkyl is unsubstituted or substituted with one or more R Ａ groups, R １８ and R １９ each is, independently, hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each alkyl, cycloalkyl, or heterosilylalkyl is, independently, unsubstituted or substituted with one or more R Ｂ or R １８ and R １９ together with the atom to which they are attached form an unsubstituted or R Ｂ substituted heterosilylalkyl ring, In the formula 【Chemical 16】 In the formula R １ is hydrogen or methoxy, R ５ and R １０ each is independently hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each alkyl, heteroalkyl, and cycloalkyl is independently unsubstituted or substituted with one or more R Ａ and is substituted, R Ａ６ is independently hydrogen, alkyl, heteroalkyl, or cycloalkyl, where each of the alkyl, heteroalkyl, or cycloalkyl is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), -C(O)R １９ , -OC(O)R １４ , -OC(O)OR １５ , or -OC(O)N(R １６ ),R １８ ), and １９ is substituted with Or e) Having the structure of formula (Ij) 【Chemical 17】 wherein, R １ is hydrogen or methoxy, and each of R ５ and R １０ is hydrogen, alkyl, or heteroalkyl, and each of alkyl and heteroalkyl is independently unsubstituted or substituted with one or more R Ａ groups. The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

6. Having the structure of formula (Ik), optionally 【Chemical Formula 18】 wherein R １ is hydrogen or methoxy, and R ４ is alkyl, heterocyclylalkyl, aryl, heteroaryl, or heteroalkyl, each of which is unsubstituted or substituted with one or more R Ａ groups. a) Having the structure of formula (Ik1), wherein In the formula 【Chemical 22】 b) Having the structure of formula (Ik2), wherein R １ is methoxy or hydrogen, and R Ａ１ 、 R Ａ２ 、 R Ａ３ 、 and R Ａ４ each is, independently, hydrogen, alkyl, or an amino acid side chain, and each alkyl or amino acid side chain is, independently, unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ 、 -NR(R １８ ), R １９ 、 -C(O)R １４ 、 -OC(O)R １５ 、 -OC(O)OR １６ 、 or -OC(O)N(R １８ ), R １９ and is substituted therewith, R １０ is hydrogen, alkyl, heteroalkyl, or cycloalkyl, and each of alkyl, heteroalkyl, and cycloalkyl is unsubstituted or substituted with one or more R Ａ groups, R Ａ５ is heteroalkyl, heterocyclylalkyl, heteroaryl, -C(O)OR １３ , -N(R １３ )C(O)OR １４ , -N(R １３ )C(O)R １４ , -C(O)R １４ , -OC(O)R １５ , or -OC(O)OR １６ and each of heteroalkyl, heterocyclylalkyl, heteroaryl is unsubstituted or substituted by one or more of alkyl, aryl, halogen, -OR １３ , -NR(R １８ )R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ )R １９ ), In the formula 【Chemical 23】 In the formula R １ is methoxy or hydrogen, and R １３ is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, or heterocyclylalkyl, and each of alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl, and heterocyclylalkyl is unsubstituted or substituted with one or more R Ｂ groups, p is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 c) Having the structure of formula (Ik3), wherein 【Chemical 24】 In the formula R １ is methoxy or hydrogen, and R Ａ１ is an alkyl or amino acid side chain, each of which is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), -C(O)R １９ , -OC(O)R １４ , -OC(O)OR １５ , -OC(O)N(R １６ ), or -OC(O)N(R １８ ), １９ and is substituted with R Ａ５ is -N(R １８ )R １９ or -N(R １３ )C(O)R １４ wherein Or d) Having the structure of formula (Is) 【Chemical Formula 50】 wherein R １ is hydrogen or methoxy, and R １５ is alkyl, heteroalkyl, cycloalkyl, aryl, or heteroaryl, each of which is unsubstituted or substituted with one or more R Ｂ groups. The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

7. Having the structure of formula (Il), wherein 【Chemical Formula 25】 In the formula R １ is methoxy or hydrogen, and R ５ is hydrogen, alkyl, or cycloalkyl, and each of the alkyl or cycloalkyl is unsubstituted or substituted with one or more R Ａ groups, R ６ is alkyl, cycloalkyl, heterocyclylalkyl, or heteroalkyl, and each of alkyl, cycloalkyl, heterocyclylalkyl, or heteroalkyl is unsubstituted or substituted with one or more R Ａ as defined in claim 1, or a pharmaceutically acceptable salt thereof.

8. Having the structure of formula (Im), wherein 【Chemical 26】 In the formula R １ is methoxy or hydrogen, and R ５ is hydrogen, alkyl, cycloalkyl, or heteroalkyl, and each of alkyl, cycloalkyl, and heteroalkyl is unsubstituted or substituted with one or more R Ａ groups, R １１ and R １２ each independently is hydrogen, cycloalkyl, aryl, heteroaryl, or alkyl, and each of alkyl, cycloalkyl, and heteroalkyl is independently unsubstituted or substituted with one or more R Ａ groups Optionally a) Having the structure of formula (Im1), wherein 【Chemical Formula 28】 In the formula R １ is methoxy or hydrogen, and R Ａ１ 、 R Ａ３ 、 and R ５ each of which is independently hydrogen, alkyl, or cycloalkyl, R Ａ２ and R Ａ４ each independently is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, or heteroaryl, -OC(O)R １５ or -OC(O)OR １６ and Each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is, independently, unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ ), R １９ and is substituted with Or b) Having the structure of formula (Im1a), wherein 【Chemical Formula 29】 In the formula R １ is methoxy or hydrogen, and R Ａ１ 、 R Ａ３ 、 and R ５ each is, independently, hydrogen, alkyl, or cycloalkyl, and each of alkyl and cycloalkyl is, independently, unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ 、 -NR(R １８ )R １９ 、 -C(O)R １４ 、 -OC(O)R １５ 、 -OC(O)OR １６ 、 or -OC(O)N(R １８ )R １９ and is substituted with R Ｂ１ and R Ｂ２ each is, independently, hydrogen, or unsubstituted or alkyl substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl, The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

9. Having the structure of formula (In), wherein 【Chemical Formula 30】 In the formula R １ is methoxy or hydrogen, and R ５ is hydrogen, alkyl, or cycloalkyl, and R ８ is hydrogen, alkyl, cycloalkyl, aryl, heteroscyclylalkyl, or heteroaryl, and R ９ and R １０ each is, independently, hydrogen or alkyl, Each cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more R Ａ groups Optionally Having the structure of formula (In1), wherein 【Chemical 31】 In the formula R １ is methoxy or hydrogen, and R Ａ１ is hydrogen, alkyl, or cycloalkyl, and each of alkyl and cycloalkyl is unsubstituted or substituted with alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), -C(O)R １９ , -OC(O)R １４ , -OC(O)OR １５ , -OC(O)N(R １６ ), or -OC(O)N(R １８ ), １９ and is substituted with R ５ and R ８ each is hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl are independently unsubstituted or substituted with one or more R Ａ groups, R １３ is hydrogen, or is unsubstituted or substituted with one or more R Ｂ groups and is alkyl The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

10. Having the structure of formula (Io), wherein 【Chemical Formula 32】 In the formula R １ is methoxy or hydrogen, and R １１ and R １２ each independently is selected from hydrogen, cycloalkyl, aryl, heteroaryl, or alkyl, and each cycloalkyl, aryl, heteroaryl, and alkyl is independently unsubstituted or substituted with one or more R Ａ or R １１ and R １２ together with the atom to which they are attached form an unsubstituted or substituted with one or more R Ａ heterocyclic alkyl ring Optionally a) Having the structure of formula (Io1), wherein 【Chemical 34】 In the formula R １ is methoxy or hydrogen, and R Ａ１ and R Ａ３ each independently is hydrogen, alkyl, or cycloalkyl, R Ａ２ and R Ａ４ each independently is alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, heteroaryl, -OC(O)R １５ or -OC(O)OR １６ wherein Each alkyl, heteroalkyl, cycloalkyl, heterocyclylalkyl, aryl, and heteroaryl is, independently, unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ ), R １９ wherein it is substituted with b) Having the structure of formula (Io2) 【Chemical 35】 wherein, R １ is methoxy or hydrogen, and R Ａ１ is aryl or heteroaryl, each of which is unsubstituted or substituted by one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), -C(O)R １９ , -OC(O)R １４ , -OC(O)OR １５ , -OC(O)NR １６ ), or -OC(O)N(R １８ ), １９ substituted with​ Or c) Having the structure of formula (Io1a), wherein 【Chemical 38】 In the formula R １ is methoxy or hydrogen, R Ａ１ and R Ａ３ each is, independently, hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is, independently, unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ ), R １９ and is substituted therewith, R Ｂ１ and R Ｂ２ each independently is hydrogen, or unsubstituted or alkyl substituted with one or more halogen, amino, cyano, hydroxyl, alkyl, acetyl, or benzoyl, The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

11. Having the structure of formula (Ip), wherein 【Chemical Formula 39】 In the formula R １ is methoxy or hydrogen, and R ８ is hydrogen, alkyl, cycloalkyl, aryl, heteroscyclylalkyl, or heteroaryl, and R ９ and R １０ each is, independently, hydrogen or alkyl, Each alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more R Ａ groups. Optionally Having the structure of formula (Ip1), wherein 【Chemical 40】 In the formula R １ is methoxy or hydrogen, and R Ａ１ is hydrogen, alkyl, or cycloalkyl, each of alkyl and cycloalkyl being unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ ), R １９ and being substituted with R ８ is hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and each alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is unsubstituted or substituted with one or more R Ａ groups, R １３ is hydrogen, or unsubstituted or substituted with one or more R Ｂ groups and is alkyl The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

12. Having the structure of formula (Iq), wherein 【Chemical 41】 In the formula R １ is methoxy or hydrogen, and R ５ is hydrogen, alkyl, or cycloalkyl, and R ６ is alkyl, cycloalkyl, heteroalkyl, heterocyclylalkyl, aryl, or heteroaryl, and Each alkyl, cycloalkyl, heteroaryl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more Rs Ａ wherein Optionally Having the structure of formula (Iq1), wherein 【Chemical Formula 42】 In the formula R １ is methoxy or hydrogen, and R ５ is hydrogen, alkyl, or cycloalkyl, and each of alkyl and cycloalkyl is unsubstituted or substituted with one or more R Ａ groups, Q １ is 【Chemical Formula 43】 And Y １ , Y ２ , or Y ３ each of which is independently —O—, —S—, —S(O)—, —S(O) ２ —, —N(R Ｙ１ ), or —NC(O)R Ｙ２ wherein R Ｙ１ and R Ｙ２ are each independently hydrogen, alkyl, heteroalkyl, or heteroaryl The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

13. Having the structure of formula (Ir), wherein 【Chemical 45】 In the formula R １ is methoxy or hydrogen, and R ５ is hydrogen, alkyl, or cycloalkyl, and R ６ is alkyl, cycloalkyl, heteroalkyl, heterocyclylalkyl, aryl, or heteroaryl, and Each alkyl, cycloalkyl, heteroaryl, heterocyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R Ａ groups. Optionally Having the structure of formula (Ir1), wherein 【Chemical Formula 46】 In the formula R １ is methoxy or hydrogen, and R ５ is hydrogen, alkyl, or cycloalkyl, each of alkyl and cycloalkyl being unsubstituted or substituted with one or more R Ａ groups, Q １ is 【Chemical 47】 And Y １ , Y ２ , or Y ３ each independently is —O—, —S—, —S(O)—, —S(O) ２ —, —N(R Ｙ１ ), or —NC(O)R Ｙ２ wherein each of R Ｙ１ and R Ｙ２ is independently hydrogen, alkyl, heteroalkyl, or heteroaryl, The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

14. a) having the structure of formula (It), 【Chemical 51】 In the formula, R １ is hydrogen or methoxy, and R １３ is alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, each of which is unsubstituted or substituted with one or more R Ｂ groups. b) having the structure of formula (Iu), 【Chemical 59】 wherein, R １ is hydrogen or methoxy, and R Ａ１ is hydrogen, alkyl, or cycloalkyl, and each of alkyl and cycloalkyl is unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), -C(O)R １９ , -OC(O)R １４ , -OC(O)OR １５ , -OC(O)N(R １６ ), or -OC(O)N(R １８ ), １９ and is substituted with R ２０ and R ２１ each is, independently, hydrogen, alkyl, cycloalkyl, aryl, heterocyclylalkyl, or heteroaryl, and each alkyl, cycloalkyl, aryl, heterocyclylalkyl, and heteroaryl is, independently, unsubstituted or substituted with one or more R Ｂ or R ２０ and R ２１ together with the atom to which they are attached form an unsubstituted or substituted with one or more R Ｂ heterocyclylalkyl ring, c) having the structure of formula (Ib-1), 【Chemical Formula 60】 wherein, R １ is methoxy or hydrogen, and R Ａ１ 、R Ａ２ 、R Ａ３ 、R Ａ４ 、R Ａ６ 、and R Ａ７ each is, independently, hydrogen, or independently, unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ 、-NR(R １８ )R １９ 、-C(O)R １４ 、-OC(O)R １５ 、-OC(O)OR １６ 、or -OC(O)N(R １８ )R １９ and is alkyl substituted with R Ａ５ is heteroalkyl, heterocyclylalkyl, heteroaryl, or -C(O)OR １３ , -N(R １３ )C(O)OR １４ , -N(R １３ )C(O)R １４ , -C(O)R １４ , -OC(O)R １５ , or -OC(O)OR １６ and each heteroalkyl, heterocyclylalkyl, and heteroaryl is independently unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ )R １９ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , or -OC(O)N(R １８ )R １９ ), d) having the structure of formula (Iv), 【Chemical Formula 61】 wherein, R １ is hydrogen or methoxy, and R ９ and R １０ each independently is alkyl, heteroalkyl, cycloalkyl, heterosilylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heterosilylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R Ａ or R ９ and R １０ together with the atom to which they are attached form an unsubstituted or substituted with one or more R Ａ heterosilylalkyl ring, R １１ and R １２ each independently is alkyl, heteroalkyl, cycloalkyl, heteroscyclylalkyl, aryl, heteroaryl, or hydrogen, and each alkyl, heteroalkyl, cycloalkyl, heteroscyclylalkyl, aryl, and heteroaryl is independently unsubstituted or substituted with one or more R Ａ or R １１ and R １２ together with the atom to which they are attached form an unsubstituted or one or more R Ａ substituted heteroscyclylalkyl ring or, e) having the structure of formula (Iw), 【Chemical Formula 62】 wherein, R １ is hydrogen or methoxy, and R Ａ１ and R Ａ２ each is, independently, hydrogen, alkyl, or cycloalkyl, and each alkyl and cycloalkyl is, independently, unsubstituted or substituted with one or more alkyl, aryl, halogen, -OR １３ , -NR(R １８ ), -C(O)R １９ , -OC(O)R １４ , -OC(O)OR １５ , -OC(O)N(R １６ ), or -OC(O)N(R １８ ), １９ and is substituted with R Ａ３ is -OR １３ , -N(R １８ )R １９ , -C(O)OR １３ , -N(R １３ )C(O)OR １４ , -N(R １３ )C(O)R １４ , -C(O)R １４ , -OC(O)R １５ , -OC(O)OR １６ , -OP(O)OR １７ [N(R １８ )R １９ , -C(O)N(R １８ )R １９ , -OC(O)N(R １８ )R １９ , or -OP(O)OR ２０ (OR ２１ ) and p is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, The compound according to claim 1, or a pharmaceutically acceptable salt thereof.

15. A pharmaceutical composition comprising the compound according to any one of claims 1 to 14, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, carrier, adjuvant, or vehicle.

16. For use in a method of treating or preventing a disease, disorder, or condition in which an increase in the level of a tryptamine hallucinogen such as DMT or 5-O-Me-DMT is beneficial, a compound according to any one of claims 1 to 14, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition according to claim 15, Optionally, wherein the condition includes post-traumatic stress disorder, major depressive disorder, schizophrenia, Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Parkinson's disease dementia, dementia, Lewy body dementia, multiple system atrophy, or substance abuse. A compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition.

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