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1. WO2020163409 - PROCÉDÉS ET COMPOSITIONS POUR MODULER L'ÉPISSAGE

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

CLAIMS

What is claimed is:

1. A compound of Formula (I), or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof:


wherein,

RA is hydrogen, deuterium, F, Cl, ‒CN, ‒OR1, ‒SR1, -S(=O)R1, -S(=O)2R1, substituted or unsubstituted C1‒C4 alkyl, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3-C4 cycloalkyl, or substituted or unsubstituted C2-C3 heterocycloalkyl;

ring Q is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

is a single bond or a double bond;

X is
and Z is C; or

X is
and Z is N or CR2;

Ring G is monocyclic, fused, or spiro C4-C12 heterocycloalkyl;

R1 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C13 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R2, when present, is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, or substituted or unsubstituted C1‒C4 haloalkyl; and

each R4 is independently hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, or substituted or unsubstituted C1‒C4 heteroalkyl.

2. A compound of Formula (II), or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof:

wherein,

RA is hydrogen, deuterium, F, Cl, ‒CN, ‒OR1, ‒SR1, -S(=O)R1, -S(=O)2R1, substituted or unsubstituted C1‒C4 alkyl, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C4 cycloalkyl, or substituted or unsubstituted C2‒C3 heterocycloalkyl;

ring Q is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

X is ‒O-, -S-, or ‒NR3-;

Z is CR2;

Ring G is monocyclic, fused, or spiro C4-C12 heterocycloalkyl;

R1 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C15 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R2 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, or substituted or unsubstituted C1‒C4 haloalkyl; and

R3 is hydrogen, ‒CN, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1-C4 heteroalkyl, -C1-C4 alkylene-OR1, substituted or unsubstituted C3‒C4 cycloalkyl, or substituted or unsubstituted C2‒C3 heterocycloalkyl.

3. A compound of Formula (III), or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof:

wherein,

RA is hydrogen, deuterium, F, Cl, ‒CN, ‒OR1, ‒SR1, -S(=O)R1, -S(=O)2R1, substituted or unsubstituted C1‒C4 alkyl, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4

heteroalkyl, substituted or unsubstituted C3‒C4 cycloalkyl, or substituted or unsubstituted C2‒C3 heterocycloalkyl;

ring Q is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

is a single bond or a double bond;

X is
and Z is C; or

X is
and Z is N or CR2;

Ring G is monocyclic, fused, or spiro C4-C12 heterocycloalkyl;

R1 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C6 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R2 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, or substituted or unsubstituted C1‒C4haloalkyl; and

each R4 is independently hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4haloalkyl, or substituted or unsubstituted C1‒C4 heteroalkyl.

4. A compound of Formula (IV), or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof:


wherein,

each RA is independently hydrogen, deuterium, F, Cl, ‒CN, ‒OR1, ‒SR1, -S(=O)R1, -S(=O)2R1, substituted or unsubstituted C1‒C4 alkyl, substituted or unsubstituted C1‒C4haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C4 cycloalkyl, or substituted or unsubstituted C2‒C3 heterocycloalkyl;

ring Q is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

X is ‒O-, -S-, or ‒NR3-;

Z is CR2;

Ring G is monocyclic, fused, or spiro C4-C12 heterocycloalkyl;

R1 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C6 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R2 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, or substituted or unsubstituted C1‒C4 haloalkyl; and

R3 is hydrogen, ‒CN, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, -C1-C4 alkylene-OR1, substituted or unsubstituted C3‒C4 cycloalkyl, or substituted or unsubstituted C2‒C3 heterocycloalkyl, provided that the compound of Formula (IV) is not:

2-(5-(methyl(2,2,6,6-tetramethylpiperidin-4-yl)amino)pyrazin-2-yl)-5-(1H-pyrazol-4-yl)phenol;

3-amino-1-(4-((5-(2-hydroxy-4-(1H-pyrazol-4-yl)phenyl)pyrazin-2-yl)(methyl)amino)piperidin-1- yl)propan-1-one;

3-amino-1-(4-((5-(2-hydroxy-4-(1H-pyrazol-4-yl)phenyl)pyrazin-2-yl)(methyl)amino)-2,2,6,6- tetramethylpiperidin-1-yl)propan-1-one;

3-amino-1-(4-((5-(2-hydroxy-4-(1H-pyrazol-4-yl)phenyl)pyrazin-2-yl)oxy)-2,2,6,6-tetramethylpiperidin- 1-yl)propan-1-one; or

5-(4-(5-((1-(3-aminopropanoyl)-2,2,6,6-tetramethylpiperidin-4-yl)(methyl)amino)pyrazin-2-yl)-3- hydroxyphenyl)pyrimidin-2(1H)-one.

5. A compound of Formula (V), or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof:


wherein,

each RA is independently hydrogen, deuterium, F, Cl, ‒CN, ‒OR1, ‒SR1, -S(=O)R1, -S(=O)2R1, substituted or unsubstituted C1‒C4 alkyl, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C4 cycloalkyl, or substituted or unsubstituted C2‒C3 heterocycloalkyl;

ring Q is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

is a single bond or a double bond;

X is and Z is C; or


X is
and Z is N or CR2;

Ring G is monocyclic, fused, or spiro C4-C12 heterocycloalkyl;

R1 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C6 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R2, when present, is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, or substituted or unsubstituted C1‒C4haloalkyl; and

each R4 is independently hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4haloalkyl, or substituted or unsubstituted C1‒C4 heteroalkyl.

6. A compound of Formula (VI), or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof:


wherein,

RA is hydrogen, deuterium, F, Cl, ‒CN, ‒OR1, ‒SR1, -S(=O)R1, -S(=O)2R 1, substituted or unsubstituted C1‒C4 alkyl, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C4 cycloalkyl, or substituted or unsubstituted C2‒C3 heterocycloalkyl;

ring Q is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

X is ‒O-, -S-, or ‒NR3-;

Z is CR2;

Ring G is monocyclic, fused, or spiro C4-C12 heterocycloalkyl;

R1 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C6 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R2 is hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, or substituted or unsubstituted C1‒C4 haloalkyl; and

R3 is hydrogen, ‒CN, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, -C1-C4 alkylene-OR1, substituted or unsubstituted C3‒C4 cycloalkyl, or substituted or unsubstituted C2-C3 heterocycloalkyl.

7. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is substituted or unsubstituted aryl.

8. The compound of claim 7, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is 2‒hydroxy‒phenyl substituted with 1, 2, or 3 substituents independently selected from:

deutenum, halogen, -OH, -NO2, -CN, -SR1, -S(=O)R1, -S(=O)2R1, -N(R1)2, -C(=O)R1, -OC(=O)R1, - C(=O)OR1, -C(=O)N(R1)2, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C2- C6 alkenyl, substituted or unsubstituted C2-C6 alkynyl, substituted or unsubstituted C1-C6 alkoxy, substituted or unsubstituted C3-C7 cycloalkyl, substituted or unsubstituted C2-C7 heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; wherein

each R1 is independently hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C6 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

9. The compound of claim 8, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is 2‒hydroxy‒phenyl substituted with substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

10. The compound of claim 9, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is 2‒hydroxy‒phenyl substituted with substituted or unsubstituted aryl, wherein if aryl is substituted then it is substituted with 1 or 2 substituents independently selected from: deutenum, halogen, -OH, -NO2, -CN, ‒SR1, ‒S(=O)R1, ‒S(=O)2R1, ‒N(R1)2. ‒C(=O)R1, ‒OC(=O)R1, ‒

C(=O)OR1, ‒C(=O)N(R1)2, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C2- C6 alkenyl, substituted or unsubstituted C2-C6 alkynyl, substituted or unsubstituted C1-C6 alkoxy, substituted or unsubstituted C3-C7 cycloalkyl, and substituted or unsubstituted C2-C7 heterocycloalkyl; wherein

each R1 is independently hydrogen, deutenum, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C6 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

11. The compound of claim 9, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is 2‒hydroxy‒phenyl substituted with substituted or unsubstituted heteroaryl, wherein if heteroaryl is substituted then it is substituted with 1 or 2 substituents independently selected from:

deutenum, halogen, -OH, -NO2, -CN, ‒SR1, ‒S(=O)R1, ‒S(=O)2R1, ‒N(R1)2. ‒C(=O)R1, ‒OC(=O)R1, ‒ C(=O)OR1, ‒C(=O)N(R1)2, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C2- C6 alkenyl, substituted or unsubstituted C2-C6 alkynyl. substituted or unsubstituted C1-C6 alkoxy, substituted or unsubstituted C3-C7 cycloalkyl, and substituted or unsubstituted C2-C7 heterocycloalkyl; wherein

each R1 is independently hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C6 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

12. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein:

ring Q is
wherein each RQ is independently selected from hydrogen, deuterium,

F, ‒Cl, -CN, ‒OH, -CH3, -CH2CH3, -CH2CH2CH3, -CH(CH3)2, ‒CF3, ‒OCH3, -OCH2CH3, - CH2OCH3, -OCH2CH2CH3, and -OCH(CH3)2; and ring P is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

13. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is substituted or unsubstituted heteroaryl.

14. The compound of claim 13, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is substituted or unsubstituted 5- or 6-membered monocyclic heteroaryl.

15. The compound of claim 14, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is substituted or unsubstituted 6-membered monocyclic heteroaryl.

16. The compound of claim 15, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is 6-membered monocyclic heteroaryl selected from:

ring Q is


wherein each RQ is independently selected from hydrogen, deuterium, ‒F, ‒Cl, -CN, ‒OH, -CH3, -CH2CH3, - CH2CH2CH3, -CH(CH3)2, ‒CF3, -O CH3, -OCH2CH3, -CH2OCH3, -OCH2CH2CH3, and -OCH(CH3)2; and ring P is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

17. The compound of claim 12 or 16, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein each RQ is independently selected from hydrogen, ‒F, ‒Cl, -CN, ‒OH, -CH3,‒ CF3, or ‒OCH3.

18. The compound of claim 12 or 16, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring P is substituted or unsubstituted heteroaryl.

19. The compound of claim 18, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring P is heteroaryl selected from the group consisting of:


wherein,

each RB is independently selected from hydrogen, deuterium, halogen, hydroxy, cyano, substituted or unsubstituted C1-C6 alkyl, -CD3, substituted or unsubstituted C1‒C6 fluoroalkyl. substituted or unsubstituted C2-C6 alkenyl, substituted or unsubstituted C2-C6 alkynyl, substituted or unsubstituted C1-C6alkoxy, deuterium substituted C1-C6alkoxy, -OCD3, substituted or unsubstituted C3‒7 cycloalkyl, substituted or unsubstituted C2‒C7 heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;

RB1 is selected from hydrogen, deuterium, substituted or unsubstituted C1-C6 alkyl, -CD3, substituted or unsubstituted C1‒C6 fluoroalkyl. substituted or unsubstituted C1-C6 heteroalkyl, substituted or unsubstituted C3-7 cycloalkyl, and substituted or unsubstituted C2‒C7 heterocycloalkyl; and

m is 1, 2, or 3.

20. The compound of claim 18, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring P is heteroaryl selected from the group consisting of:


wherein,

each RB is independently selected from hydrogen, deuterium, halogen, hydroxy, cyano, substituted or unsubstituted C1-C6 alkyl, -CD3, substituted or unsubstituted C1‒C6 fluoroalkyl. substituted or unsubstituted C2-C6 alkenyl, substituted or unsubstituted C2-C6 alkynyl, substituted or unsubstituted C1-C6alkoxy, deuterium substituted C1-C6alkoxy, -OCD3, substituted or unsubstituted C3‒7 cycloalkyl, substituted or unsubstituted C2‒C7 heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;

RB1 is selected from hydrogen, deuterium, substituted or unsubstituted C1-C6 alkyl, -CD3, substituted or unsubstituted C1‒C6 fluoroalkyl, substituted or unsubstituted C1-C6 heteroalkyl, substituted or unsubstituted C3‒7 cycloalkyl, and substituted or unsubstituted C2‒C7 heterocycloalkyl; and m is 1, 2, or 3.

21. The compound of claim 19 or 20, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein each RB is independently selected from hydrogen, deuterium, ‒F, ‒Cl, -CN, ‒ CH3, ‒CF3 ‒OH, or ‒OCH3.

22. The compound of claim 21, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein each RB is independently ‒F or ‒OCH3.

23. The compound of claim 19 or 20, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein RB1 is selected from hydrogen, deuterium, ‒CH3, ‒CF3,and ‒CD3.

24. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is 2‒naphthyl substituted at the 3 position with 0, 1, and 2 substituents independently selected from:

deutenum, halogen, -OH, -NO2, -CN, ‒SR1, ‒S(=O)R1, ‒S(=O)2R1, ‒N(R1)2, ‒C(=O)R1, ‒OC(=O)R1, ‒ C(=O)OR1, ‒C(=O)N(R1)2, substituted or unsubstituted C1-C6 alkyl. substituted or unsubstituted C2- C6 alkenyl, substituted or unsubstituted C2-C6 alkynyl. substituted or unsubstituted C1-C6 alkoxy, substituted or unsubstituted C3-C7 cycloalkyl, substituted or unsubstituted C2-C7 heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; wherein

each R1 is independently hydrogen, deuterium, substituted or unsubstituted C1‒C4 alkyl, -CD3, substituted or unsubstituted C1‒C4 haloalkyl, substituted or unsubstituted C1‒C4 heteroalkyl, substituted or unsubstituted C3‒C6 cycloalkyl, substituted or unsubstituted C2‒C5 heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

25. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is selected from the group consisting of:


26. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is selected from the group consisting of:


27. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is selected from the group consisting of:


28. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring Q is selected from the group consisting of:



wherein

RB1 is selected from hydrogen, deuterium, substituted or unsubstituted C1-C6 alkyl. -CD3, substituted or unsubstituted C1‒C6 fluoroalkyl. substituted or unsubstituted C1-C6 heteroalkyl. substituted or unsubstituted C3‒7 cycloalkyl, and substituted or unsubstituted C2‒C7 heterocycloalkyl.

29. The compound of any one of claims 6-28, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring G is:


wherein

each RC is independently selected from H, D, F, -CN, -OH, -OR1, substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted C1-C4 haloalkyl, substituted or unsubstituted C1-C4 heteroalkyl, substituted or unsubstituted C3-C6 cycloalkyl, and substituted or unsubstituted C2-C5 heterocycloalkyl; and q is 3, 4, 5, or 6.

30. The compound of any one of claims 6-28, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring G is:


wherein

each RC is independently selected from H, D, F, -CN, -OH, -OR1, substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted C1-C4 haloalkyl, substituted or unsubstituted C1-C4 heteroalkyl, substituted or unsubstituted C3-C6 cycloalkyl, and substituted or unsubstituted C2-C5 heterocycloalkyl; and q is 2, 3, 4, 5, or 6.

31. The compound of any one of claims 6-28, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring G is:


wherein R is H, D, substituted or unsubstituted C1-C4 alkyl, or substituted or unsubstituted C1-C4 haloalkyl.

32. The compound of any one of claims 6-28, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein ring G is:


wherein

each RC is independently selected from H, D, F, -CN, -OH, -OR1, substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted C1-C4 haloalkyl, substituted or unsubstituted C1-C4 heteroalkyl, substituted or unsubstituted C3-C6 cycloalkyl, and substituted or unsubstituted C2-C5 heterocycloalkyl; and q is 2, 3, 4, 5, or 6.

33. The compound of any one of claims 6-28, or a pharmaceutically acceptable salt or solvate thereof, wherein:

ring G is


or
wherein

each RC is independently selected from H, D, F, -CN, -OH, -OR1, substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted C1-C4 haloalkyl, substituted or unsubstituted C1-C4 heteroalkyl, substituted or unsubstituted C3-C6 cycloalkyl, and substituted or unsubstituted C2-C5 heterocycloalkyl; and q is 3, 4, 5, or 6.

34. The compound of any one of claims 6-28, or a pharmaceutically acceptable salt or solvate thereof, wherein:

ring G is



wherein

each RC is independently selected from H, D, F, -CN, -OH, -OR1, substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted C1-C4 haloalkyl, substituted or unsubstituted C1-C4 heteroalkyl, substituted or unsubstituted C3-C6 cycloalkyl, and substituted or unsubstituted C2-C5 heterocycloalkyl; and q is 2, 3, 4, 5, or 6.

35. The compound of any one of claims 6‒34, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein X is ‒O-.

36. The compound of any one of claims 6‒34, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein X is ‒S-.

37. The compound of any one of claims 6‒34, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein X is ‒NR3-.

38. The compound of claim 37, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein R3 is hydrogen, -CH3, -CH2CH3, -CH(CH3)2, -CH2F, -CHF2, -CF3, cyclopropyl, or oxetanyl.

39. The compound of claim 37, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein R3 is hydrogen, -CH3, -CH2CH3, -CH(CH3)2, -CF3, cyclopropyl, or oxetanyl.

40. The compound of claim 37, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein R3 is hydrogen, -CH3, -CH(CH3)2, cyclopropyl, or oxetanyl.

41. The compound of claim 37, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein R3 is hydrogen, -CH3, or cyclopropyl.

42. The compound of any one of claims 6‒41, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein R2 is hydrogen, -CH3, or -OCH3.

43. The compound of claim 42, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein R2 is hydrogen.

44. The compound of any one of claims 6‒43, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein RA is hydrogen, F, Cl, -CN, -CH3, -CH2CH3, -CH2CH2CH3, - CH(CH3)2, -OH, -OCH3, -OCH2CH3, -OCF3, -CH2F, -CHF2, or -CF3

45. The compound of any one of claims 6‒43, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein RA is hydrogen, F, Cl, -CN, -CH3, -OH, - OCH3, -OCF3, -CH2F, -CHF2, or -CF3.

46. The compound of any one of claims 6‒43, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein RA is hydrogen, F, Cl, -CN, -CH3, or - OCH3.

47. The compound of any one of claims 6‒43, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein RA is hydrogen, F, Cl, or -CH3.

48. The compound of any one of claims 6‒43, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein RA is hydrogen.

49. The compound of claim 6, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, that is:

50. A method of modulating splicing comprising contacting a compound of any one of the preceding claims to cells, wherein the compound modulates splicing at a splice site sequence of a pre-mRNA that encodes a mRNA, wherein the mRNA encodes a target protein or a functional RNA.

51. A method of treating a disease or condition comprising administering a compound of any one of the preceding claims to a subject in need thereof.

52. A compound, or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein the compound is selected from Table 1A, Table 1B, Table 1C, Table 1D, Table 1E, or Table 1F.

53. A pharmaceutical composition comprising a compound of any one of claims 1-52 or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, and a pharmaceutically acceptable excipient or carrier.

54. A method of treating a condition or disease comprising administering a compound of any one of claims 1-49 or 52 or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof to a subject in need thereof.

55. Use of a compound of any one of claims 1-49 or 52 or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof in the manufacture of a medicament for the treatment of a condition or disease.