IP Library Granted Patent US 10,851,058
Granted Patent B2
US 10,851,058 · App. 15/740,437 · Granted Dec 1, 2020

Histone deacetylase inhibitors

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Quick Facts
Patent No.
US 10,851,058
App. No.
15/740,437
Granted
Dec 1, 2020
Kind
B2
Abstract

Provided herein are compounds and methods for inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

Claims (41)

1. A compound having a structure of formula (I), or a pharmaceutically acceptable salt thereof

wherein

ring A is a 4-7 membered saturated heterocycle containing one nitrogen ring atom or a 7-9 membered saturated bicyclic heterocycle containing one nitrogen ring atom;

Z is O, NR 3 , S, SO, or SO 2 ;

R 1 is H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C(O)C 1-6 alkyl, C 0-3 alkylene-C 3-10 cycloalkyl, or saturated C 0-3 alkylene-C 2-5 heterocycle having 1 or 2 heteroatoms selected from O, S, N, and N(C 1-4 alkyl);

R 2 is H, F, Cl, or CH 3 ;

R 3 is H, C 1-6 alkyl, C 1-6 haloalkyl, C 0-3 alkylene-C 3-7 cycloalkyl, C(O)C 1-6 -alkyl, or C(O)C 0-3 alkylene-C 3-7 cycloalkyl; and

R 4 is H or C 1-3 alkyl.

2. The compound of claim 1 , wherein ring A is a 4-7 membered saturated heterocycle containing one nitrogen ring atom or a 7-9 membered bicyclic saturated heterocycle containing one nitrogen ring atom; Z is O, NR 3 , S, or SO 2 ; R 1 is C 1-6 alkyl, C 1-6 hydroxyalkyl, or C 0-3 alkylene-C 3-7 cycloalkyl; R 2 is H, F, Cl, or CH 3 ; R 3 is H, C 1-6 -alkyl, C 1-6 haloalkyl, C 0-3 alkylene-C 3-7 cycloalkyl, C(O)C 1-6 -alkyl, or C(O)C 0-3 alkylene-C 3-7 cycloalkyl; and R 4 is H or C 1-3 alkyl.

3. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 1 is H, C 1-6 -alkyl, C 1-6 hydroxyalkyl, C 0-3 alkylene-C 3-10 cycloalkyl, or saturated C 0-3 alkylene-C 2-5 heterocycle having 1 or 2 heteroatoms selected from O, S, N, and N(C 1-4 alkyl).

4. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 1 is C 1-6 alkyl, C 1-6 hydroxyalkyl, or C 0-3 alkylene-C 3-10 cycloalkyl.

5. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 1 is methyl, isopropyl, sec-butyl, CH 2 C(CH 3 ) 3 , or

6. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 1 is cyclopropyl, cyclobutyl, cyclohexyl, adamantanyl, CH 2 cyclopropyl, (1-methylcyclopropyl)methyl, CH 2 cyclobutyl, CH 2 cyclohexyl, CH 2 -adamantanyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, or morpholinyl.

7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof,

wherein

ring A is selected from the group consisting of:

Z is O, NR 3 , S, SO, or SO 2 ;

R 1 is selected from the group consisting of H, CH 3 , C(O)CH 3 ,

R 2 is H, F, Cl, or CH 3 ;

R 3 is H, C 1-6 -alkyl, C 1-6 haloalkyl, C 0-3 alkylene-C 3-7 cycloalkyl, C(O)C 1-6 -alkyl, or C(O)C 0-3 alkylene-C 3-7 cycloalkyl; and

R 4 is H or C 1-3 alkyl.

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof,

wherein ring A is selected from the group consisting of

Z is O, NR 3 , S, SO, or SO 2 ; R 1 is selected from the group consisting of H, CH 3 , C(O)CH 3 ,

and R 3 is H, C 1-6 -alkyl, C 1-6 haloalkyl, C 0-3 alkylene-C 3-7 cycloalkyl, C(O)C 1-6 alkyl, or C(O)C 0-3 alkylene-C 3-7 cycloalkyl.

9. The compound or pharmaceutically acceptable salt of claim 1 , wherein ring A is selected from the group consisting of

10. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 2 is H.

11. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 1 is selected from the group consisting of

12. The compound or pharmaceutically acceptable salt of claim 1 , wherein ring A is selected from the group consisting of

Z is O or NR 3 ; and R 1 is selected from the group consisting of

13. The compound of claim 1 , wherein the compound of formula (I) is a compound of formula (III), or a pharmaceutically acceptable salt thereof

wherein Z is O, NR 3 , S, SO, or SO 2 ; R 1 is selected from the group consisting of

R 2 is H, F, Cl, or CH 3 ; R 3 is H, C 1-6 -alkyl, C 1-6 haloalkyl, C 0-3 alkylene-C 3-7 cycloalkyl, C(O)C 1-6 -alkyl, or C(O)C 0-3 alkylene-C 3-7 cycloalkyl; and R 4 is H or C 1-3 alkyl.

14. The compound or pharmaceutically acceptable salt of claim 1 , wherein Z is O, NR 3 , S, or SO 2 ; and R 1 is selected from the group consisting of

15. The compound of claim 1 having a structure selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

16. The compound of claim 1 selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

17. A pharmaceutical composition comprising the compound of claim 1 , or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

18. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

Assignments (2)
SECURITY INTEREST Recorded Apr 27, 2026
From: BIOMARIN PHARMACEUTICAL INC.; AMICUS THERAPEUTICS, INC.
To: CITIBANK, N.A., AS COLLATERAL AGENT
Reel/Frame 075493/0968 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 29, 2017
From: BHAGWAT, SHRIPAD; LUEDTKE, GREGORY; BRIDGES, ALEXANDER J.
To: BIOMARIN PHARMACEUTICAL INC.
Reel/Frame 044505/0001 →