IP Library › Granted Patent US 12,162,820
Granted Patent B2
US 12,162,820 · App. 17/442,296 · Granted Dec 10, 2024

Peripheral alkyl and alkenyl chains extended benzene derivatives and pharmaceutical composition including the same

Inventors: Syaulan S. Yang (Zhubei, TW); Yan-feng Jiang (Kaohsiung, TW); Meng-hsien Liu (Toufen, TW); Chia-hao Chang (New Taipei, TW); Hao Shiuan Liu (Taichung, TW); Ying-chu Shih (Zhubei, TW); Sheng Hung Liu (Zhubei, TW); Chiung Wen Wang (Zhubei, TW); Ting-ni Huang (Taipei, TW)
Assignee: TAIWANJ PHARMACEUTICALS CO., LTD.
C07C233/42C07C235/38C07C259/06C07C311/20C07D209/14C07D233/74
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Quick Facts
Patent No.
US 12,162,820
App. No.
17/442,296
Granted
Dec 10, 2024
Kind
B2
Abstract

The compounds represented by Formula (I), which are peripheral alkyl and alkenyl chains extended benzene derivatives, are useful as dual autotaxin (ATX)/histone deacetylase (HD AC) inhibitors. These compounds may be included in a pharmaceutical composition along with a pharmaceutically acceptable carrier, and be used in a therapeutically effective amount for prophylaxis or treatment of various diseases and disorders.

Claims (67)

1. A compound selected from the group consisting of the compounds delineated in Table A or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof:

TABLE A

(No.)

Structure

 4

 5

 6

 7

 8

 9

10

11

12

13

14

66

67

68

71

72

73

74

75

78

79

80

81

82

83

2. The compound according to claim 1 , wherein the compound is a dual autotaxin/HDAC inhibitor.

3. A pharmaceutical composition comprising a therapeutically effective amount of the compound according to claim 1 and a pharmaceutically acceptable carrier.

4. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

5. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

6. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

7. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

8. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

9. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

10. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

11. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

12. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

13. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

14. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

15. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

16. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

17. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

18. The compound according to claim 1 , wherein the compound

is or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

19. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

20. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

21. The compound according to claim 1 , wherein the compound is

or a geometric isomer, enantiomer, diastereomer, racemate, pharmaceutically acceptable salt or solvate thereof.

Assignments (2)
CONFIRMATORY LICENSE Recorded Dec 13, 2023
From: COLD SPRING HARBOR LABORATORY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 065968/0306 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 23, 2021
From: YANG, SYAULAN S.; JIANG, YAN-FENG; LIU, MENG-HSIEN; CHANG, CHIA-HAO; LIU, HAO SHIUAN; SHIH, YING-CHU; LIU, SHENG HUNG; WANG, CHIUNG WEN; HUANG, TING-NI
To: TAIWANJ PHARMACEUTICALS CO., LTD.
Reel/Frame 057580/0861 →
Continuity (2)
Provisional Application 62825977 · Mar 29, 2019
Related Publication 20220153687A1 · May 19, 2022