IP Library Granted Patent US 11,912,687
Granted Patent B2
US 11,912,687 · App. 17/466,480 · Granted Feb 27, 2024

3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof

Inventors: Kenneth A. Witt (Edwardsville, IL); Albert M. Crider (Maryville, IL); William Neumann (St. Louis, MO); Audrey Hospital (Robbinsville, NJ); Karin Sandoval (Edwardsville, IL); Maria Kontoyianni (Glen Carbon, IL)
Assignee: Board of Trustees of the Southern Illinois University
C07D403/14C07D401/14C07D403/06
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 11,912,687
App. No.
17/466,480
Granted
Feb 27, 2024
Kind
B2
Abstract

The present disclosure describes novel compounds that are somatostatin receptor type 4 agonists. The present disclosure is also directed to a compound of Formula (II):

Claims (33)

1. A compound of Formula (II):

wherein

are independently a single bond or is absent;

A is C(H) or N;

B and C are independent C(H), N, N(H), O, or S, provided that when B or C is C(H) or N, is a single bond, and when B or C is N(H), O, or S, is absent;

D is S, O, NR 16 , P, sulfone, or sulfoxide, wherein R 16 is hydrogen, C 1 -C 6 alkyl, aryl, or benzyl;

R 1 and R 7 are independently hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted cycloalkyl or substituted or unsubstituted fused ring system;

R 2 is substituted or unsubstituted C 1 -C 6 alkyl;

R 3 , R 4 , and R 5 are independently hydrogen, F, Cl, Br, I, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted amine, thiosulfinate, thiosulfonate, thioamide, sulfimide, sulfoximide, sulfonediimine, or sulfur halide;

R 6 and R 8 are independently hydrogen, F, Cl, Br, I, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted cycloalkyl; and

R 9 and R 15 are independently substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted cycloalkyl;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein are each a single bond and A, B, and C are N.

3. The compound of claim 1 , wherein D is S, sulfone, or sulfoxide.

4. The compound of claim 1 , wherein R 9 is substituted or unsubstituted C 1 -C 3 alkyl.

5. The compound of claim 1 , wherein R 15 is unsubstituted C 1 -C 3 alkyl.

6. The compound of claim 1 , wherein R 6 and R 8 are independently hydrogen or substituted or unsubstituted C 1 -C 3 alkyl.

7. The compound of claim 1 , wherein R 1 and R 7 are independently substituted or unsubstituted aryl or a substituted or unsubstituted fused ring system.

8. The compound of claim 7 , wherein R 1 is a substituted or unsubstituted fused ring system.

9. The compound of claim 8 , wherein R 1 is substituted or unsubstituted indole, substituted or unsubstituted naphthalene, or substituted or unsubstituted quinolone.

10. The compound of claim 7 , wherein R 7 is substituted or unsubstituted aryl or substituted or unsubstituted indole.

11. The compound of claim 10 , wherein R 7 is

and R 10 , R 11 , R 12 , R 13 and R 14 are independently hydrogen, F, Cl, Br, I, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted amine, thiosulfinate, thiosulfonate, thioamide, sulfimide, sulfoximide, sulfonediimine, or sulfur halide.

12. The compound of claim 10 , wherein R 7 is

and R 10 , R 11 , R 12 , R 13 , and R 14 are independently hydrogen, F, Cl, Br, I, CF 3 , OCH 3 , NO 2 , OCH 2 (C 6 H 4 ), C 6 H 4 , SO 2 CH 3 , or OCF 3 .

13. The compound of claim 1 , wherein R 2 is substituted or unsubstituted C 1 -C 3 alkyl.

14. The compound of claim 1 , wherein R 3 , R 4 , and R 5 are independently hydrogen, F, Cl, Br, I, or substituted or unsubstituted alkyl.

15. The compound of claim 14 , wherein R 3 , R 4 , and R 5 are hydrogen.

16. The compound of claim 1 , wherein R 15 is unsubstituted C 1 -C 6 alkyl.

17. The compound of claim 1 , wherein the compound is selected from the group consisting of:

18. The compound of claim 1 , wherein the compound is selected from the group consisting of:

19. A method for the treatment of pain or inflammation which comprises administering to a subject in need thereof a therapeutically effective amount of a compound according to claim 1 .

20. A pharmaceutical composition containing a compound according to claim 1 and a pharmaceutically acceptable carrier.

Assignments (3)
CONFIRMATORY LICENSE Recorded Aug 16, 2023
From: SOUTHERN ILLINOIS UNIV AT EDWARDSVILLE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 064602/0835 →
CONFIRMATORY LICENSE Recorded May 23, 2023
From: SOUTHERN ILLINOIS UNIVERSITY EDWARDSVILLE
To: NATIONAL INSTITUTES OF HEALTH
Reel/Frame 063727/0570 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 3, 2021
From: WITT, KENNETH A.; CRIDER, ALBERT M.; NEUMANN, WILLIAM; HOSPITAL, AUDREY; SANDOVAL, KARIN; KONTOYIANNI, MARIA
To: BOARD OF TRUSTEES OF SOUTHERN ILLINOIS UNIVERSITY
Reel/Frame 057383/0841 →
Continuity (3)
Continuation In Part 16613086
Provisional Application 62505384 · May 12, 2017
Related Publication 20220002274A1 · Jan 6, 2022