IP Library Granted Patent US 11,773,110
Granted Patent B2
US 11,773,110 · App. 17/513,093 · Granted Oct 3, 2023

Heterocycle amines and uses thereof

Inventors: Koc-Kan Ho (Salt Lake City, UT); David Diller (East Windsor, NJ); Jeffrey J. Letourneau (East Windsor, NJ); Brian F. McGuinness (Plainsboro, NJ); Andrew G. Cole (Robbinsville, NJ); David Rosen (Kendall Park, NJ); Cornelis A. van Oeveren (San Diego, CA); Jason C. Pickens (San Diego, CA); Lin Zhi (San Diego, CA); Yixing Shen (Encinitas, CA); Bijan Pedram (San Diego, CA)
Assignee: LIGAND PHARMACEUTICALS INCORPORATED
C07D513/04A61K31/407A61K31/4168A61K31/4353A61P29/00A61P37/00C07D235/02C07D269/02C07D277/42C07D277/60C07D417/12C07D417/14C07D471/04
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 11,773,110
App. No.
17/513,093
Granted
Oct 3, 2023
Kind
B2
Abstract

Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.

Claims (22)

1. A method of preparing a compound of Formula (IV):

wherein:

X is N;

R 1 is selected from hydrogen, halogen, OR 6 , CN, NR 7 R 8 , CH 2 OR 6 , CH 2 NR 7 R 8 , an optionally substituted C 1 -C 6 alkyl, an optionally substituted C 1 -C 6 haloalkyl, an optionally substituted C 1 -C 6 alkenyl, an optionally substituted C 1 -C 6 alkynyl, CO 2 R 6 , CONR 7 R 8 , SO 3 R 6 , and SO 2 NR 7 R 8 ;

R 2 , R 3 and R 5 are each hydrogen;

R 4 is selected from halogen, OR 6 , CN, NR 7 R 8 , CH 2 OR 6 , an optionally substituted aryl, an optionally substituted three to nine membered heteroaryl, an optionally substituted three to nine membered non-aromatic ring, an optionally substituted three to nine membered carbocycle, an optionally substituted C 1 -C 6 alkyl, an optionally substituted C 1 -C 6 haloalkyl, an optionally substituted C 1 -C 6 alkenyl, an optionally substituted C 1 -C 6 alkynyl, CO 2 R 6 , SO 3 R 6 , SO 2 R 6 and SO 2 NR 7 R 8 ;

each R 6 is independently selected from an optionally substituted aryl, an optionally substituted three to nine membered heteroaryl, and an optionally substituted three to nine membered non-aromatic ring, each optionally fused with a substituted aryl or a substituted three to nine membered heteroaryl, hydrogen, an optionally substituted C 1 -C 10 alkyl;

each R 7 and R 8 is independently selected from an optionally substituted aryl, an optionally substituted three to nine membered heteroaryl, an optionally substituted three to nine membered non-aromatic ring, each optionally fused with a substituted aryl or a substituted three to nine membered heteroaryl, hydrogen, an optionally substituted C 1 -C 10 alkyl, an optionally substituted C 1 -C 10 haloalkyl, an optionally substituted C 1 -C 10 alkenyl, and an optionally substituted C 1 -C 10 alkynyl, or R 7 and R 8 are linked to form an optionally substituted three to nine membered non-aromatic ring; and

each optionally substituted group is either unsubstituted or substituted with one or more groups independently selected from alkyl, alkenyl, alkynyl, haloalkyl, heterohaloalkyl, aryl, arylalkyl, three to nine membered heteroaryl, three to nine membered non-aromatic ring, hydroxy, alkoxy, aryloxy, mercapto, alkylthio, arylthio, cyano, halo, —C(═O)R, —C(═S)R, —O(C═O)NR 2 , ROC(═O)NH—, —O(C═S)NR 2 , ROC(═S)NH—, —(C═O)NR 2 , RC(═O)NH—, —S(═O) 2 NR, RS(═O) 2 NH—, —C(═O)OR, RC(═O)O isocyanato, thiocyanato, isothiocyanato, nitro, silyl, trihalomethanesulfonyl, ═O, ═S, and amino, wherein each R is independently selected from the group consisting of alkyl, cycloalkyl, aryl, three to nine membered heteroaryl, and three to nine membered non-aromatic ring; wherein the method comprises:

coupling a 2-halopyridine with an aminoimidazopyridine.

2. The method of claim 1 , wherein the 2-halopyridine has the structure:

and

the aminoimidazopyridine has the structure:

3. The method of claim 1 , wherein the coupling is performed in the presence of a palladium catalyst and a base.

4. The method of claim 1 , wherein R 1 is NR 7 R 8 , CH 2 NR 7 R 8 , or an optionally substituted C 1 -C 6 alkyl.

5. The method of claim 4 , wherein R 1 is selected from NR 7 R 8 , or CH 2 NR 7 R 8 .

6. The method of claim 1 , wherein R 4 is selected from an optionally substituted heteroaryl selected from C 3 -C 6 cycloalkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, and an optionally substituted heteroaryl selected from pyridine, pyrazole, pyridazine, pyrimidine, wherein the heteroaryl is optionally substituted with 1-2 substituents selected from C 1 -C 6 alkyl and CN.

7. The method of claim 1 , wherein R 4 is selected from cyano, triazolyl, oxazolyl, isoxazolyl, imidazoyl, pyridyl, pyrazolyl, pyrimidinyl, pyridazinyl, and C 1 -C 6 alkyl.

8. The method of claim 7 , wherein R 4 is selected from pyridyl, pyrazolyl, pyrimidinyl, and pyridazinyl.

9. The method of claim 8 , wherein R 4 is selected from pyridyl and pyrazolyl.

10. The method of claim 9 , wherein R 4 is pyrazolyl.

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

Assignments (2)
SECURITY INTEREST Recorded Oct 18, 2023
From: CYDEX PHARMACEUTICALS, INC.; LIGAND PHARMACEUTICALS INCORPORATED; METABASIS THERAPEUTICS, INC.; PFENEX INC.
To: CITIBANK, N.A., AS ADMINISTRATIVE AGENT
Reel/Frame 065271/0025 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 29, 2021
From: HO, KOC-KAN; DILLER, DAVID; LETOURNEAU, JEFFREY J; MCGUINNESS, BRIAN F; COLE, ANDREW G; ROSEN, DAVID; VAN OEVEREN, CORNELIS A; PICKENS, JASON C; ZHI, LIN; SHEN, YIXING; PEDRAM, BIJAN
To: LIGAND PHARMACEUTICALS INCORPORATED
Reel/Frame 057963/0204 →
Continuity (7)
Continuation 16735988 · Jan 7, 2020
Continuation 16015925 · Jun 22, 2018
Continuation 15006940 · Jan 26, 2016
Continuation 14137318 · Dec 20, 2013
Continuation 13885138
Provisional Application 61415685 · Nov 19, 2010
Related Publication 20220119413A1 · Apr 21, 2022