IP Library Granted Patent US 10,787,430
Granted Patent B2
US 10,787,430 · App. 16/310,258 · Granted Sep 29, 2020

Hemoglobin modifier compounds and uses thereof

Inventors: Bohan Jin (San Diego, CA); Qing Dong (San Diego, CA); Gene Hung (San Diego, CA)
Assignee: FRONTHERA U.S. PHARMACEUTICALS LLC
C07D401/04C07D401/14C07D403/04C07D405/14C07D409/14C07D413/04C07D413/14C07D417/04C07D417/14C07D471/04C07D491/048A61K31/155A61K31/198C07K16/2854
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Quick Facts
Patent No.
US 10,787,430
App. No.
16/310,258
Granted
Sep 29, 2020
Kind
B2
Abstract

Described herein are compounds, including pharmaceutically acceptable salts thereof, methods of making such compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat, prevent or diagnose blood-based diseases, disorders or conditions.

Claims (45)

1. A compound that has the structure of Formula (II), or a pharmaceutically acceptable salt or solvate thereof:

wherein,

R 1 is H or D;

L 1 is X;

X is —O—;

R 2 is H, D, substituted or unsubstituted C 1 -C 6 alkyl, or substituted or unsubstituted C 1 -C 6 deuteroalkyl;

R 3 is D, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 deuteroalkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, or substituted or unsubstituted C 1 -C 6 heteroalkyl;

or R 2 and R 3 together with the carbon that they are attached to form a substituted or unsubstituted C 3 -C 6 cycloalkyl or a substituted or unsubstituted C 2 -C 8 heterocycloalkyl;

or R 3 and R C are taken together with the carbons that they are attached to forma substituted or unsubstituted C 3 -C 6 cycloalkyl or a substituted or unsubstituted C 2 -C 8 heterocycloalkyl;

or R 3 and R A are taken together with the carbons that they are attached to form a substituted or unsubstituted C 3 -C 6 cycloalkyl or a substituted or unsubstituted C 2 -C 8 heterocycloalkyl;

ring A is a phenyl;

ring C is a monocyclic heterocycle or a monocyclic carbocycle;

ring D is a monocyclic 5-membered N-containing heterocycle;

each R A , R C , and R D is independently H, D, halogen, —CN, —OH, —OR 5 , —SR 5 , —S(═O)R 6 , —NO 2 , —N(R 5 ) 2 , —S(═O) 2 R 6 , —NHS(═O) 2 R 6 , —S(═O) 2 N(R) 2 , —C(═O)R 6 , —OC(═O)R 6 , —CO 2 R 5 , —OCO 2 R 6 , —C(═O)N(R) 2 , —OC(═O)N(R) 2 , —NR 5 C(═O)N(R) 2 , —NR 5 C(═O)R 6 , —NR 5 C(═O)OR 6 , substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 deuteroalkyl, substituted or unsubstituted C 2 -C 6 alkenyl, substituted or unsubstituted C 2 -C 6 alkynyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 1 -C 6 heteroalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

each R 5 is independently H, D, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 deuteroalkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

or two R 5 on the same N atom are taken together with the N atom to which they are attached to form a N-containing heterocycloalkyl;

each R 6 is independently substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 deuteroalkyl, substituted or unsubstituted C 1 -C 6 heteroalkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 3 -C 6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

p is 0, 1, 2 or 3;

m is 0, 1, 2 or 3; and

n is 0, 1, 2 or 3.

2. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein:

3. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein:

R 2 is D; and

R 3 is D, substituted or unsubstituted C 1 -C 3 alkyl, substituted or unsubstituted C 1 -C 3 fluoroalkyl, or substituted or unsubstituted C 1 -C 3 heteroalkyl.

4. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate or solvate thereof, wherein:

R 2 and R 3 are each D.

5. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein:

R 2 and R 3 together with the carbon that they are attached to form a substituted or unsubstituted C 3 -C 6 cycloalkyl or a substituted or unsubstituted C 2 -C 8 heterocycloalkyl.

6. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein:

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

ring C is a monocyclic heterocycle with 1-3 N atoms in the ring.

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

9. The compound of claim 1 , wherein the compound of Formula (II) has the structure of Formula (IIa), or a pharmaceutically acceptable salt or solvate thereof:

10. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein:

11. The compound of claim 1 , wherein the compound of Formula (II) has a structure of Formula (IIb), or pharmaceutically acceptable salt or solvate thereof:

12. The compound of claim 1 , wherein the compound of Formula (II) has a structure of Formula (IIc), or pharmaceutically acceptable salt or solvate thereof:

13. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein:

R D is H, D, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 1 -C 6 heteroalkyl.

14. The compound of claim 1 , or the pharmaceutically acceptable salt or solvate thereof, wherein the compound has one of the following structures:

15. A pharmaceutical composition comprising a compound as claimed in claim 1 , or a pharmaceutically acceptable salt or solvate thereof, and at least one pharmaceutically acceptable excipient.

16. A method of treating a disease or condition in a subject comprising administering the compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, to the subject; wherein the disease or condition is associated with oxygen deficiency, a mitochondrial disease, or a hypoxemic pulmonary disorder.

17. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein:

each R A is independently H, D, halogen, or —OH.

18. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof, wherein:

each R C is independently H, D, or halogen.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 2, 2021
From: FRONTHERA U.S. PHARMACEUTICALS LLC
To: SICHUAN HAISCO PHARMACEUTICAL CO., LTD.
Reel/Frame 055809/0009 →
RELEASE OF SECURITY INTEREST Recorded Mar 8, 2021
From: HAISCO PHARMACEUTICAL CO., LIMITED
To: FRONTHERA U.S. PHARMACEUTICALS LLC; FRONTHERA INTERNATIONAL GROUP LIMITED
Reel/Frame 055528/0734 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 12, 2019
From: JIN, BOHAN; DONG, QING; HUNG, GENE
To: FRONTHERA U.S. PHARMACEUTICALS LLC
Reel/Frame 050993/0227 →
SECURITY INTEREST Recorded Aug 6, 2019
From: FRONTHERA U.S. PHARMACEUTICALS LLC; FRONTHERA INTERNATIONAL GROUP LIMITED
To: HAISCO PHARMACEUTICAL CO., LIMITED
Reel/Frame 049977/0645 →
Continuity (2)
Provisional Application 62351708 · Jun 17, 2016
Related Publication 20190330181A1 · Oct 31, 2019