IP Library › Granted Patent US 12,268,660
Granted Patent B2
US 12,268,660 · App. 17/257,458 · Granted Apr 8, 2025

Oral pharmaceutical formulations of bitter compounds for pulmonary hypertension

Inventors: Tien-Li Lee (San Diego, CA); Zhenhuan Zheng (San Diego, CA)
Assignee: Aardvark Therapeutics Inc.
A61K31/216A61K31/167A61K45/06A61P9/12
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Quick Facts
Patent No.
US 12,268,660
App. No.
17/257,458
Granted
Apr 8, 2025
Kind
B2
Abstract

There is disclosed an oral pharmaceutical formulation of bitter compounds that are agonists of TAS2R receptors for the treatment of pulmonary hypertension (PAH). More specifically, there is disclosed a PAH oral formulation comprising a bitter agent selected from the group consisting of 3-caffeoylquinic-1,5-lactone (3-CQL), chlorogenic acid (CGA), denatonium benzoate (DB), denatonium chloride (DC), denatonium saccharide (DS), denatonium acetate (DA), and combinations thereof and a PDE-5 inhibitor.

Claims (9)

1. A method for treating pulmonary arterial hypertension (PAH) with an orally administered therapeutic formulation comprising a bitter agent selected from the group consisting of denatonium acetate (DA), denatonium citrate (DC), denatonium maleate (DM), and 3-caffeoylquinic-1,5-lactone (3-CQL).

2. The method for treating PAH with an orally administered therapeutic formulation of claim 1 , further comprising a PDE-5 inhibitor.

3. The method for treating PAH with an orally administered therapeutic formulation of claim 2 , wherein the PDE-5 inhibitor is selected from the group consisting of sildenafil, tadalafil, vardenafil, zaprinast, udenafil, microdenafil, lodenafil, and avanafil.

4. The method for treating PAH with an orally administered therapeutic formulation of claim 3 , wherein the PDE-5 inhibitor is sildenafil as an oral daily dose of from about 10 mg to about 100 mg administered once or twice daily.

5. The method for treating PAH with an orally administered therapeutic formulation of claim 1 , wherein the bitter agent is DA.

6. The method for treating PAH with an orally administered therapeutic formulation of claim 5 , wherein the daily dosage of DA for an adult is from about 10 mg to about 400 mg.

7. The method for treating PAH with an orally administered therapeutic formulation of claim 6 , wherein the daily dosage of DA for an adult is from about 10 mg to about 200 mg.

8. The method for treating PAH with an orally administered therapeutic formulation of claim 1 , wherein the daily dosage of DA for an adult is from about 10 mg to about 100 mg.

9. The method for treating PAH with an orally administered therapeutic formulation of claim 8 , wherein the daily dosage of 3-CQL or CGA for an adult is from about 10 mg to about 5000 mg.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 31, 2020
From: LEE, TIEN-LI
To: AARDVARK THERAPEUTICS INC
Reel/Frame 054787/0251 →
Continuity (2)
Provisional Application 62696528 · Jul 11, 2018
Related Publication 20210260013A1 · Aug 26, 2021
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