IP Library › Granted Patent US 12,503,422
Granted Patent B2
US 12,503,422 · App. 17/583,081 · Granted Dec 23, 2025

Gemcabene, pharmaceutically acceptable salts thereof, compositions thereof and methods of use therefor

Inventors: Daniela Carmen Oniciu (Gainesville, FL); Charles Larry Bisgaier (Ann Arbor, MI); José Rui Gomes (Basel, CH); Stefan Heckhoff (Loerrach, DE)
Assignee: NeuroBo Pharmaceuticals, Inc.
C07C62/08A61K9/2018A61K9/2054A61K31/194C07C51/43C07C51/47C07C59/305
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Quick Facts
Patent No.
US 12,503,422
App. No.
17/583,081
Granted
Dec 23, 2025
Kind
B2
Abstract

This present invention provides gemcabene pharmaceutically acceptable salts having a PSD90 of 35 μm to about 90 μm, methods for purifying crude gemcabene, pharmaceutically acceptable salts of purified gemcabene, pharmaceutical compositions of a gemcabene pharmaceutically acceptable salt and therapeutic and prophylactic methods useful for various conditions, including dyslipidemia.

Claims (8)

1 . A pharmaceutically acceptable salt of gemcabene, the pharmaceutically acceptable salt having a PSD90 ranging from 40 μm to about 75 μm as measured by laser light diffraction and providing a plasma gemcabene AUC (0-24) ranging from about 200 μg·hr/mL at steady state to about 6000 μg·hr/mL at steady state when administered to a human subject at a dose of about 50 mg to about 900 mg.

2 . The pharmaceutically acceptable salt of claim 1 , wherein the pharmaceutically acceptable salt has a dissolution profile characterized by a % dissolution value of (1) at least 80% in pH 5.0 potassium acetate buffer at 37° C.±5° C. in no more than 45 minutes as measured by high-performance liquid chromatography using a detection wavelength of 210 nm or (2) at least 70% in pH 5.0 potassium acetate buffer at 37° C.±5° C. in no more than 30 minutes as measured by high-performance liquid chromatography using a detection wavelength of 210 nm.

3 . The pharmaceutically acceptable salt of claim 1 , wherein the pharmaceutically acceptable salt is a calcium salt.

4 . A pharmaceutically acceptable salt of gemcabene, the pharmaceutically acceptable salt having a PSD90 ranging from 40 μm to about 75 μm as measured by laser light diffraction and providing a plasma gemcabene AUC last ranging from about 50 μg·hr/mL to about 7500 μg·hr/mL after a single dose administration of about 50 mg to about 900 mg to a human subject.

5 . The pharmaceutically acceptable salt of claim 4 , wherein the pharmaceutically acceptable salt has a dissolution profile characterized by a % dissolution value of (1) at least 80% in pH 5.0 potassium acetate buffer at 37° C.±5° C. in no more than 45 minutes as measured by high-performance liquid chromatography using a detection wavelength of 210 nm or (2) at least 70% in pH 5.0 potassium acetate buffer at 37° C.±5° C. in no more than 30 minutes as measured by high-performance liquid chromatography using a detection wavelength of 210 nm.

6 . The pharmaceutically acceptable salt of claim 4 , wherein the pharmaceutically acceptable salt is a calcium salt.

7 . A composition comprising an effective amount of the pharmaceutically acceptable salt of claim 1 and a pharmaceutically acceptable carrier or vehicle.

8 . A composition comprising an effective amount of the pharmaceutically acceptable salt of claim 4 and a pharmaceutically acceptable carrier or vehicle.

Continuity (7)
Continuation 16402853 · May 3, 2019
Continuation 15956172 · Apr 18, 2018
Provisional Application 62584576 · Nov 10, 2017
Provisional Application 62569358 · Oct 6, 2017
Provisional Application 62486728 · Apr 18, 2017
Provisional Application 62486822 · Apr 18, 2017
Related Publication 20220332672A1 · Oct 20, 2022
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