IP Library Granted Patent US 11,021,460
Granted Patent B2
US 11,021,460 · App. 16/577,946 · Granted Jun 1, 2021

Compositions comprising methylphenidate-prodrugs, processes of making and using the same

Inventors: Travis Mickle (Kissimmee, FL); Sven Guenther (Coralville, IA); Guochen Chi (Coralville, IA)
Assignee: KemPharm, Inc.
C07D401/12A61K9/0053A61K31/4458A61K31/4545A61K47/545C07D211/34
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Quick Facts
Patent No.
US 11,021,460
App. No.
16/577,946
Granted
Jun 1, 2021
Kind
B2
Abstract

The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate. The pharmaceutical kit may comprise a specified amount of individual doses in a package. Each individual dose in the package may contain a pharmaceutically effective amount of a conjugate of d-threo methylphenidate.

Claims (14)

1. A method of providing a stimulant based treatment modality and dosage form for an eating disorder or a binge eating disorder, wherein the method comprises administering a composition comprising a compound to a subject in need thereof, wherein the compound is a conjugate of d-methylphenidate having the following chemical formula:

salts thereof, or mixtures thereof.

2. The method of claim 1 , wherein the salt of the compound is at least one pharmaceutically or therapeutically acceptable salt form or salt mixture thereof.

3. The method of claim 2 , wherein the at least one pharmaceutically or therapeutically acceptable salt form is independently selected from the group consisting of acetate, l-aspartate, besylate, bicarbonate, carbonate, d-camsylate, l-camsylate, citrate, edisylate, formate, fumarate, gluconate, hydrobromide/bromide, hydrochloride/chloride, d-lactate, l-lactate, d,l-lactate, d,l-malate, l-malate, mesylate, pamoate, phosphate, succinate, sulfate, bisulfate, d-tartrate, martrate, d,l-tartrate, meso-tartrate, benzoate, gluceptate, d-glucuronate, hybenzate, isethionate, malonate, methylsulfate, 2-napsylate, nicotinate, nitrate, orotate, stearate, tosylate, thiocyanate, acefyllinate, aceturate, aminosalicylate, ascorbate, borate, butyrate, camphorate, camphocarbonate, decanoate, hexanoate, cholate, cypionate, dichloroacetate, edentate, ethyl sulfate, furate, fusidate, galactarate, galacturonate, gallate, gentisate, glutamate, glutarate, glycerophosphate, heptanoate, hydroxybenzoate, hippurate, phenylpropionate, iodide, xinafoate, lactobionate, laurate, maleate, mandelate, methanesulfonate, myristate, napadisilate, oleate, oxalate, palmitate, picrate, pivalate, propionate, pyrophosphate, salicylate, salicylsulfate, sulfosalicylate, tannate, terephthalate, thiosalicylate, tribrophenate, valerate, valproate, adipate, 4-acetamidobenzoate, camsylate, octanoate, estolate, esylate, glycolate, thiocyanate, and undecylenate.

4. The method of claim 2 , wherein the at least one pharmaceutically or therapeutically acceptable salt form of the compound is independently selected from the group consisting of chloride, hydrochloride, hydrogen carbonate (bicarbonate), iodide, bromide, citrate, acetate, formate, salicylate, hydrogen sulfate (bisulfate), hydroxide, nitrate, hydrogen sulfite (bisulfite), propionate, benzene sulfonate, hypophosphite, phosphate, bromate, iodate, chlorate, fluoride, and nitrite.

5. The method of claim 1 , wherein the composition is in a dosage form selected from the group consisting of a sublingual, a gummy, a chewable tablet, a rapidly dissolving tablet, a tablet, a capsule, a caplet, a troche, a lozenge, an oral powder, a solution, a thin strip, an oral thin film (OTF), an oral strip, a rectal film, a syrup, a suspension, and a suppository.

6. The method of claim 5 , wherein the dosage form is administered orally.

7. The method of claim 5 , wherein the composition has a dosing regimen that is selected from the group consisting of about four times a day or less, about three times a day or less, about two times a day or less, and about one time a day.

8. The method of claim 7 , wherein the composition has a dosing regimen that is about one time a day.

9. The method of claim 1 , wherein the composition provides a dose amount that is the molar equivalent to a dose from about 0.1 mg to about 500 mg d-methylphenidate hydrochloride per dose.

10. The method of claim 1 , wherein the composition is provided in a unit dose form, blister pack, roll, or bulk bottle.

11. The method of claim 10 , wherein the unit dose form provides an amount of d-methylphenidate that is molar equivalent to about 0.5 mg to about 500 mg d-methylphenidate hydrochloride.

12. The method of claim 1 , wherein the composition further comprises one or more excipients or one or more additional pharmaceutically active ingredients.

13. The method of claim 12 , wherein the excipients are selected from the group consisting of antiadherents, binders, coatings, disintegrants, gel forming agents, fillers, flavors and colors, glidants, lubricants, preservatives, sorbents and sweeteners.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2026
From: ZEVRA THERAPEUTICS, INC.
To: COMMAVE THERAPEUTICS SA
Reel/Frame 074195/0008 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 25, 2026
From: ZEVRA THERAPEUTICS, INC.
To: COMMAVE THERAPEUTICS SA
Reel/Frame 074186/0531 →
RELEASE OF SECURITY INTEREST Recorded Mar 13, 2026
From: ALTER DOMUS (US) LLC
To: ZEVRA THERAPEUTICS, INC.
Reel/Frame 075080/0907 →
SECURITY INTEREST Recorded Apr 8, 2024
From: ZEVRA THERAPEUTICS, INC.
To: ALTER DOMUS (US) LLC
Reel/Frame 067040/0637 →
CHANGE OF NAME Recorded Feb 26, 2024
From: KEMPHARM, INC.
To: ZEVRA THERAPEUTICS, INC.
Reel/Frame 066679/0668 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 23, 2020
From: MICKLE, TRAVIS; GUENTHER, SVEN; CHI, GUOCHEN
To: KEMPHARM, INC.
Reel/Frame 053863/0418 →
Continuity (9)
Continuation 16577876 · Sep 20, 2019
Continuation 16431468 · Jun 4, 2019
Continuation 16431422 · Jun 4, 2019
Continuation 16431275 · Jun 4, 2019
Continuation PCTUS2017065482 · Dec 9, 2017
Provisional Application 62541695 · Aug 5, 2017
Provisional Application 62519627 · Jun 14, 2017
Provisional Application 62432675 · Dec 11, 2016
Related Publication 20200016273A1 · Jan 16, 2020