IP Library Granted Patent US 12,251,445
Granted Patent B2
US 12,251,445 · App. 18/303,226 · Granted Mar 18, 2025

Gamma-hydroxybutyrate delivering compounds and processes for making and using them

Inventors: Sanjib Bera (Blacksburg, VA); Sven Guenther (Coralville, IA); Adam Smith (Orlando, FL); Travis Mickle (Kissimmee, FL)
A61K47/542A61K45/06A61P25/20C07C69/14C07C69/88C07C69/96C07C233/47C07C271/64C07C271/66C07C301/00C07C307/02C07C307/06C07C333/10C07D307/20C07D407/12C07F9/09C07F9/2404C07F9/2458A61K9/0048
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Quick Facts
Patent No.
US 12,251,445
App. No.
18/303,226
Granted
Mar 18, 2025
Kind
B2
Abstract

Disclosed are one or more compounds comprising chemically modified gamma-hydroxybutyrate (GHB), 2-hydroxytetrahydrofuran, and/or 1,4-butanediol, and salts of such compounds (GHB delivering compounds and salts thereof). Also disclosed are compositions comprising at least one GHB delivering compound, or a salt thereof, methods of making such compounds, and methods of using such GHB delivering compounds and compositions. Methods of treatment using the compounds are also disclosed.

Claims (20)

1. A compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

2. A composition comprising the compound claim 1 , or a pharmaceutically acceptable salt of the compound, wherein the pharmaceutically acceptable salt is selected from the group consisting of an 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, L-tartrate, 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, undecylenate, sodium, potassium, calcium, magnesium, zinc, aluminum, lithium, cholinate, lysinium, ammonium, troethamine, and a mixture thereof.

3. A method of preventing or treating a sleep disorder or sleep syndrome in a subject in need thereof, comprising administering to the subject a composition comprising the composition of claim 2 .

4. The method of claim 3 , wherein the sleep disorder is a symptom of a degenerative neurological disease or disorder and/or is a side effect of treating a degenerative neurological disease or disorder with medication or a therapeutic compound, wherein the degenerative neurological disease or disorder is selected from the group consisting of Parkinson's disease, primary parkinsonism, paralysis agitans, and idiopathic parkinsonism.

5. The method of any one of claims 3 to 4 , wherein the composition further comprises amantadine, aplindore, apomorphine, benztropine, bromocriptine, carbidopa, entacapone, fenoldopam, istradefylline, levodopa (L-dopa), opicapone, pramipexole, rasagiline, ropinirole, rotigotine, safinamide, tolcapone, trihexyphenidyl, amphetamine, armodafinil, caffeine, mazindol, methylphenidate, modafinil, pitolisant, reboxetine, samelisant, serdexmethylphenidate, solriamfetol, or combinations thereof.

6. The method of claim 3 , wherein the sleep disorder is excessive daytime sleepiness associated with central hypersomnolence disorders, obstructive sleep apnea, or shift work disorder, wherein the central hypersomnolence disorder is selected from the group consisting of narcolepsy type-1 (with cataplexy), narcolepsy type 2, idiopathic hypersomnia, Kleine-Levin syndrome, hypersomnia due to a medical condition, hypersomnia due to a medication or substance, hypersomnia associated with a psychiatric condition, and insufficient sleep syndrome.

7. The composition of claim 2 , wherein the composition further comprises one or more excipients, wherein the excipients are selected from the group consisting of anti-adherents, binders, coatings, disintegrants, fillers, flavors, dyes, colors, glidants, lubricants, preservatives, sorbents, sweeteners, derivatives thereof, and combinations thereof.

8. The composition of claim 2 , composition has a dosing regimen that is about one to two times a day.

9. The composition of claim 8 , wherein the composition has a dosing regimen that is about one time a day, wherein the composition is orally administered to a human or an animal subject.

10. A kit comprising a therapeutically effective amount of a compound of claim 1 or pharmaceutically acceptable salt thereof, wherein the compound is in a unit dosage form, and wherein further the unit dosage form is 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 liquid, a thin strip, an oral thin film (OTF), an oral strip, a syrup, a suspension, a slurry, a sachet, a buccal tablet, and a suppository, and instructions for use thereof.

11. The kit of claim 10 , wherein the kit further comprises an additional therapeutic compound, wherein the additional therapeutic compound is selected from the group consisting of amantadine, aplindore, apomorphine, benztropine, bromocriptine, carbidopa, entacapone, fenoldopam, istradefylline, levodopa (L-dopa), opicapone, pramipexole, rasagiline, ropinirole, rotigotine, safinamide, tolcapone, trihexyphenidyl, amphetamine, armodafinil, caffeine, mazindol, methylphenidate, modafinil, pitolisant, reboxetine, samelisant, serdexmethylphenidate, solriamfetol, and combinations thereof.

12. The kit of claim 11 , wherein the additional therapeutic compound is in a unit dosage form, wherein the unit dosage form is 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 liquid, a thin strip, an oral thin film (OTF), an oral strip, a syrup, a suspension, a slurry, a sachet, a buccal tablet, and a suppository.

13. The kit of claim 12 , wherein the compound claim 4 is in a liquid dosage form and the additional therapeutic compound is in an oral powder form or sachet form.

14. The kit of claim 13 , wherein the additional therapeutic compound is added to the liquid dosage form of the compound prior to administration.

15. An oral formulation comprising a therapeutically effective dose of compound of claim 1 or a pharmaceutically acceptable salt thereof.

16. The oral formulation of claim 15 , wherein the oral formulation further comprises one or more excipients, wherein the excipients are selected from the group consisting of anti-adherents, binders, coatings, disintegrants, fillers, flavors, dyes, colors, glidants, lubricants, preservatives, sorbents, sweeteners, derivatives thereof, and combinations thereof.

17. The oral formulation of claim 15 or claim 16 , wherein the therapeutically effective dose is in a unit dosage form, wherein the unit dosage form is 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 liquid, a thin strip, an oral thin film (OTF), an oral strip, a syrup, a suspension, a slurry, a sachet, and a buccal tablet.

18. The oral formulation of claim 17 , wherein the oral formulation has a dosing regimen that is about one to two times a day.

19. The oral formulation of claim 18 , wherein the oral formulation has a dosing regimen that is about one time a day, wherein the oral formulation is orally administered to a human or an animal subject.

Assignments (3)
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 23, 2024
From: KEMPHARM, INC.
To: ZEVRA THERAPEUTICS, INC.
Reel/Frame 066664/0108 →
Continuity (2)
Provisional Application 63333391 · Apr 21, 2022
Related Publication 20230382880A1 · Nov 30, 2023
References Cited (35)
US 20020009667A1 · Nishimura et al. · 2002 [cited by applicant]
US 20020009668A1 · Nishimura et al. · 2002 [cited by applicant]
US 20040214755A1 · Albericio et al. · 2004 [cited by applicant]
US 20040241580A1 · Nishimura et al. · 2004 [cited by applicant]
US 20190194120A1 · Xiang et al. · 2019 [cited by applicant]
CN 103226290 · 2013 [cited by applicant]
EP 0388868 · 1990 [cited by applicant]
EP 1162506 · 2001 [cited by applicant]
EP 1164434 · 2001 [cited by applicant]
JP 0859596 · 1996 [cited by applicant]
JP 4973304 · 2008 [cited by applicant]
WO 2014093791 · 2014 [cited by applicant]
WO 2015083129 · 2015 [cited by applicant]
WO 2015083129A1 · 2015 [cited by applicant]
WO 2017050259 · 2017 [cited by applicant]
WO 2018191221 · 2018 [cited by applicant]
WO 2022214025 · 2022 [cited by applicant]
Kumar et. al., 2009, Allyl tetrahydropyranyl ether: a versatile alcohol/thiol protecting reagent, Tetrahedron Letters, 50, 6236-6240 (Year: 2009). [cited by examiner]
PCT, International Search Report regarding Application No. PCT/US2023/019097, 19 pages, dated Sep. 4, 2023. [cited by applicant]
Database Registry, accession No. 1502828-48-9. [cited by applicant]
Database Registry, accession No. 1508153-72-7. [cited by applicant]
Chee, Gaik-Lean, “Selective Deprotection of Isopropyl Esters, Carbamates and Carbonates with Aluminum Chloride,” Synlett, 2001, (10), 3 pgs., received Aug. 9, 2001. [cited by applicant]
Martin, S.F., et al., “Tetrahedron Letters,” 39 (12), Department of Chemistry and Biochemistry, The University of Texas at Austin, 4 pgs., received Nov. 26, 1997. [cited by applicant]
Strasdeit, H., et al., “Syntheses and Properties of Zinc and Calcium Complexes of Valinate and Isovalinate:- Metal a-Amino Acidates as Possible Constituents of the Early Earth's Chemical Inventory,” A European Journal, … [cited by applicant]
PCT, International Search Report regarding Application No. PCT/US2023/019107, 20 pages, dated Jun. 19, 2023. [cited by applicant]
Hall, C. Dennis, et al., “Kinetics and mechanism of the hydrolysis of tetrahydro-2-furyl and tetrahydropyran-2-yl alkanoates,” J Chem. Soc., Perkin Trans. 2, 1998, 23 pages, dated Mar. 25, 1998. [cited by applicant]
Macías-Benítez, Pablo, et al, “Microwave-Enhanced Coupling of Carboxylic Acids with Liquid Ketones and Cyclic Ethers Using Tetrabutylammonium Iodide/t Butyl Hydroperoxide,” J. Org. Chem. 2020, 85, 6027-6043, dated Apr. … [cited by applicant]
Lee, Sunggi, et al., “Asymmetric Catalysis via Cyclic, Aliphatic Oxocarbenium Ions,” J. Amer. Chem. Society 2017, 4 pages, dated Feb. 7, 2017. [cited by applicant]
PCT, International Search Report regarding Application No. PCT/US2023/019101, 13 pages, dated Aug. 23, 2023. [cited by applicant]
Gromek, S.M., et al.: “Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity”, Bioorganic & Medicinal Chemistry, vol. 24, No. 21, Aug. 24, 2016 (Aug. 24, … [cited by applicant]
Van Vranken, D.L. , et al.: “Catalysis of carbamate hydrolysis by an antibody”, Tetrahedron Letters, vol. 35, No. 23, Sep. 6, 1994 (Sep. 6, 1994), pp. 3873-3876, XP093068584, Elsevier Science Publishers, Oxford, GB ISSN… [cited by applicant]
Patent Cooperation Treaty, “International Preliminary Report on Patentability and Written Opinion”, issued in connection with International Patent Application No. PCT/US2023/019097, dated Oct. 8, 2024, 7 pages. [cited by applicant]
Patent Cooperation Treaty, “International Preliminary Report on Patentability and Written Opinion”, issued in connection with International Patent Application No. PCT/US2023/019101, dated Oct. 8, 2024, 8 pages. [cited by applicant]
Patent Cooperation Treaty, “International Preliminary Report on Patentability and Written Opinion”, issued in connection with International Patent Application No. PCT/US2023/019107, dated Oct. 8, 2024, 11 pages. [cited by applicant]
Patent Cooperation Treaty, “International Preliminary Report on Patentability and Written Opinion”, issued in connection with International Patent Application No. PCT/US2023/019112, dated Oct. 8, 2024, 10 pages. [cited by applicant]