AU2019211458B2 - Compositions and methods of enhancing 5-hydroxytryptophan bioavailability - Google Patents

Compositions and methods of enhancing 5-hydroxytryptophan bioavailability Download PDF

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AU2019211458B2
AU2019211458B2 AU2019211458A AU2019211458A AU2019211458B2 AU 2019211458 B2 AU2019211458 B2 AU 2019211458B2 AU 2019211458 A AU2019211458 A AU 2019211458A AU 2019211458 A AU2019211458 A AU 2019211458A AU 2019211458 B2 AU2019211458 B2 AU 2019211458B2
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htp
carbidopa
dose
low
serotonin
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AU2019211458A1 (en
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Marc G. Caron
Jacob P.R. Jacobsen
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Duke University
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Duke University
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/15—Oximes (>C=N—O—); Hydrazines (>N—N<); Hydrazones (>N—N=) ; Imines (C—N=C)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2019211458A 2018-01-29 2019-01-28 Compositions and methods of enhancing 5-hydroxytryptophan bioavailability Active AU2019211458B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862623073P 2018-01-29 2018-01-29
US62/623,073 2018-01-29
US201862743816P 2018-10-10 2018-10-10
US62/743,816 2018-10-10
PCT/US2019/015391 WO2019148087A1 (en) 2018-01-29 2019-01-28 Compositions and methods of enhancing 5-hydroxytryptophan bioavailability

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AU2019211458A1 AU2019211458A1 (en) 2020-08-06
AU2019211458B2 true AU2019211458B2 (en) 2024-08-29

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US (1) US11337963B2 (https=)
EP (1) EP3746058B1 (https=)
JP (2) JP7758320B2 (https=)
KR (2) KR20200116110A (https=)
CN (1) CN111902137A (https=)
AU (1) AU2019211458B2 (https=)
BR (1) BR112020015068A2 (https=)
ES (1) ES2948788T3 (https=)
IL (1) IL276059B2 (https=)
MX (1) MX2020007760A (https=)
MY (1) MY209656A (https=)
RU (1) RU2020125170A (https=)
SG (1) SG11202007178VA (https=)
WO (1) WO2019148087A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12409163B2 (en) * 2021-07-30 2025-09-09 Evecxia Therapeutics, Inc. Method of enhancing 5-hydroxytryptophan (5-HTP) exposure
WO2023009841A1 (en) * 2021-07-30 2023-02-02 Evecxia Therapeutics, Inc. 5-hydroxytryptophan gastroretentive dosage forms
US11779567B2 (en) 2021-10-14 2023-10-10 Evecxia Therapeutics, Inc. Method for optimizing 5-hydroxytryptamine function in the brain for therapeutic purposes
DE102022103658A1 (de) * 2022-02-16 2023-08-17 Joachim Kamprad Arzneimittelzusammensetzung enthaltend L-Tryptophan (L-Try) und L-5-Hydroxytryptophan (5-HTP) sowie einen peripheren Abbauhemmer
WO2024148354A1 (en) 2023-01-06 2024-07-11 Evecxia Therapeutics, Inc. A method of enhancing 5-hydroxytryptophan (5-htp) exposure
CN119074695A (zh) * 2024-08-29 2024-12-06 江南大学 一种可提高脑内5-ht水平的口服缓释制剂及其在改善失眠中的应用

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US4658038A (en) 1982-10-07 1987-04-14 Research Foundation For Mental Hygiene, Inc. N-acylated 5-hydroxytryptophan amide derivatives
FR2654931B1 (fr) * 1989-11-24 1993-08-27 Trouillas Paul Compositions pharmaceutiques possedant une activite sur l'ataxie et les troubles de l'equilibre, cerebelleux ou autres, de toutes origines, comprenant l'association de l-5-hydroxytryptophane et de carbidopa.
CA2290624C (en) 1997-06-06 2006-12-05 John W. Shell Gastric-retentive oral drug dosage forms for controlled release of highly soluble drugs
US6635280B2 (en) 1997-06-06 2003-10-21 Depomed, Inc. Extending the duration of drug release within the stomach during the fed mode
US6207699B1 (en) 1999-06-18 2001-03-27 Richard Brian Rothman Pharmaceutical combinations for treating obesity and food craving
TWI312285B (en) 2001-10-25 2009-07-21 Depomed Inc Methods of treatment using a gastric retained gabapentin dosage
CA2409552A1 (en) 2001-10-25 2003-04-25 Depomed, Inc. Gastric retentive oral dosage form with restricted drug release in the lower gastrointestinal tract
US6723340B2 (en) 2001-10-25 2004-04-20 Depomed, Inc. Optimal polymer mixtures for gastric retentive tablets
US20060013875A1 (en) 2002-05-29 2006-01-19 Impax Laboratories, Inc. Combination immediate release controlled release levodopa/carbidopa dosage forms
AU2003293423A1 (en) 2002-12-06 2004-06-30 Xenoport, Inc. Carbidopa prodrugs and uses thereof
EP1746985A4 (en) * 2004-05-21 2010-08-11 Univ Duke METHOD FOR INCREASING THE EFFECT OF SEROTONINE RECOVERY INHIBITORS
US20070213370A1 (en) 2005-11-18 2007-09-13 H. Lundbeck A/S 5-HTP Combination Therapy
US8969400B2 (en) 2007-10-01 2015-03-03 Duke University Pharmaceutical compositions of 5-hydroxytryptophan and serotonin-enhancing compound
JP2012500221A (ja) 2008-08-15 2012-01-05 ディポメド，インコーポレイティド Ｃｎｓ障害の処理及び予防のための胃保持性医薬組成物
RU2012133467A (ru) * 2010-02-05 2014-02-10 Фосфейдженикс Лимитед Композиция носителя
EP2629615B1 (en) * 2010-10-22 2018-10-10 Duke University Slow-release formulations of 5-hydroxytryptophan as an adjunct to pro-serotonergic therapies
CN103554005A (zh) 2013-11-22 2014-02-05 长沙理工大学 一种左旋5-羟基色氨酸的简便合成新方法

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Publication number Publication date
BR112020015068A2 (pt) 2021-01-05
IL276059B2 (en) 2024-08-01
EP3746058B1 (en) 2023-06-07
EP3746058A4 (en) 2021-12-22
JP7758320B2 (ja) 2025-10-22
MX2020007760A (es) 2020-10-28
CN111902137A (zh) 2020-11-06
AU2019211458A1 (en) 2020-08-06
EP3746058C0 (en) 2023-06-07
KR20200116110A (ko) 2020-10-08
JP2023153871A (ja) 2023-10-18
ES2948788T3 (es) 2023-09-19
KR20250025043A (ko) 2025-02-20
US11337963B2 (en) 2022-05-24
RU2020125170A (ru) 2022-02-28
WO2019148087A1 (en) 2019-08-01
EP3746058A1 (en) 2020-12-09
JP2021511365A (ja) 2021-05-06
IL276059A (en) 2020-08-31
US20210346345A1 (en) 2021-11-11
IL276059B1 (en) 2024-04-01
CA3089068A1 (en) 2019-08-01
MY209656A (en) 2025-07-29
SG11202007178VA (en) 2020-08-28

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