TWI670058B - 經取代的甘胺酸化合物的共晶及其用途 - Google Patents

經取代的甘胺酸化合物的共晶及其用途 Download PDF

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Publication number
TWI670058B
TWI670058B TW107101039A TW107101039A TWI670058B TW I670058 B TWI670058 B TW I670058B TW 107101039 A TW107101039 A TW 107101039A TW 107101039 A TW107101039 A TW 107101039A TW I670058 B TWI670058 B TW I670058B
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TW
Taiwan
Prior art keywords
eutectic
crystal
alkyl
disorder
methylglycine
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TW107101039A
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English (en)
Chinese (zh)
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TW201840308A (zh
Inventor
蔡果荃
王景正
謝天嵐
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心悅生醫股份有限公司
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Publication of TW201840308A publication Critical patent/TW201840308A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic 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
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/12Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/15Fumaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255Tartaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/62Three oxygen atoms, e.g. ascorbic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Medicinal Preparation (AREA)
TW107101039A 2017-02-13 2018-01-11 經取代的甘胺酸化合物的共晶及其用途 TWI670058B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15/430,750 US9877942B1 (en) 2017-02-13 2017-02-13 Co-crystals of substituted glycine and uses thereof
US15430750 2017-02-13

Publications (2)

Publication Number Publication Date
TW201840308A TW201840308A (zh) 2018-11-16
TWI670058B true TWI670058B (zh) 2019-09-01

Family

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TW107101039A TWI670058B (zh) 2017-02-13 2018-01-11 經取代的甘胺酸化合物的共晶及其用途

Country Status (11)

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US (4) US9877942B1 (enExample)
EP (1) EP3579828B1 (enExample)
JP (2) JP2020507567A (enExample)
KR (1) KR20190118574A (enExample)
CN (1) CN110520117A (enExample)
CA (1) CA3051284A1 (enExample)
IL (1) IL268220B (enExample)
MX (1) MX393880B (enExample)
RU (1) RU2019128576A (enExample)
TW (1) TWI670058B (enExample)
WO (1) WO2018145553A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102403048B1 (ko) * 2016-06-13 2022-05-26 신유알엑스 인터내셔널 (타이완) 코포레이션 벤조산나트륨의 공-결정 및 그의 용도
US9877942B1 (en) 2017-02-13 2018-01-30 Syneurx International (Taiwan) Corp. Co-crystals of substituted glycine and uses thereof
CN113233976B (zh) * 2021-05-08 2021-11-16 广州萃普生物科技有限公司 一种没食子酸和氨基乙酸共晶及含有该共晶的美白膏霜
EP4419499A1 (en) 2021-10-20 2024-08-28 Purac Biochem B.V. Co-crystal of citric acid and glycine and uses thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008153945A2 (en) * 2007-06-06 2008-12-18 University Of South Florida Nutraceutical co-crystal compositions

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69936848T2 (de) * 1998-04-14 2008-05-15 The General Hospital Corp., Boston Verwendung von d-serin oder d-alanin zur behandlung von schizophrenie
WO2005055983A2 (en) * 2003-12-09 2005-06-23 Medcrystalforms, Llc Method of preparation of mixed phase co-crystals with active agents
WO2009018368A1 (en) * 2007-07-30 2009-02-05 Los Angeles Biomedical Research Institute At Harbor-Ucla Medical Center Combination treatment of nmda (n-methyl-d-aspartate)-enhancer, glycine transporter inhibitor, d-amino acid oxidase inhibitor (daaoi) for neuropsychiatric disorders
GB201411802D0 (en) * 2014-07-02 2014-08-13 Univ Bradford Effervescent compositions
US9877942B1 (en) 2017-02-13 2018-01-30 Syneurx International (Taiwan) Corp. Co-crystals of substituted glycine and uses thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008153945A2 (en) * 2007-06-06 2008-12-18 University Of South Florida Nutraceutical co-crystal compositions

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
H. X. Zhang et al."The glycine transport inhibitor sarcosine is an NMDA receptor co-agonist that differs from glycine." The Journal of Physiology,Vol.587(13) ,pp.3207-3220, 2009 *
H. X. Zhang et al."The glycine transport inhibitor sarcosine is an NMDA receptor co-agonist that differs from glycine." The Journal of Physiology,Vol.587(13) ,pp.3207-3220, 2009。
M. Fleck et al."Two forms of sarcosine sarcosinium hydrogen L-tartrate." Journal of Molecular Structure,Vol.1045, pp.95-103, 2013 *
M. Fleck et al."Two forms of sarcosine sarcosinium hydrogen L-tartrate." Journal of Molecular Structure,Vol.1045, pp.95-103, 2013。

Also Published As

Publication number Publication date
RU2019128576A3 (enExample) 2021-05-14
TW201840308A (zh) 2018-11-16
IL268220A (en) 2019-09-26
WO2018145553A1 (en) 2018-08-16
EP3579828B1 (en) 2025-03-26
US10328041B2 (en) 2019-06-25
EP3579828A4 (en) 2020-11-18
US10328042B2 (en) 2019-06-25
US20180228753A1 (en) 2018-08-16
US20180228754A1 (en) 2018-08-16
MX393880B (es) 2025-03-24
US9877942B1 (en) 2018-01-30
JP2020507567A (ja) 2020-03-12
IL268220B (en) 2022-04-01
US10765651B2 (en) 2020-09-08
RU2019128576A (ru) 2021-03-15
CN110520117A (zh) 2019-11-29
KR20190118574A (ko) 2019-10-18
EP3579828A1 (en) 2019-12-18
US20190262299A1 (en) 2019-08-29
CA3051284A1 (en) 2018-08-16
JP7723991B2 (ja) 2025-08-15
JP2023082101A (ja) 2023-06-13
MX2019009616A (es) 2019-10-14

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