CN112543758A - 墨蝶呤的药学上可接受的盐 - Google Patents

墨蝶呤的药学上可接受的盐 Download PDF

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Publication number
CN112543758A
CN112543758A CN201980050845.2A CN201980050845A CN112543758A CN 112543758 A CN112543758 A CN 112543758A CN 201980050845 A CN201980050845 A CN 201980050845A CN 112543758 A CN112543758 A CN 112543758A
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crystal
pharmaceutically acceptable
salt
acceptable salt
subject
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Chinese (zh)
Inventor
D·E·莱维
N·史密斯
J·雷斯
H·约施诺
T·科莫达
Y·施罗
S·穆拉塔
T·马楚莫托
K·基施莫托
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Ptc Medical Mp Co
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Ptc Medical Mp Co
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Publication of CN112543758A publication Critical patent/CN112543758A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/02Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/04Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/30Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of nitrogen-to-oxygen or nitrogen-to-nitrogen bonds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/08Malonic acid
    • 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
    • C07C59/01Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
    • C07C59/06Glycolic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/03Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
    • C07C65/05Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring o-Hydroxy carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • C07D213/80Acids; Esters in position 3
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CN201980050845.2A 2018-05-30 2019-05-30 墨蝶呤的药学上可接受的盐 Pending CN112543758A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201862678025P 2018-05-30 2018-05-30
US62/678025 2018-05-30
US201862726612P 2018-09-04 2018-09-04
US62/726612 2018-09-04
US201962822336P 2019-03-22 2019-03-22
US62/822336 2019-03-22
GC201937661 2019-05-28
GC2019/37661 2019-05-28
PCT/US2019/034505 WO2019232120A1 (en) 2018-05-30 2019-05-30 Pharmaceutically acceptable salts of sepiapterin

Publications (1)

Publication Number Publication Date
CN112543758A true CN112543758A (zh) 2021-03-23

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CN201980050845.2A Pending CN112543758A (zh) 2018-05-30 2019-05-30 墨蝶呤的药学上可接受的盐

Country Status (13)

Country Link
US (1) US20210269443A1 (https=)
EP (1) EP3807279B1 (https=)
JP (2) JP7778477B2 (https=)
KR (1) KR20210038848A (https=)
CN (1) CN112543758A (https=)
AU (2) AU2019277372B2 (https=)
BR (1) BR112020024332A2 (https=)
CA (1) CA3102070A1 (https=)
CL (1) CL2020003101A1 (https=)
CO (1) CO2020016582A2 (https=)
IL (1) IL279101A (https=)
MX (1) MX2020012978A (https=)
WO (1) WO2019232120A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11072614B2 (en) 2016-11-29 2021-07-27 Ptc Therapeutics Mp, Inc. Polymorphs of sepiapterin and salts thereof
US11130760B2 (en) 2016-11-29 2021-09-28 Ptc Therapeutics Mp, Inc. Polymorphic form of sepiapterin
JP7811085B2 (ja) 2017-09-01 2026-02-04 ピーティーシー セラピューティクス エムピー,インコーポレイテッド セピアプテリンを含む医薬組成物及びその使用
EP3801536B1 (en) 2018-05-30 2024-07-17 PTC Therapeutics MP, Inc. Administration of sepiapterin without food for use in a method for increasing sepiapterin plasma exposure
AU2019277372B2 (en) * 2018-05-30 2024-12-19 Ptc Therapeutics Mp, Inc. Pharmaceutically acceptable salts of sepiapterin
CN112654356A (zh) * 2018-05-30 2021-04-13 Ptc医疗Mp公司 增加四氢生物蝶呤血浆暴露的组合物和方法
IL290321B1 (en) 2019-08-05 2026-04-01 Ptc Therapeutics Inc Use of spiapterin and its metabolites for radiation exposure treatment
IL291565B1 (en) 2019-09-25 2026-04-01 Ptc Therapeutics Inc Method for treating phenylalanine irregularity
CA3165636A1 (en) 2020-01-24 2021-07-29 Neil Smith Methods for treating parkinson's disease with sepiapterin
CN114621198B (zh) 2020-12-11 2025-01-21 北京夏禾科技有限公司 有机电致发光材料及其器件
JP2024506336A (ja) 2021-02-09 2024-02-13 ピーティーシー セラピューティクス エムピー,インコーポレイテッド 膠芽腫の治療方法
EP4291196A1 (en) 2021-02-09 2023-12-20 PTC Therapeutics MP, Inc. Methods for treating covid-19 with sepiapterin

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5910304A (en) 1982-12-13 1999-06-08 Texas A&M University System Low-dose oral administration of interferons
CA1320905C (en) 1986-11-06 1993-08-03 Joseph M. Cummins Treatment of immuno-resistant disease
ATE218345T1 (de) * 1994-08-05 2002-06-15 Suntory Ltd Arzneimittel gegen spinocerebellare degeneration
US6036949A (en) 1998-03-05 2000-03-14 Amarillo Biosciences, Inc. Treatment of fibromyalgia with low doses of interferon
WO2008128049A2 (en) * 2007-04-11 2008-10-23 Biomarin Pharmaceutical Inc. Methods of administering tetrahydrobiopterin, associated compositions, and methods of measuring
JP2012512848A (ja) 2008-12-23 2012-06-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 有機化合物の塩の形態
EP2562176B1 (en) 2010-04-22 2018-08-15 Nihon University Medicinal agent and beverage/food for preventing cerebral dysfunction and improving same
IN2014DN09053A (https=) 2012-05-07 2015-05-22 Shiratori Pharm
WO2017218421A1 (en) * 2016-06-13 2017-12-21 Meharry Medical College Modulation of the nitric oxide synthase pathway for oral health
US11130760B2 (en) * 2016-11-29 2021-09-28 Ptc Therapeutics Mp, Inc. Polymorphic form of sepiapterin
US11072614B2 (en) * 2016-11-29 2021-07-27 Ptc Therapeutics Mp, Inc. Polymorphs of sepiapterin and salts thereof
JP7811085B2 (ja) 2017-09-01 2026-02-04 ピーティーシー セラピューティクス エムピー,インコーポレイテッド セピアプテリンを含む医薬組成物及びその使用
AU2019277372B2 (en) * 2018-05-30 2024-12-19 Ptc Therapeutics Mp, Inc. Pharmaceutically acceptable salts of sepiapterin

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Publication number Publication date
AU2019277372A1 (en) 2021-01-21
EP3807279A4 (en) 2022-04-06
CL2020003101A1 (es) 2021-05-14
CA3102070A1 (en) 2019-12-05
IL279101A (en) 2021-01-31
AU2025201002A1 (en) 2025-03-06
WO2019232120A1 (en) 2019-12-05
JP7841008B2 (ja) 2026-04-06
EP3807279B1 (en) 2025-12-31
JP2021527031A (ja) 2021-10-11
US20210269443A1 (en) 2021-09-02
KR20210038848A (ko) 2021-04-08
MX2020012978A (es) 2021-04-28
CO2020016582A2 (es) 2021-04-08
BR112020024332A2 (pt) 2021-02-23
AU2019277372B2 (en) 2024-12-19
EP3807279A1 (en) 2021-04-21
JP7778477B2 (ja) 2025-12-02
JP2024063143A (ja) 2024-05-10

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