CN115160402A - 结晶盐形式 - Google Patents

结晶盐形式 Download PDF

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Publication number
CN115160402A
CN115160402A CN202210620260.3A CN202210620260A CN115160402A CN 115160402 A CN115160402 A CN 115160402A CN 202210620260 A CN202210620260 A CN 202210620260A CN 115160402 A CN115160402 A CN 115160402A
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Prior art keywords
crystalline form
compound
xrpd
characteristic peaks
salt
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Pending
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CN202210620260.3A
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English (en)
Chinese (zh)
Inventor
S.M.邓肯
M.P.雷蒙
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Stealth Biotherapeutics Corp
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Stealth Biotherapeutics Corp
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Publication of CN115160402A publication Critical patent/CN115160402A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1019Tetrapeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0815Tripeptides with the first amino acid being basic
    • C07K5/0817Tripeptides with the first amino acid being basic the first amino acid being Arg
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/06Free radical scavengers or antioxidants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07C55/06Oxalic acid
    • C07C55/07Salts thereof
    • 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
    • C07C55/10Succinic 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
    • C07C63/00Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings
    • C07C63/04Monocyclic monocarboxylic acids
    • C07C63/06Benzoic acid
    • C07C63/08Salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Toxicology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN202210620260.3A 2016-03-11 2017-03-10 结晶盐形式 Pending CN115160402A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662307095P 2016-03-11 2016-03-11
US62/307095 2016-03-11
CN201780029335.8A CN109476700A (zh) 2016-03-11 2017-03-10 结晶盐形式
PCT/US2017/021790 WO2017156403A1 (en) 2016-03-11 2017-03-10 Crystalline salt forms

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201780029335.8A Division CN109476700A (zh) 2016-03-11 2017-03-10 结晶盐形式

Publications (1)

Publication Number Publication Date
CN115160402A true CN115160402A (zh) 2022-10-11

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CN202210620260.3A Pending CN115160402A (zh) 2016-03-11 2017-03-10 结晶盐形式
CN201780029335.8A Pending CN109476700A (zh) 2016-03-11 2017-03-10 结晶盐形式

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Country Status (6)

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US (3) US10683326B2 (enExample)
EP (1) EP3426675B1 (enExample)
JP (1) JP7038675B2 (enExample)
CN (2) CN115160402A (enExample)
CA (1) CA3017359A1 (enExample)
WO (1) WO2017156403A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115160402A (zh) 2016-03-11 2022-10-11 隐形生物治疗公司 结晶盐形式
WO2018187400A1 (en) 2017-04-05 2018-10-11 Stealth Biotherapeutics Corp. Crystalline salt forms of boc-d-arg-dmt-lys-(boc)-phe-nh2
US10676506B2 (en) 2018-01-26 2020-06-09 Stealth Biotherapeutics Corp. Crystalline bis- and tris-hydrochloride salt of elamipretide
CA3095869C (en) 2018-04-02 2025-10-21 Stealth Biotherapeutics Inc. CRYSTALLINE DIPEPTIDES USEFUL IN THE SYNTHESIS OF ELAMIPRETIDE

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103933542A (zh) * 2009-03-20 2014-07-23 通用医疗公司以马萨诸塞州通用医疗公司名义经营 预防和治疗烧伤损伤和继发性并发症的方法
WO2015060462A1 (en) * 2013-10-23 2015-04-30 Kaneka Corporation Tetrapeptide compound and method for producing same
CN104725472A (zh) * 2010-01-25 2015-06-24 康奈尔大学 芳香族阳离子肽及其用途
WO2016001042A1 (en) * 2014-06-30 2016-01-07 Flamma S.P.A. Process for the production of d-arginyl-2,6-dimethyl-l-tyrosyl-l-lysyl-l-phenylalaninamide

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ES2085865T3 (es) * 1988-06-30 1996-06-16 Astra Ab Analogos de dermorfina, sus metodos de preparacion, composiciones farmaceuticas, y metodos de tratamiento terapeutico que los emplean.
SI2656854T1 (sl) 2003-02-04 2015-09-30 Cornell Research Foundation, Inc. Uporabe aromatsko-kationskega peptida
US20120178762A1 (en) * 2006-12-15 2012-07-12 Warner Chilcott Company, Llc Compositions of azimilide dihydrochloride
WO2010125004A1 (en) 2009-04-29 2010-11-04 Nerviano Medical Sciences S.R.L. Cdk inhibitor salts
SMT202300433T1 (it) * 2009-08-24 2024-01-10 Stealth Biotherapeutics Inc Peptide per l'uso nella prevenzione o nel trattamento della degenerazione maculare
CA2786280A1 (en) * 2009-12-31 2011-07-07 Stealth Peptides International, Inc. Methods for the prevention or treatment of vessel occlusion injury
WO2011116007A1 (en) * 2010-03-15 2011-09-22 Stealth Peptides International, Inc. Combination therapies using cyclosporine and aromatic cationic peptides
WO2011156473A1 (en) 2010-06-09 2011-12-15 Abbott Laboratories Crystalline forms of kinase inhibitors
HK1204988A1 (en) * 2012-02-22 2015-12-11 Stealth Peptides International, Inc. Methods and compositions for preventing or treating ophthalmic conditions
CN110339339A (zh) * 2013-03-01 2019-10-18 康德生物医疗技术公司 治疗线粒体疾病的方法
JP6634016B2 (ja) 2013-12-03 2020-01-22 アムジエン・インコーポレーテツド N−(4−((3−(2−アミノ−4−ピリミジニル)−2−ピリジニル)オキシ)フェニル)−4−(4−メチル−2−チエニル)−1−フタラジンアミンの薬学的に許容される塩の結晶形態及びその使用
WO2016004067A1 (en) * 2014-06-30 2016-01-07 Stealth Biotherapeutics Corp Aromatic-cationic peptide formulations, compositions and methods of use
AU2015287583A1 (en) * 2014-07-10 2017-02-02 Rhode Island Hospital Treating arrhythmia with mitochondrial-targeted antioxidants
EP3800192A1 (en) 2015-03-06 2021-04-07 Stealth Biotherapeutics Corp Processes for preparing pharmaceutically relevant peptides
CN115160402A (zh) 2016-03-11 2022-10-11 隐形生物治疗公司 结晶盐形式
US10961273B2 (en) * 2016-08-16 2021-03-30 Stealth Biotherapeutics Corp. N-carboxyanhydride-based-scale synthesis of elamipretide
WO2018187400A1 (en) 2017-04-05 2018-10-11 Stealth Biotherapeutics Corp. Crystalline salt forms of boc-d-arg-dmt-lys-(boc)-phe-nh2
US10676506B2 (en) * 2018-01-26 2020-06-09 Stealth Biotherapeutics Corp. Crystalline bis- and tris-hydrochloride salt of elamipretide
CA3095869C (en) * 2018-04-02 2025-10-21 Stealth Biotherapeutics Inc. CRYSTALLINE DIPEPTIDES USEFUL IN THE SYNTHESIS OF ELAMIPRETIDE

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103933542A (zh) * 2009-03-20 2014-07-23 通用医疗公司以马萨诸塞州通用医疗公司名义经营 预防和治疗烧伤损伤和继发性并发症的方法
CN104725472A (zh) * 2010-01-25 2015-06-24 康奈尔大学 芳香族阳离子肽及其用途
WO2015060462A1 (en) * 2013-10-23 2015-04-30 Kaneka Corporation Tetrapeptide compound and method for producing same
WO2016001042A1 (en) * 2014-06-30 2016-01-07 Flamma S.P.A. Process for the production of d-arginyl-2,6-dimethyl-l-tyrosyl-l-lysyl-l-phenylalaninamide

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Publication number Publication date
EP3426675A1 (en) 2019-01-16
US10683326B2 (en) 2020-06-16
JP2019512542A (ja) 2019-05-16
JP7038675B2 (ja) 2022-03-18
WO2017156403A1 (en) 2017-09-14
EP3426675B1 (en) 2020-08-05
US20210047368A1 (en) 2021-02-18
US20230279049A1 (en) 2023-09-07
CA3017359A1 (en) 2017-09-14
US11555053B2 (en) 2023-01-17
CN109476700A (zh) 2019-03-15
US20190382442A1 (en) 2019-12-19
US12252553B2 (en) 2025-03-18
EP3426675A4 (en) 2019-10-16

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