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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China
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C07K5/0817—Tripeptides with the first amino acid being basic the first amino acid being Arg
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/06—Oxalic acid
    • C07C55/07—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/10—Succinic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C63/00—Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings
    • C07C63/04—Monocyclic monocarboxylic acids
    • C07C63/06—Benzoic acid
    • C07C63/08—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Toxicology (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

Family

ID=59789873

Family Applications (2)

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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

Family Applications After (1)

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

Country Status (6)

Country Link
US (4) 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
WO2017156403A1 (en) 2016-03-11 2017-09-14 Stealth Biotherapeutics Crystalline salt forms
US11034724B2 (en) 2017-04-05 2021-06-15 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
ES2941266T3 (es) * 2018-04-02 2023-05-19 Stealth Biotherapeutics Inc Dipéptidos cristalinos útiles en la síntesis 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

Family Cites Families (19)

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Publication number Priority date Publication date Assignee Title
SG64368A1 (en) * 1988-06-30 1999-04-27 Astra Ab Dermorphin analogs their methods of preparation pharmaceutical compositions and methods of therapeutic treatment using the same
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
SI3708178T1 (sl) 2009-08-24 2024-01-31 Stealth Biotherapeutics Inc. Peptid za uporabo pri preprečevanju ali zdravljenju degeneracije makule
US20130195837A1 (en) * 2009-12-31 2013-08-01 Stealth Peptides International, Inc. Methods for the prevention or treatment of vessel occlusion injury
EP2808029A3 (en) * 2010-03-15 2015-04-01 Stealth Peptides International, Inc. Combination therapies using cyclosporine and aromatic cationic peptides
CN103003283A (zh) * 2010-06-09 2013-03-27 Abbvie公司 激酶抑制剂的结晶形式
HK1204988A1 (en) * 2012-02-22 2015-12-11 Stealth Peptides International, Inc. Methods and compositions for preventing or treating ophthalmic conditions
US10793597B2 (en) * 2013-03-01 2020-10-06 Stealth Biotherapeutics Corp Methods for the treatment of mitochondrial diseases associated with a mutation in SURF 1 or POLG gene resulting in a disruption of mitochondrial oxidative phosphorylation
SG11201604517WA (en) * 2013-12-03 2016-07-28 Amgen Inc Crystalline forms of n-(4-((3-(2-amino-4-pyrimidinyl) - 2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1 -phthalazinamine pharmaceutically acceptable salts and uses thereof
WO2016004067A1 (en) * 2014-06-30 2016-01-07 Stealth Biotherapeutics Corp Aromatic-cationic peptide formulations, compositions and methods of use
WO2016007921A1 (en) * 2014-07-10 2016-01-14 Rhodel Island Hospital Treating arrhythmia with mitochondrial-targeted antioxidants
JP6854771B2 (ja) 2015-03-06 2021-04-07 ステルス バイオセラピューティックス コープ 薬学的に適切なペプチドを調製するための方法
WO2017156403A1 (en) 2016-03-11 2017-09-14 Stealth Biotherapeutics Crystalline salt forms
CN110087667A (zh) * 2016-08-16 2019-08-02 隐形生物治疗公司 Elamipretide的基于N-羧基酸酐的规模合成
US11034724B2 (en) * 2017-04-05 2021-06-15 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
ES2941266T3 (es) * 2018-04-02 2023-05-19 Stealth Biotherapeutics Inc Dipéptidos cristalinos útiles en la síntesis 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

Also Published As

Publication number Publication date
EP3426675A1 (en) 2019-01-16
EP3426675A4 (en) 2019-10-16
CA3017359A1 (en) 2017-09-14
JP7038675B2 (ja) 2022-03-18
US20230279049A1 (en) 2023-09-07
US20210047368A1 (en) 2021-02-18
US12252553B2 (en) 2025-03-18
CN109476700A (zh) 2019-03-15
US20190382442A1 (en) 2019-12-19
EP3426675B1 (en) 2020-08-05
US10683326B2 (en) 2020-06-16
WO2017156403A1 (en) 2017-09-14
JP2019512542A (ja) 2019-05-16
US11555053B2 (en) 2023-01-17
US20260015385A1 (en) 2026-01-15

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