JP7038675B2 - 結晶塩形態 - Google Patents

結晶塩形態 Download PDF

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JP7038675B2
JP7038675B2 JP2018567022A JP2018567022A JP7038675B2 JP 7038675 B2 JP7038675 B2 JP 7038675B2 JP 2018567022 A JP2018567022 A JP 2018567022A JP 2018567022 A JP2018567022 A JP 2018567022A JP 7038675 B2 JP7038675 B2 JP 7038675B2
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JP2019512542A5 (enExample
JP2019512542A (ja
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エム ダンカン，スコット
ピー レッドモン，マーティン
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Stealth Biotherapeutics Inc
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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
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • 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
    • 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)
JP2018567022A 2016-03-11 2017-03-10 結晶塩形態 Active JP7038675B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662307095P 2016-03-11 2016-03-11
US62/307,095 2016-03-11
PCT/US2017/021790 WO2017156403A1 (en) 2016-03-11 2017-03-10 Crystalline salt forms

Publications (3)

Publication Number Publication Date
JP2019512542A JP2019512542A (ja) 2019-05-16
JP2019512542A5 JP2019512542A5 (enExample) 2020-03-26
JP7038675B2 true JP7038675B2 (ja) 2022-03-18

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JP2018567022A Active JP7038675B2 (ja) 2016-03-11 2017-03-10 結晶塩形態

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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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015084649A1 (en) 2013-12-03 2015-06-11 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
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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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
EP3563862B1 (en) * 2009-03-20 2021-05-05 The General Hospital Corporation d/b/a Massachusetts General Hospital D-arg-2'6'-dimethyltyrosine-lys-phe-nh2 for use in the prevention of secondary complications of burn injuries
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
CA2787331A1 (en) * 2010-01-25 2011-07-28 Hazel H. Szeto Aromatic-cationic peptides and uses of same
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
EP3060573B1 (en) * 2013-10-23 2019-07-17 Kaneka Corporation Tetrapeptide compound and method for producing same
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015084649A1 (en) 2013-12-03 2015-06-11 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
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

Non-Patent Citations (2)

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Title
Ｃ．Ｇ．ＷＥＲＭＵＴＨ編，「最新 創薬化学 下巻」，３４７～３６５頁，株式会社 テクノミック，1999年
芦澤 一英、他，医薬品の多形現象と晶析の科学，丸善プラネット株式会社，2002年09月20日，第３０５－３１７頁

Also Published As

Publication number Publication date
EP3426675A1 (en) 2019-01-16
EP3426675A4 (en) 2019-10-16
CA3017359A1 (en) 2017-09-14
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
CN115160402A (zh) 2022-10-11
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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