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)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
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)

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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 (3) US10683326B2 (enExample)
EP (1) EP3426675B1 (enExample)
JP (1) JP7038675B2 (enExample)
CN (2) CN109476700A (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
KR20250010134A (ko) 2018-04-02 2025-01-20 스텔스 바이오테라퓨틱스 인코포레이티드 엘라미프레티드의 합성에 유용한 결정질 디펩티드

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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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.
US7576061B2 (en) * 2003-02-04 2009-08-18 Cornell Research Foundation, Inc. Methods for preventing mitochondrial permeability transition
US20120178762A1 (en) * 2006-12-15 2012-07-12 Warner Chilcott Company, Llc Compositions of azimilide dihydrochloride
EP2408463B1 (en) * 2009-03-20 2016-10-19 The General Hospital Corporation d/b/a Massachusetts General Hospital D-arg-2'6'-dimethyltyrosine-lys-phe-nh2 for use in the prevention and treatment of burn injuries and secondary complications
WO2010125004A1 (en) 2009-04-29 2010-11-04 Nerviano Medical Sciences S.R.L. Cdk inhibitor salts
CN102625709A (zh) * 2009-08-24 2012-08-01 康肽德生物医药技术有限公司 用于预防或治疗眼科病症的方法和组合物
AU2010339410A1 (en) * 2009-12-31 2012-07-19 Stealth Peptides International, Inc. Methods for the prevention or treatment of vessel occlusion injury
EP2733150A1 (en) * 2010-01-25 2014-05-21 Cornell University Aromatic-cationic peptides and uses of same
WO2011116007A1 (en) * 2010-03-15 2011-09-22 Stealth Peptides International, Inc. Combination therapies using cyclosporine and aromatic cationic peptides
JP5727599B2 (ja) * 2010-06-09 2015-06-03 アボット・ラボラトリーズＡｂｂｏｔｔ Ｌａｂｏｒａｔｏｒｉｅｓ キナーゼ阻害剤の結晶形態
CN104244964A (zh) * 2012-02-22 2014-12-24 康肽德生物医药技术有限公司 用于预防或治疗眼科病状的方法和组合物
JP6839490B2 (ja) * 2013-03-01 2021-03-10 ステルス バイオセラピューティックス コープ ミトコンドリア疾患の治療のための方法
JP2016539931A (ja) * 2013-10-23 2016-12-22 株式会社カネカ テトラペプチド化合物及びその製造方法
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WO2016007921A1 (en) * 2014-07-10 2016-01-14 Rhodel 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
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
KR20250010134A (ko) * 2018-04-02 2025-01-20 스텔스 바이오테라퓨틱스 인코포레이티드 엘라미프레티드의 합성에 유용한 결정질 디펩티드

Patent Citations (2)

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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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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
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Publication number Publication date
CA3017359A1 (en) 2017-09-14
CN109476700A (zh) 2019-03-15
CN115160402A (zh) 2022-10-11
EP3426675A1 (en) 2019-01-16
EP3426675A4 (en) 2019-10-16
US20230279049A1 (en) 2023-09-07
EP3426675B1 (en) 2020-08-05
US20190382442A1 (en) 2019-12-19
US20210047368A1 (en) 2021-02-18
WO2017156403A1 (en) 2017-09-14
US12252553B2 (en) 2025-03-18
US10683326B2 (en) 2020-06-16
US11555053B2 (en) 2023-01-17
JP2019512542A (ja) 2019-05-16

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