CN109476700A - 结晶盐形式 - Google Patents

结晶盐形式 Download PDF

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Publication number
CN109476700A
CN109476700A CN201780029335.8A CN201780029335A CN109476700A CN 109476700 A CN109476700 A CN 109476700A CN 201780029335 A CN201780029335 A CN 201780029335A CN 109476700 A CN109476700 A CN 109476700A
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CN
China
Prior art keywords
crystalline form
compound
xrpd
values
following
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201780029335.8A
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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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Priority to CN202210620260.3A priority Critical patent/CN115160402A/zh
Publication of CN109476700A publication Critical patent/CN109476700A/zh
Pending legal-status Critical Current

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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
    • C07K5/08—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
    • 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
    • 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)
CN201780029335.8A 2016-03-11 2017-03-10 结晶盐形式 Pending CN109476700A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202210620260.3A CN115160402A (zh) 2016-03-11 2017-03-10 结晶盐形式

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662307095P 2016-03-11 2016-03-11
US62/307095 2016-03-11
PCT/US2017/021790 WO2017156403A1 (en) 2016-03-11 2017-03-10 Crystalline salt forms

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202210620260.3A Division CN115160402A (zh) 2016-03-11 2017-03-10 结晶盐形式

Publications (1)

Publication Number Publication Date
CN109476700A true CN109476700A (zh) 2019-03-15

Family

ID=59789873

Family Applications (2)

Application Number Title Priority Date Filing Date
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 Before (1)

Application Number Title Priority Date Filing Date
CN202210620260.3A Pending CN115160402A (zh) 2016-03-11 2017-03-10 结晶盐形式

Country Status (6)

Country Link
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
EP3426675B1 (en) 2016-03-11 2020-08-05 Stealth BioTherapeutics Inc. Crystalline salt forms
EP3606938A1 (en) 2017-04-05 2020-02-12 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
FI3774844T3 (fi) 2018-04-02 2023-04-04 Stealth Biotherapeutics Inc Elamipretidin synteesissä hyödyllisiä kiteisiä dipeptidejä

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102428086A (zh) * 2009-04-29 2012-04-25 内尔维阿诺医学科学有限公司 Cdk抑制剂的盐类
US20120178762A1 (en) * 2006-12-15 2012-07-12 Warner Chilcott Company, Llc Compositions of azimilide dihydrochloride
CN103003283A (zh) * 2010-06-09 2013-03-27 Abbvie公司 激酶抑制剂的结晶形式
CN103751763A (zh) * 2009-12-31 2014-04-30 康肽德生物医药技术有限公司 用于预防或治疗血管阻塞损伤的方法
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
WO2015060462A1 (en) * 2013-10-23 2015-04-30 Kaneka Corporation Tetrapeptide compound and method for producing same
WO2016007921A1 (en) * 2014-07-10 2016-01-14 Rhodel Island Hospital Treating arrhythmia with mitochondrial-targeted antioxidants

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Publication number Priority date Publication date Assignee Title
ATE136905T1 (de) * 1988-06-30 1996-05-15 Astra Ab Dermorphin-analoge, deren herstellungsverfahren, pharmazeutische zusammensetzungen und methode zur therapeutischen behandlung unter verwendung der analoge
ES2436011T3 (es) 2003-02-04 2013-12-26 Cornell Research Foundation, Inc. Métodos para prevenir la transición de la permeabilidad mitocondrial
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
WO2011025734A1 (en) 2009-08-24 2011-03-03 Stealth Peptides International, Inc. Methods and compositions for preventing or treating ophthalmic conditions
CA3008993A1 (en) * 2010-01-25 2011-07-28 Cornell University Aromatic-cationic peptides and uses of same
EP3040080A1 (en) * 2010-03-15 2016-07-06 Stealth Peptides International, Inc. Combination therapies using cyclosporine and aromatic cationic peptides
CN116474071A (zh) * 2013-03-01 2023-07-25 康德生物医疗有限公司 治疗线粒体疾病的方法
AU2014357545B2 (en) 2013-12-03 2018-10-25 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
US10112976B2 (en) * 2014-06-30 2018-10-30 Flamma S.P.A. Process for the production of D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide
WO2016004067A1 (en) * 2014-06-30 2016-01-07 Stealth Biotherapeutics Corp Aromatic-cationic peptide formulations, compositions and methods of use
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
EP3426675B1 (en) 2016-03-11 2020-08-05 Stealth BioTherapeutics Inc. Crystalline salt forms
WO2018034901A1 (en) * 2016-08-16 2018-02-22 Stealth Biotherapeutics N-carboxyanhydride-based-scale synthesis of elamipretide
EP3606938A1 (en) 2017-04-05 2020-02-12 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
FI3774844T3 (fi) * 2018-04-02 2023-04-04 Stealth Biotherapeutics Inc Elamipretidin synteesissä hyödyllisiä kiteisiä dipeptidejä

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120178762A1 (en) * 2006-12-15 2012-07-12 Warner Chilcott Company, Llc Compositions of azimilide dihydrochloride
CN102428086A (zh) * 2009-04-29 2012-04-25 内尔维阿诺医学科学有限公司 Cdk抑制剂的盐类
CN103751763A (zh) * 2009-12-31 2014-04-30 康肽德生物医药技术有限公司 用于预防或治疗血管阻塞损伤的方法
CN103003283A (zh) * 2010-06-09 2013-03-27 Abbvie公司 激酶抑制剂的结晶形式
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
WO2015060462A1 (en) * 2013-10-23 2015-04-30 Kaneka Corporation Tetrapeptide compound and method for producing same
WO2016007921A1 (en) * 2014-07-10 2016-01-14 Rhodel Island Hospital Treating arrhythmia with mitochondrial-targeted antioxidants

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
DAO-FU DAI 等: ""Mitochondrial Targeted Antioxidant Peptide Ameliorates Hypertensive Cardiomyopathy"", 《J AM COLL CARDIOL》 *
HANI N SABBAH 等: ""Chronic Therapy With Elamipretide (MTP-131), a Novel Mitochondria-Targeting Peptide, Improves Left Ventricular and Mitochondrial Function in Dogs With Advanced Heart Failure"", 《CIRC HEART FAIL》 *
HANI N. SABBAH 等: ""Long-term therapy with Bendavia (MTP-131), a novel mitochondria-targeting peptide, normalizes functional mitochondrial abnormalities in left ventricular myocardium of dogs with heart failure"", 《MITOCHONDRION》 *
YANG XUE-JIAO 等: ""Role of mitochondria in the pathogenesis and treatment of glaucoma"", 《中华医学杂志（英文版）》 *
周巧艳: ""靶向线粒体肽对碘造影剂致高胆固醇血症大鼠急性肾损伤的保护作用"", 《中国优秀硕士学位论文全文数据库(电子期刊) 医药卫生科技辑》 *

Also Published As

Publication number Publication date
WO2017156403A1 (en) 2017-09-14
US20230279049A1 (en) 2023-09-07
US12252553B2 (en) 2025-03-18
JP7038675B2 (ja) 2022-03-18
US11555053B2 (en) 2023-01-17
EP3426675A4 (en) 2019-10-16
CN115160402A (zh) 2022-10-11
CA3017359A1 (en) 2017-09-14
EP3426675A1 (en) 2019-01-16
US10683326B2 (en) 2020-06-16
EP3426675B1 (en) 2020-08-05
US20210047368A1 (en) 2021-02-18
US20190382442A1 (en) 2019-12-19
JP2019512542A (ja) 2019-05-16

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