CA3017359A1 - Crystalline salt forms - Google Patents

Crystalline salt forms Download PDF

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Publication number
CA3017359A1
CA3017359A1 CA3017359A CA3017359A CA3017359A1 CA 3017359 A1 CA3017359 A1 CA 3017359A1 CA 3017359 A CA3017359 A CA 3017359A CA 3017359 A CA3017359 A CA 3017359A CA 3017359 A1 CA3017359 A1 CA 3017359A1
Authority
CA
Canada
Prior art keywords
crystalline form
theta
pattern
compound
salt
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
CA3017359A
Other languages
English (en)
French (fr)
Inventor
Scott M. Duncan
Martin P. Redmon
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Stealth Biotherapeutics Inc
Original Assignee
Stealth Biotherapeutics Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Stealth Biotherapeutics Corp filed Critical Stealth Biotherapeutics Corp
Publication of CA3017359A1 publication Critical patent/CA3017359A1/en
Pending legal-status Critical Current

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Classifications

    • 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

Landscapes

  • 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)
CA3017359A 2016-03-11 2017-03-10 Crystalline salt forms Pending CA3017359A1 (en)

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 (1)

Publication Number Publication Date
CA3017359A1 true CA3017359A1 (en) 2017-09-14

Family

ID=59789873

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3017359A Pending CA3017359A1 (en) 2016-03-11 2017-03-10 Crystalline salt forms

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

Family Cites Families (23)

* Cited by examiner, † Cited by third party
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
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
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
PL3160985T3 (pl) * 2014-06-30 2021-12-27 Flamma S.P.A. Sposób wytwarzania d-arginylo-2,6-dimetylo-l-tyrozylo-l-lizylo-l-fenyloalaninoamidu
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

Also Published As

Publication number Publication date
EP3426675A1 (en) 2019-01-16
EP3426675A4 (en) 2019-10-16
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
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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