ES3032779T3 - Methods of making bempedoic acid - Google Patents

Methods of making bempedoic acid

Info

Publication number
ES3032779T3
ES3032779T3 ES20737750T ES20737750T ES3032779T3 ES 3032779 T3 ES3032779 T3 ES 3032779T3 ES 20737750 T ES20737750 T ES 20737750T ES 20737750 T ES20737750 T ES 20737750T ES 3032779 T3 ES3032779 T3 ES 3032779T3
Authority
ES
Spain
Prior art keywords
compound
formula
hours
approximately
hour
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.)
Active
Application number
ES20737750T
Other languages
English (en)
Spanish (es)
Inventor
Richard Copp
Mohamed Abdelnasser
Christopher M Cimarusti
Jonathan Lane
Michael Barkman
Rasidul Amin
Arthur John Cooper
Damodaragounder Gopal
Philipp Selig
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.)
Esperion Therapeutics Inc
Original Assignee
Esperion Therapeutics Inc
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Application filed by Esperion Therapeutics Inc filed Critical Esperion Therapeutics Inc
Application granted granted Critical
Publication of ES3032779T3 publication Critical patent/ES3032779T3/es
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/04—Preparation of carboxylic acids or their salts, halides or anhydrides from carboxylic acid halides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C315/00—Preparation of sulfones; Preparation of sulfoxides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/36—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atoms of the amino groups bound to hydrogen atoms or to carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/09—Preparation of carboxylic acids or their salts, halides or anhydrides from carboxylic acid esters or lactones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/285—Polyhydroxy dicarboxylic acids having five or more carbon atoms, e.g. saccharic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/347—Saturated compounds containing more than one carboxyl group containing keto groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/307—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/31—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of functional groups containing oxygen only in singly bound form
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/313—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of doubly bound oxygen containing functional groups, e.g. carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/62—Halogen-containing esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/732—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/738—Esters of keto-carboxylic acids or aldehydo-carboxylic acids
    • 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)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
ES20737750T 2019-06-21 2020-06-19 Methods of making bempedoic acid Active ES3032779T3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962864873P 2019-06-21 2019-06-21
PCT/US2020/038622 WO2020257571A1 (en) 2019-06-21 2020-06-19 Methods of making bempedoic acid and compositions of the same

Publications (1)

Publication Number Publication Date
ES3032779T3 true ES3032779T3 (en) 2025-07-24

Family

ID=71528020

Family Applications (1)

Application Number Title Priority Date Filing Date
ES20737750T Active ES3032779T3 (en) 2019-06-21 2020-06-19 Methods of making bempedoic acid

Country Status (13)

Country Link
US (11) US12344578B2 (enExample)
EP (3) EP3986860A1 (enExample)
JP (4) JP2022537049A (enExample)
KR (3) KR20220024815A (enExample)
CN (3) CN112437765A (enExample)
AU (3) AU2020296094B2 (enExample)
BR (1) BR112021025964A2 (enExample)
CA (2) CA3243601A1 (enExample)
ES (1) ES3032779T3 (enExample)
HU (1) HUE072061T2 (enExample)
IL (3) IL288909A (enExample)
MX (2) MX2021015936A (enExample)
WO (2) WO2020257573A1 (enExample)

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CN112437765A (zh) 2019-06-21 2021-03-02 艾斯柏伦治疗公司 贝派地酸的盐形式及其使用方法
US12528759B2 (en) 2019-10-03 2026-01-20 Synthon B.V. Crystalline forms of bempedoic acid
EP4069668A1 (en) 2019-12-06 2022-10-12 Synthon B.V. Crystalline forms of sodium salt of bempedoic acid
CN111559961A (zh) * 2020-05-26 2020-08-21 杭州科巢生物科技有限公司 一种贝派地酸晶型及其制备方法
WO2021255180A1 (en) * 2020-06-19 2021-12-23 Synthon B.V. Salts of bempedoic acid
CN112521282A (zh) * 2020-12-02 2021-03-19 苏州汉德创宏生化科技有限公司 一种贝派地酸中间体及其合成方法
WO2022149161A1 (en) * 2021-01-05 2022-07-14 Dr. Reddy's Laboratories Limited Process for preparation of bempedoic acid and its intermediates
JP2024521354A (ja) 2021-06-02 2024-05-31 エスペリオン・セラピューティクス・インコーポレイテッド ベンペド酸とトルバブタンを含む組成物及びそれらを用いた治療方法
CN115504914B (zh) * 2021-06-23 2024-05-07 武汉武药科技有限公司 一种贝派地酸中间体的制备方法
CN114436837B (zh) * 2021-12-27 2024-02-20 甘李药业股份有限公司 一种贝派地酸中间体的纯化方法
WO2023187833A1 (en) * 2022-03-30 2023-10-05 Enaltec Labs Private Limited A novel salt of bempedoic acid
CN117551009A (zh) * 2022-08-05 2024-02-13 武汉武药科技有限公司 一种贝派地酸中间体的合成方法
WO2024151311A1 (en) 2023-01-09 2024-07-18 Esperion Therapeutics, Inc. Methods of treatment using bempedoic acid
CN116589341A (zh) * 2023-04-14 2023-08-15 苏州汉德创宏生化科技有限公司 一种抗高血酯药物中间体的制备方法
TW202602886A (zh) 2024-03-20 2026-01-16 瑞典商阿斯特捷利康公司 Pcsk9抑制劑及其使用方法
TW202539678A (zh) 2024-03-20 2025-10-16 瑞典商阿斯特捷利康公司 Pcsk9抑制劑及其使用方法
TW202602866A (zh) 2024-03-20 2026-01-16 瑞典商阿斯特捷利康公司 Pcsk9抑制劑及其使用方法
TW202612699A (zh) 2024-05-16 2026-04-01 瑞典商阿斯特捷利康公司 組合療法
WO2026125708A1 (en) 2024-12-12 2026-06-18 Krka, D.D., Novo Mesto Tablets comprising bempedoic acid or bempedoic acid and ezetimibe

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