CN112437766A - 制备贝派地酸及其组合物的方法 - Google Patents

制备贝派地酸及其组合物的方法 Download PDF

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Publication number
CN112437766A
CN112437766A CN202080003150.1A CN202080003150A CN112437766A CN 112437766 A CN112437766 A CN 112437766A CN 202080003150 A CN202080003150 A CN 202080003150A CN 112437766 A CN112437766 A CN 112437766A
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formula
compound
hours
pharmaceutical material
certain embodiments
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Chinese (zh)
Inventor
R.科普
M.阿布德尔纳瑟
C.M.西马鲁斯蒂
J.莱恩
M.巴克曼
R.阿明
A.J.库珀
D.戈帕尔
P.塞利格
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Esperion Therapeutics Inc
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Esperion Therapeutics Inc
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Application filed by Esperion Therapeutics Inc filed Critical Esperion Therapeutics Inc
Priority to CN202211022415.XA priority Critical patent/CN115429784A/zh
Publication of CN112437766A publication Critical patent/CN112437766A/zh
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    • 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

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  • Chemical & Material Sciences (AREA)
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  • 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)
CN202080003150.1A 2019-06-21 2020-06-19 制备贝派地酸及其组合物的方法 Pending CN112437766A (zh)

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Applications Claiming Priority (3)

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US201962864873P 2019-06-21 2019-06-21
US62/864,873 2019-06-21
PCT/US2020/038622 WO2020257571A1 (en) 2019-06-21 2020-06-19 Methods of making bempedoic acid and compositions of the same

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CN202080003150.1A Pending CN112437766A (zh) 2019-06-21 2020-06-19 制备贝派地酸及其组合物的方法
CN202211022415.XA Pending CN115429784A (zh) 2019-06-21 2020-06-19 制备贝派地酸及其组合物的方法
CN202080003148.4A Pending CN112437765A (zh) 2019-06-21 2020-06-19 贝派地酸的盐形式及其使用方法

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CN202080003148.4A Pending CN112437765A (zh) 2019-06-21 2020-06-19 贝派地酸的盐形式及其使用方法

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US (10) US12344578B2 (enExample)
EP (3) EP3986860A1 (enExample)
JP (3) JP2022537049A (enExample)
KR (3) KR20220024816A (enExample)
CN (3) CN112437766A (enExample)
AU (3) AU2020295503A1 (enExample)
BR (2) BR112021025928A2 (enExample)
CA (2) CA3144372A1 (enExample)
ES (1) ES3032779T3 (enExample)
HU (1) HUE072061T2 (enExample)
IL (3) IL288909A (enExample)
MX (2) MX2021015936A (enExample)
WO (2) WO2020257571A1 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
CN114436837A (zh) * 2021-12-27 2022-05-06 甘李药业股份有限公司 一种贝派地酸中间体的纯化方法
CN115504914A (zh) * 2021-06-23 2022-12-23 武汉武药科技有限公司 一种贝派地酸中间体的制备方法

Families Citing this family (13)

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CA3144372A1 (en) 2019-06-21 2020-12-24 Esperion Therapeutics, Inc. Salt forms of bempedoic acid and methods for using the same
EP4038045A1 (en) 2019-10-03 2022-08-10 Synthon B.V. Crystalline forms of bempedoic acid
WO2021110929A1 (en) * 2019-12-06 2021-06-10 Synthon B.V. Crystalline forms of sodium salt of bempedoic acid
WO2021255180A1 (en) * 2020-06-19 2021-12-23 Synthon B.V. Salts of bempedoic acid
WO2022149161A1 (en) * 2021-01-05 2022-07-14 Dr. Reddy's Laboratories Limited Process for preparation of bempedoic acid and its intermediates
US20240366625A1 (en) 2021-06-02 2024-11-07 Esperion Therapeutics, Inc. Compositions containing and therapies using bempedoic acid and tolvaptan
WO2023187833A1 (en) * 2022-03-30 2023-10-05 Enaltec Labs Private Limited A novel salt of bempedoic acid
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
WO2025196153A1 (en) 2024-03-20 2025-09-25 Astrazeneca Ab Pcsk9 inhibitors and methods of use thereof
WO2025196154A1 (en) 2024-03-20 2025-09-25 Astrazeneca Ab Pcsk9 inhibitors and methods of use thereof
WO2025196155A1 (en) 2024-03-20 2025-09-25 Astrazeneca Ab Pcsk9 inhibitors and methods of use thereof
WO2025238159A1 (en) 2024-05-16 2025-11-20 Astrazeneca Ab Combination therapy comprising azd0780 and ezetimibe

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