BR112021025928A2 - Métodos de preparação de ácido bempedoico e composições do mesmo - Google Patents
Métodos de preparação de ácido bempedoico e composições do mesmoInfo
- Publication number
- BR112021025928A2 BR112021025928A2 BR112021025928A BR112021025928A BR112021025928A2 BR 112021025928 A2 BR112021025928 A2 BR 112021025928A2 BR 112021025928 A BR112021025928 A BR 112021025928A BR 112021025928 A BR112021025928 A BR 112021025928A BR 112021025928 A2 BR112021025928 A2 BR 112021025928A2
- Authority
- BR
- Brazil
- Prior art keywords
- compositions
- preparation methods
- methods
- acid preparation
- bempedoic acid
- Prior art date
Links
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)
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 |
|---|---|
| BR112021025928A2 true BR112021025928A2 (pt) | 2022-05-10 |
Family
ID=71528020
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112021025928A BR112021025928A2 (pt) | 2019-06-21 | 2020-06-19 | Métodos de preparação de ácido bempedoico e composições do mesmo |
| BR112021025964A BR112021025964A2 (pt) | 2019-06-21 | 2020-06-19 | Formas de sal de ácido bempedoico e métodos para uso das mesmas |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112021025964A BR112021025964A2 (pt) | 2019-06-21 | 2020-06-19 | Formas de sal de ácido bempedoico e métodos para uso das mesmas |
Country Status (13)
| Country | Link |
|---|---|
| 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) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| US20240366625A1 (en) | 2021-06-02 | 2024-11-07 | Esperion Therapeutics, Inc. | Compositions containing and therapies using bempedoic acid and tolvaptan |
| 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 |
| 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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| WO2019161307A1 (en) | 2018-02-16 | 2019-08-22 | Esperion Therapeutics, Inc. | Sustained release formulations of bempedoic acid |
| EP3666750A1 (en) * | 2018-12-10 | 2020-06-17 | Sandoz AG | Crystalline form of bempedoic acid |
| JP2022516530A (ja) * | 2018-12-31 | 2022-02-28 | ルピン・リミテッド | ベンペド酸の新規塩及び多形体 |
| CA3144372A1 (en) | 2019-06-21 | 2020-12-24 | Esperion Therapeutics, Inc. | Salt forms of bempedoic acid and methods for using the same |
| WO2021110929A1 (en) * | 2019-12-06 | 2021-06-10 | Synthon B.V. | Crystalline forms of sodium salt 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 |
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