CN111328280A - 制备和使用内昔芬的方法 - Google Patents
制备和使用内昔芬的方法 Download PDFInfo
- Publication number
- CN111328280A CN111328280A CN201880072905.6A CN201880072905A CN111328280A CN 111328280 A CN111328280 A CN 111328280A CN 201880072905 A CN201880072905 A CN 201880072905A CN 111328280 A CN111328280 A CN 111328280A
- Authority
- CN
- China
- Prior art keywords
- composition
- endoxifen
- formula
- endoxifene
- compound
- 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
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
- C07C217/14—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
- C07C217/18—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
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- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/10—Separation; Purification; Stabilisation; Use of additives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- C07B2200/09—Geometrical 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)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Endocrinology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Dental Preparations (AREA)
- Primary Cells (AREA)
- Paper (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202310795504.6A CN116832020A (zh) | 2017-09-11 | 2018-09-10 | 制备和使用内昔芬的方法 |
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762556884P | 2017-09-11 | 2017-09-11 | |
| US201762556799P | 2017-09-11 | 2017-09-11 | |
| US62/556,799 | 2017-09-11 | ||
| US62/556,884 | 2017-09-11 | ||
| US201862624787P | 2018-01-31 | 2018-01-31 | |
| US62/624,787 | 2018-01-31 | ||
| US201862693885P | 2018-07-03 | 2018-07-03 | |
| US62/693,885 | 2018-07-03 | ||
| PCT/US2018/050272 WO2019051416A1 (en) | 2017-09-11 | 2018-09-10 | METHODS FOR THE MANUFACTURE AND USE OF ENDOXIFEN |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202310795504.6A Division CN116832020A (zh) | 2017-09-11 | 2018-09-10 | 制备和使用内昔芬的方法 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN111328280A true CN111328280A (zh) | 2020-06-23 |
Family
ID=65635248
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880072905.6A Pending CN111328280A (zh) | 2017-09-11 | 2018-09-10 | 制备和使用内昔芬的方法 |
| CN202310795504.6A Pending CN116832020A (zh) | 2017-09-11 | 2018-09-10 | 制备和使用内昔芬的方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202310795504.6A Pending CN116832020A (zh) | 2017-09-11 | 2018-09-10 | 制备和使用内昔芬的方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (12) | US11261151B2 (enExample) |
| EP (1) | EP3681491A4 (enExample) |
| JP (3) | JP7766316B2 (enExample) |
| KR (3) | KR20260048646A (enExample) |
| CN (2) | CN111328280A (enExample) |
| AU (3) | AU2018329202B2 (enExample) |
| CA (1) | CA3073836A1 (enExample) |
| IL (3) | IL272924B2 (enExample) |
| MX (1) | MX2020002649A (enExample) |
| SG (1) | SG11202002105WA (enExample) |
| TW (2) | TWI878810B (enExample) |
| WO (1) | WO2019051416A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113975279A (zh) * | 2021-10-13 | 2022-01-28 | 复旦大学附属肿瘤医院 | 维拉佐酮及其衍生物在制备抗肿瘤药物中的应用 |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3681491A4 (en) | 2017-09-11 | 2021-06-30 | Atossa Therapeutics, Inc. | PROCESS FOR MANUFACTURING AND USE OF ENDOXIFES |
| WO2021003433A1 (en) * | 2019-07-03 | 2021-01-07 | Atossa Therapeutics, Inc. | Sustained release compositions of endoxifen |
| CN110564962B (zh) * | 2019-10-14 | 2020-12-22 | 中南大学 | 一种黑白钨混合矿的冶炼方法 |
| IL314075A (en) * | 2022-01-12 | 2024-09-01 | Atossa Therapeutics Inc | Compositions of (Z)-endoxifen and methods for their enrichment |
| EP4514327A1 (en) * | 2022-04-26 | 2025-03-05 | Atossa Therapeutics, Inc. | High dose endoxifen formulations and methods of use |
| AU2024294879A1 (en) * | 2023-07-19 | 2026-01-22 | Atossa Therapeutics, Inc. | Endoxifen compositions and methods of use thereof and synthesis thereof |
| AU2024409147A1 (en) | 2023-12-18 | 2026-06-25 | Atossa Therapeutics, Inc. | Oral formulations of (z)-endoxifen and methods of use thereof |
| AU2025207748A1 (en) | 2024-01-08 | 2026-07-02 | Atossa Therapeutics, Inc. | Endoxifen for treatment of rare cancers |
| WO2025207636A1 (en) | 2024-03-25 | 2025-10-02 | Atossa Therapeutics, Inc. | Endoxifen for treating duchenne muscular dystrophy |
Citations (6)
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| CN101891635A (zh) * | 2009-05-21 | 2010-11-24 | 扬子江药业集团有限公司 | 枸橼酸他莫昔芬的晶型及晶型a的制备方法 |
| CN102448467A (zh) * | 2009-05-27 | 2012-05-09 | 利西拉公司 | 治疗局部脂肪组织的给药方法和制剂 |
| WO2014141292A2 (en) * | 2013-03-04 | 2014-09-18 | Intas Pharmaceuticals Limited | Endoxifen citrate polymorph and process for preparing the same |
| CN105579044A (zh) * | 2013-05-31 | 2016-05-11 | 德玛医药 | 双脱水半乳糖醇及其类似物与衍生物用于治疗复发性恶性神经胶瘤或进行性继发脑瘤的用途 |
| WO2017070651A1 (en) * | 2015-10-22 | 2017-04-27 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Process for preparing (z)-endoxifen of high purity |
| WO2017080770A1 (de) * | 2015-11-10 | 2017-05-18 | Robert Bosch Gesellschaft Für Medizinische Forschung Mbh | Synthese von (z)-endoxifenhydrochlorid |
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