EA201892566A1 - Кристаллический полиморф 15в-гидрокси-осатерона ацетата - Google Patents
Кристаллический полиморф 15в-гидрокси-осатерона ацетатаInfo
- Publication number
- EA201892566A1 EA201892566A1 EA201892566A EA201892566A EA201892566A1 EA 201892566 A1 EA201892566 A1 EA 201892566A1 EA 201892566 A EA201892566 A EA 201892566A EA 201892566 A EA201892566 A EA 201892566A EA 201892566 A1 EA201892566 A1 EA 201892566A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- hydroxy
- acetate
- osateron
- polymorphic form
- crystalline polymorphic
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 title 1
- PUVIUQNYQQPAQB-LZGXPLDUSA-N [(1r,3r,3as,3br,9ar,9bs,11as)-1-acetyl-5-chloro-3-hydroxy-9a,11a-dimethyl-7-oxo-2,3,3a,3b,9,9b,10,11-octahydroindeno[4,5-h]isochromen-1-yl] acetate Chemical compound C1=C(Cl)C2=CC(=O)OC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1[C@H](O)C[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 PUVIUQNYQQPAQB-LZGXPLDUSA-N 0.000 abstract 2
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 230000008018 melting Effects 0.000 abstract 1
- 238000002844 melting Methods 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 238000001228 spectrum Methods 0.000 abstract 1
Classifications
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
- C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
- C07J73/003—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by oxygen as hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Представлена кристаллическая полиморфная форма A 15β-гидрокси-осатерона ацетата, обладающая улучшенной стабильностью (стабильностью при хранении, стабильностью при тонком измельчении и характеристиками абсорбции). В спектре порошковой рентгеновской дифракции характеристические дифракционные пики кристаллической полиморфной формы A 15β-гидрокси-осатерона ацетата присутствуют при углах дифракции 2θ 9,6±0,2°, 17,1±0,2° и 20,2±0,2°. Кристаллическая полиморфная форма A имеет температуру плавления 280-283°C и представляет собой призматический кристалл.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2016095382 | 2016-05-11 | ||
| PCT/JP2017/017619 WO2017195804A1 (ja) | 2016-05-11 | 2017-05-10 | 15β-ヒドロキシ-酢酸オサテロンの結晶多形 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201892566A1 true EA201892566A1 (ru) | 2019-04-30 |
| EA034965B1 EA034965B1 (ru) | 2020-04-13 |
Family
ID=60267316
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201892566A EA034965B1 (ru) | 2016-05-11 | 2017-05-10 | Кристаллический полиморф 15бета-гидроксиосатерона ацетата |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10508130B2 (ru) |
| EP (1) | EP3456729B1 (ru) |
| JP (2) | JP7210278B2 (ru) |
| KR (1) | KR102383617B1 (ru) |
| CN (1) | CN109153701B (ru) |
| AU (1) | AU2017264187B2 (ru) |
| CA (1) | CA3021179C (ru) |
| EA (1) | EA034965B1 (ru) |
| ES (1) | ES2829578T3 (ru) |
| MX (1) | MX374533B (ru) |
| MY (1) | MY195203A (ru) |
| PH (1) | PH12018502365A1 (ru) |
| SG (1) | SG11201809127PA (ru) |
| WO (1) | WO2017195804A1 (ru) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2017264187B2 (en) * | 2016-05-11 | 2021-02-18 | Aska Pharmaceutical Co., Ltd. | Crystalline polymorph of 15β-hydroxy-osaterone acetate |
| EP4039328A4 (en) * | 2019-10-02 | 2023-10-25 | ASKA Pharmaceutical Co., Ltd. | Dysuria-alleviating agent |
| WO2021065027A1 (ja) * | 2019-10-02 | 2021-04-08 | あすか製薬株式会社 | 排尿障害改善剤 |
| US20220110238A1 (en) | 2020-10-09 | 2022-04-14 | Deere & Company | Machine control using a predictive map |
| WO2022131354A1 (ja) * | 2020-12-18 | 2022-06-23 | あすか製薬株式会社 | 固形製剤 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61204199A (ja) * | 1985-03-07 | 1986-09-10 | Teikoku Hormone Mfg Co Ltd | 2−アザプレグナン化合物 |
| EP0193871B1 (en) | 1985-03-07 | 1989-05-31 | Teikoku Hormone Mfg. Co., Ltd. | 2-oxa- or aza-pregnane compounds |
| JPS61204198A (ja) * | 1985-03-07 | 1986-09-10 | Teikoku Hormone Mfg Co Ltd | 2−オキサプレグナン化合物 |
| JPS62195398A (ja) * | 1986-02-21 | 1987-08-28 | Teikoku Hormone Mfg Co Ltd | 黄体ホルモン剤 |
| JP2591640B2 (ja) * | 1988-02-04 | 1997-03-19 | 帝国臓器製薬株式会社 | 新規な2−オキサプレグナン化合物 |
| JP2980992B2 (ja) * | 1990-12-28 | 1999-11-22 | 帝国臓器製薬株式会社 | 6−ハロゲノ−2−オキサプレグナ−4,6−ジエン−3−オン化合物の製造方法 |
| JP2591640Y2 (ja) | 1993-05-13 | 1999-03-10 | 株式会社吉野工業所 | 液体収納袋 |
| AU2017264187B2 (en) * | 2016-05-11 | 2021-02-18 | Aska Pharmaceutical Co., Ltd. | Crystalline polymorph of 15β-hydroxy-osaterone acetate |
-
2017
- 2017-05-10 AU AU2017264187A patent/AU2017264187B2/en active Active
- 2017-05-10 WO PCT/JP2017/017619 patent/WO2017195804A1/ja not_active Ceased
- 2017-05-10 KR KR1020187035313A patent/KR102383617B1/ko active Active
- 2017-05-10 US US16/095,782 patent/US10508130B2/en active Active
- 2017-05-10 ES ES17796164T patent/ES2829578T3/es active Active
- 2017-05-10 CN CN201780028401.XA patent/CN109153701B/zh active Active
- 2017-05-10 EP EP17796164.6A patent/EP3456729B1/en active Active
- 2017-05-10 MY MYPI2018001883A patent/MY195203A/en unknown
- 2017-05-10 CA CA3021179A patent/CA3021179C/en active Active
- 2017-05-10 MX MX2018013786A patent/MX374533B/es active IP Right Grant
- 2017-05-10 SG SG11201809127PA patent/SG11201809127PA/en unknown
- 2017-05-10 EA EA201892566A patent/EA034965B1/ru not_active IP Right Cessation
- 2017-05-10 JP JP2018517047A patent/JP7210278B2/ja active Active
-
2018
- 2018-11-09 PH PH12018502365A patent/PH12018502365A1/en unknown
-
2021
- 2021-06-04 JP JP2021094176A patent/JP7241807B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| PH12018502365A1 (en) | 2019-09-09 |
| MX2018013786A (es) | 2019-03-28 |
| EA034965B1 (ru) | 2020-04-13 |
| EP3456729A1 (en) | 2019-03-20 |
| MX374533B (es) | 2025-03-06 |
| JP7210278B2 (ja) | 2023-01-23 |
| WO2017195804A1 (ja) | 2017-11-16 |
| MY195203A (en) | 2023-01-11 |
| JP7241807B2 (ja) | 2023-03-17 |
| US20190127417A1 (en) | 2019-05-02 |
| CA3021179A1 (en) | 2017-11-16 |
| SG11201809127PA (en) | 2018-11-29 |
| BR112018071950A2 (pt) | 2019-02-05 |
| ES2829578T3 (es) | 2021-06-01 |
| EP3456729B1 (en) | 2020-09-02 |
| AU2017264187B2 (en) | 2021-02-18 |
| EP3456729A4 (en) | 2019-05-22 |
| US10508130B2 (en) | 2019-12-17 |
| KR20190004787A (ko) | 2019-01-14 |
| AU2017264187A1 (en) | 2018-11-15 |
| JP2021121645A (ja) | 2021-08-26 |
| CN109153701A (zh) | 2019-01-04 |
| KR102383617B1 (ko) | 2022-04-05 |
| JPWO2017195804A1 (ja) | 2019-03-07 |
| CN109153701B (zh) | 2021-02-02 |
| CA3021179C (en) | 2024-07-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM |