JP2016512526A - オナプリストン多形体及び使用方法 - Google Patents
オナプリストン多形体及び使用方法 Download PDFInfo
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- JP2016512526A JP2016512526A JP2016501305A JP2016501305A JP2016512526A JP 2016512526 A JP2016512526 A JP 2016512526A JP 2016501305 A JP2016501305 A JP 2016501305A JP 2016501305 A JP2016501305 A JP 2016501305A JP 2016512526 A JP2016512526 A JP 2016512526A
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- onapristone
- pharmaceutical composition
- ona
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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
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- 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
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- 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
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/569—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
-
- 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
-
- 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
- A61P15/18—Feminine contraceptives
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
- C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
-
- 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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Epoxy Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
本出願は、2013年3月12日に出願された米国特許仮出願第61/777,752号の優先権の利益を主張する。上記参照出願は、全て言い換えられるかのように、参照によりここに組み込まれる。
Claims (20)
- 図3の高分解能粉末X線回折パターンを特徴とする、オナプリストン結晶形体。
- 図4の粉末X線回折パターンを特徴とする、オナプリストン結晶形体。
- 図7の高分解能粉末X線回折パターンを特徴とする、オナプリストン結晶形体。
- 図8の粉末X線回折パターンを特徴とする、オナプリストン結晶形体。
- 図11の高分解能粉末X線回折パターンを特徴とする、オナプリストン結晶形体。
- 図12の粉末X線回折パターンを特徴とする、オナプリストン結晶形体。
- 図13の粉末X線回折パターンを特徴とする、オナプリストン結晶形体。
- 図14の粉末X線回折パターンを特徴とする、オナプリストン結晶形体。
- 請求項1〜8のいずれか一項に記載のオナプリストン結晶形体及び薬学的に許容される賦形剤、希釈剤、又は担体を含む薬剤組成物。
- 単位剤形中の、請求項9に記載の薬剤組成物。
- 単位剤形が錠剤、丸剤、カプセル剤、及びトローチ剤からなる群より選択される、請求項10に記載の薬剤組成物。
- オナプリストン結晶形体が約10〜約200mgの量で存在する、請求項9に記載の薬剤組成物。
- 少なくとも1つの追加活性薬剤をさらに含む、請求項9に記載の薬剤組成物。
- 追加活性薬剤が抗腫瘍剤、ホルモン、ステロイド、又はレチノイドからなる群より選択される、請求項13に記載の薬剤組成物。
- 追加活性薬剤がエベロリムス、トラスツズマブ、TM1-D、抗HER2薬、ベバシズマブ、パクリタキセル、ドセタキセル、タキサン、ドキソルビシン、リポソマールドキソルビシン、ペグ化リポソマールドキソルビシン、アントラサイクリン、アントラセンジオン、カルボプラチン、シスプラチン、5-FU、ゲムシタビン及びシクロホスファミドからなる群より選択される、請求項14に記載の薬剤組成物。
- 請求項9〜15に記載の薬剤組成物の治療有効量を、治療を必要とする哺乳動物に投与することを含む、哺乳動物を治療する方法。
- 治療有効量が約2.5mg〜約200mgである、請求項16に記載の方法。
- 薬剤組成物が経口、非経口、舌下、鼻腔内、髄腔内、局所、又は直腸からなる群より選択される投与経路により哺乳動物に投与される、請求項16に記載の方法。
- 哺乳動物が人間である、請求項16に記載の方法。
- オナプリストンと水、メタノール、エタノール、イソプロパノール、アセトン、ブタノン、2-, 酢酸エチル、ジオキサン、1,4-, tert-ブチルメチルエーテル、テトラヒドロフラン、アセトニトリル、クロロホルム、シクロヘキサン、n-ヘプタン、トルエン、キシレン、p-, クメン、アニソール、ギ酸エチル、及び酢酸ブチルからなる群より選択される溶媒とを混合させることを含む、オナプリストン多形体の製造法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361777752P | 2013-03-12 | 2013-03-12 | |
US61/777,752 | 2013-03-12 | ||
PCT/US2014/023651 WO2014164861A1 (en) | 2013-03-12 | 2014-03-11 | Onapristone polymorphic forms and methods of use |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2018090510A Division JP2018138594A (ja) | 2013-03-12 | 2018-05-09 | オナプリストン多形体及び使用方法 |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2016512526A true JP2016512526A (ja) | 2016-04-28 |
Family
ID=50774842
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016501305A Pending JP2016512526A (ja) | 2013-03-12 | 2014-03-11 | オナプリストン多形体及び使用方法 |
JP2018090510A Pending JP2018138594A (ja) | 2013-03-12 | 2018-05-09 | オナプリストン多形体及び使用方法 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2018090510A Pending JP2018138594A (ja) | 2013-03-12 | 2018-05-09 | オナプリストン多形体及び使用方法 |
Country Status (11)
Country | Link |
---|---|
US (2) | US9193757B2 (ja) |
EP (1) | EP2968364A1 (ja) |
JP (2) | JP2016512526A (ja) |
KR (1) | KR20150130359A (ja) |
CN (2) | CN113201042A (ja) |
AU (1) | AU2014248928B2 (ja) |
CA (1) | CA2904116C (ja) |
HK (1) | HK1218388A1 (ja) |
MX (1) | MX2015012142A (ja) |
RU (1) | RU2015137837A (ja) |
WO (1) | WO2014164861A1 (ja) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2016081383A1 (en) * | 2014-11-17 | 2016-05-26 | Arno Therapeutics, Inc. | Onapristone extended-release compositions and methods |
US10308676B2 (en) | 2015-09-25 | 2019-06-04 | Context Biopharma Inc. | Methods of making onapristone intermediates |
JP2019503353A (ja) | 2015-12-15 | 2019-02-07 | コンテキスト・バイオファーマ・インコーポレイテッド | 非晶質オナプリストン組成物およびそれを作製する方法 |
US20170266204A1 (en) * | 2016-03-21 | 2017-09-21 | Arno Therapeutics, Inc. | Onapristone metabolite compositions and methods |
WO2018102369A1 (en) * | 2016-11-30 | 2018-06-07 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
WO2023172909A1 (en) * | 2022-03-08 | 2023-09-14 | Context Biopharma Inc. | Compositions comprising anti-progestins and selective estrogen receptor modulators and methods of using the same |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS6041695A (ja) * | 1983-06-15 | 1985-03-05 | シエ−リング・アクチエンゲゼルシヤフト | 13α−アルキルゴナン、その製造方法及び該化合物を含有する、抗ゲスタ−ゲン作用を有する製剤製品 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4780461A (en) | 1983-06-15 | 1988-10-25 | Schering Aktiengesellschaft | 13α-alkyl-gonanes, their production, and pharmaceutical preparations containing same |
DE3822770A1 (de) | 1988-07-01 | 1990-01-04 | Schering Ag | 13-alkyl-11ss-phenylgonane |
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2014
- 2014-03-11 AU AU2014248928A patent/AU2014248928B2/en active Active
- 2014-03-11 US US14/203,814 patent/US9193757B2/en not_active Expired - Fee Related
- 2014-03-11 CN CN202110467985.9A patent/CN113201042A/zh active Pending
- 2014-03-11 CA CA2904116A patent/CA2904116C/en active Active
- 2014-03-11 CN CN201480014329.1A patent/CN105142644A/zh active Pending
- 2014-03-11 RU RU2015137837A patent/RU2015137837A/ru not_active Application Discontinuation
- 2014-03-11 WO PCT/US2014/023651 patent/WO2014164861A1/en active Application Filing
- 2014-03-11 EP EP14725930.3A patent/EP2968364A1/en not_active Withdrawn
- 2014-03-11 KR KR1020157027542A patent/KR20150130359A/ko not_active IP Right Cessation
- 2014-03-11 MX MX2015012142A patent/MX2015012142A/es unknown
- 2014-03-11 JP JP2016501305A patent/JP2016512526A/ja active Pending
-
2015
- 2015-03-18 US US14/661,382 patent/US20150231155A1/en not_active Abandoned
-
2016
- 2016-06-05 HK HK16106390.5A patent/HK1218388A1/zh unknown
-
2018
- 2018-05-09 JP JP2018090510A patent/JP2018138594A/ja active Pending
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS6041695A (ja) * | 1983-06-15 | 1985-03-05 | シエ−リング・アクチエンゲゼルシヤフト | 13α−アルキルゴナン、その製造方法及び該化合物を含有する、抗ゲスタ−ゲン作用を有する製剤製品 |
Non-Patent Citations (8)
Title |
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HANCOCK,B. C.,ET AL, JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 86, no. 1, JPN6014008491, 1997, pages 1 - 12, ISSN: 0003910612 * |
NEEF,G. ET AL: "New steroids with antiprogestational and antiglucocorticoid activities", STEROIDS, vol. 44, no. 4, JPN6017035107, 1984, pages 349 - 72, XP055129817, ISSN: 0003910606, DOI: 10.1016/S0039-128X(84)80027-6 * |
厚生労働省医薬局審査管理課長: "新医薬品の規格及び試験方法の設定について", 医薬審発第568号, JPN6015027393, 1 May 2001 (2001-05-01), ISSN: 0003910608 * |
小嶌隆史: "医薬品開発における結晶性選択の効率化を目指して", 薬剤学, vol. 68, no. 5, JPN6009053757, 1 September 2008 (2008-09-01), pages 344 - 349, ISSN: 0003910609 * |
山野光久: "医薬品のプロセス研究における結晶多形現象への取り組み", 有機合成化学協会誌, vol. 65, no. 9, JPN6010003277, 1 September 2007 (2007-09-01), pages 907 - 69, ISSN: 0003910613 * |
川口洋子ら: "医薬品と結晶多形", 生活工学研究, vol. Voo.4, No.2, JPN6015027394, 2002, pages 310 - 7, ISSN: 0003910607 * |
平山令明, 有機化合物結晶作製ハンドブック, JPN6014035600, 2008, pages 17 - 23, ISSN: 0003910611 * |
芹澤一英, 医薬品の多形現象と晶析の科学, JPN6015027444, 2002, pages 273 - 278, ISSN: 0003910610 * |
Also Published As
Publication number | Publication date |
---|---|
MX2015012142A (es) | 2016-01-15 |
HK1218388A1 (zh) | 2017-02-17 |
CA2904116C (en) | 2021-09-14 |
US20140271819A1 (en) | 2014-09-18 |
JP2018138594A (ja) | 2018-09-06 |
US20150231155A1 (en) | 2015-08-20 |
CN113201042A (zh) | 2021-08-03 |
US9193757B2 (en) | 2015-11-24 |
EP2968364A1 (en) | 2016-01-20 |
KR20150130359A (ko) | 2015-11-23 |
WO2014164861A1 (en) | 2014-10-09 |
AU2014248928A1 (en) | 2015-09-24 |
RU2015137837A (ru) | 2017-04-18 |
AU2014248928B2 (en) | 2018-12-06 |
CA2904116A1 (en) | 2014-10-09 |
CN105142644A (zh) | 2015-12-09 |
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