JP6013911B2 - 9e−15−(2−ピロリジン−1−イル−エトキシ)−7,12,25−トリオキサ−19,21,24−トリアザ−テトラシクロ[18.3.1.1(2,5).1(14,18)]ヘキサコサ−1(24),2,4,9,14,16,18(26),20,22−ノナエンのクエン酸塩 - Google Patents
9e−15−(2−ピロリジン−1−イル−エトキシ)−7,12,25−トリオキサ−19,21,24−トリアザ−テトラシクロ[18.3.1.1(2,5).1(14,18)]ヘキサコサ−1(24),2,4,9,14,16,18(26),20,22−ノナエンのクエン酸塩 Download PDFInfo
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- JP6013911B2 JP6013911B2 JP2012520571A JP2012520571A JP6013911B2 JP 6013911 B2 JP6013911 B2 JP 6013911B2 JP 2012520571 A JP2012520571 A JP 2012520571A JP 2012520571 A JP2012520571 A JP 2012520571A JP 6013911 B2 JP6013911 B2 JP 6013911B2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Description
上述のように、今や、9E−15−(2−ピロリジン−1−イル−エトキシ)−7,12,25−トリオキサ−19,21,24−トリアザ−テトラシクロ[18.3.1.1(2,5).1(14,18)]ヘキサコサ−1(24),2,4,9,14,16,18(26),20,22−ノナエンの特定の塩類が、単一の頑丈な多形体として存在することがわかった。特に、本出願人は、この化合物のクエン酸塩が、単一の多形体として存在することを見出した。
○角度範囲:2〜42°2θ
○ステップサイズ:0.05°2θ
○収集時間:0.5秒/ステップ
Claims (13)
- X線回折において、2シータスケールで、22.4o±0.5oでピークを示す、9E−15−(2−ピロリジン−1−イル−エトキシ)−7,12,25−トリオキサ−19,21,24−トリアザ−テトラシクロ[18.3.1.1(2,5).1(14,18)]ヘキサコサ−1(24),2,4,9,14,16,18(26),20,22−ノナエンのクエン酸塩の結晶。
- 塩が1:1塩である、請求項1記載のクエン酸塩の結晶。
- X線回折において、2シータスケールで、10.0°±0.5°、15.6°±0.5°及び17.2°±0.5°でもピークを示す請求項1記載のクエン酸塩の結晶。
- X線回折において、2シータスケールで、7.9°±0.5°、10.0°±0.5°、15.6°±0.5°、15.9°±0.5°、16.8°±0.5°、17.2°±0.5°、21.1°±0.5°及び22.4°±0.5°からなる群より選択される、少なくとも4つのピークを示す、請求項1〜3のいずれか一項記載のクエン酸塩の結晶。
- X線回折において、2シータスケールで、7.9°±0.5°、10.0°±0.5°、15.6°±0.5°、15.9°±0.5°、16.8°±0.5°、17.2°±0.5°、21.1°±0.5°及び22.4°±0.5°からなる群より選択される、少なくとも6つのピークを示す、請求項4記載のクエン酸塩の結晶。
- X線回折において、2シータスケールで、7.9°±0.5°、10.0°±0.5°、15.6°±0.5°、15.9°±0.5°、16.8°±0.5°、17.2°±0.5°、21.1°±0.5°及び22.4°±0.5°でピークを示す、請求項5記載のクエン酸塩の結晶。
- X線回折において、2シータスケールで、11.1°±0.5°、18.1°±0.5°、21.8°±0.5°、23.2°±0.5°及び27.6°±0.5°でもピークを示す、請求項6記載のクエン酸塩の結晶。
- X線回折において、2シータスケールで、7.0°±0.5°、14.0°±0.5°、19.0°±0.5°、19.8°±0.5°、23.6°±0.5°、24.3°±0.5°、25.2°±0.5°、25.7°±0.5°、26.1°±0.5°、26.5°±0.5°及び32.1°±0.5°でもピークを示す、請求項6記載のクエン酸塩の結晶。
- 請求項1〜8のいずれか一項記載のクエン酸塩の結晶を含む、医薬組成物。
- 増殖性障害を治療又は予防するための、請求項9記載の医薬組成物。
- 増殖性障害が癌である、請求項10記載の医薬組成物。
- 増殖性障害を治療又は予防するための薬剤の製造における、請求項1〜8のいずれか一項記載のクエン酸塩の結晶の使用。
- 増殖性障害が癌である、請求項12記載の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22560909P | 2009-07-15 | 2009-07-15 | |
US61/225,609 | 2009-07-15 | ||
PCT/SG2010/000265 WO2011008172A1 (en) | 2009-07-15 | 2010-07-14 | 9e-15-(2-pyrrolidin-1-yl-ethoxy)-7,12,25-trioxa-19,21,24-triaza- tetracyclo[18.3.1.1(2,5).1(14)18)]hexacosa-1(24),2,4,9,14,16,18(26),20,22-nonaene citrate salt |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015094972A Division JP2015164941A (ja) | 2009-07-15 | 2015-05-07 | 9e−15−(2−ピロリジン−1−イル−エトキシ)−7,12,25−トリオキサ−19,21,24−トリアザ−テトラシクロ[18.3.1.1(2,5).1(14,18)]ヘキサコサ−1(24),2,4,9,14,16,18(26),20,22−ノナエンのクエン酸塩 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2012533539A JP2012533539A (ja) | 2012-12-27 |
JP2012533539A5 JP2012533539A5 (ja) | 2013-08-29 |
JP6013911B2 true JP6013911B2 (ja) | 2016-10-25 |
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Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2012520571A Active JP6013911B2 (ja) | 2009-07-15 | 2010-07-14 | 9e−15−(2−ピロリジン−1−イル−エトキシ)−7,12,25−トリオキサ−19,21,24−トリアザ−テトラシクロ[18.3.1.1(2,5).1(14,18)]ヘキサコサ−1(24),2,4,9,14,16,18(26),20,22−ノナエンのクエン酸塩 |
JP2015094972A Pending JP2015164941A (ja) | 2009-07-15 | 2015-05-07 | 9e−15−(2−ピロリジン−1−イル−エトキシ)−7,12,25−トリオキサ−19,21,24−トリアザ−テトラシクロ[18.3.1.1(2,5).1(14,18)]ヘキサコサ−1(24),2,4,9,14,16,18(26),20,22−ノナエンのクエン酸塩 |
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JP2015094972A Pending JP2015164941A (ja) | 2009-07-15 | 2015-05-07 | 9e−15−(2−ピロリジン−1−イル−エトキシ)−7,12,25−トリオキサ−19,21,24−トリアザ−テトラシクロ[18.3.1.1(2,5).1(14,18)]ヘキサコサ−1(24),2,4,9,14,16,18(26),20,22−ノナエンのクエン酸塩 |
Country Status (19)
Country | Link |
---|---|
US (1) | US9062074B2 (ja) |
EP (1) | EP2454266B1 (ja) |
JP (2) | JP6013911B2 (ja) |
CN (1) | CN102762577B (ja) |
AR (2) | AR077483A1 (ja) |
BR (1) | BR112012000750B1 (ja) |
CA (1) | CA2768210C (ja) |
DK (1) | DK2454266T3 (ja) |
ES (1) | ES2429525T3 (ja) |
HK (1) | HK1178159A1 (ja) |
HR (1) | HRP20130941T1 (ja) |
MX (1) | MX2012000680A (ja) |
PL (1) | PL2454266T3 (ja) |
PT (1) | PT2454266E (ja) |
RU (1) | RU2543721C2 (ja) |
SI (1) | SI2454266T1 (ja) |
SM (1) | SMT201300112B (ja) |
TW (1) | TWI537276B (ja) |
WO (1) | WO2011008172A1 (ja) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3247362A4 (en) | 2014-11-17 | 2018-10-10 | Context Biopharma Inc. | Onapristone extended-release compositions and methods |
AU2016326657B2 (en) | 2015-09-25 | 2019-10-24 | Context Biopharma, Inc. | Methods of making onapristone intermediates |
KR20180113988A (ko) | 2015-12-15 | 2018-10-17 | 컨텍스트 바이오파마 인코포레이티드 | 비정질 오나프리스톤 조성물 및 그 제조방법 |
WO2018102369A1 (en) | 2016-11-30 | 2018-06-07 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
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MY110603A (en) * | 1993-05-27 | 1998-08-29 | Novartis Ag | Tetrahydropyran derivatives |
WO2004078682A2 (en) | 2003-03-05 | 2004-09-16 | Irm Llc | Cyclic compounds and compositions as protein kinase inhibitors |
JP5380073B2 (ja) * | 2005-11-16 | 2014-01-08 | エス*バイオ プライベート リミティッド | ヘテロアルキル結合ピリミジン誘導体 |
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2010
- 2010-07-14 RU RU2012105044/04A patent/RU2543721C2/ru active
- 2010-07-14 CN CN201080032627.5A patent/CN102762577B/zh active Active
- 2010-07-14 SI SI201030347T patent/SI2454266T1/sl unknown
- 2010-07-14 CA CA2768210A patent/CA2768210C/en active Active
- 2010-07-14 EP EP10737645.1A patent/EP2454266B1/en active Active
- 2010-07-14 JP JP2012520571A patent/JP6013911B2/ja active Active
- 2010-07-14 ES ES10737645T patent/ES2429525T3/es active Active
- 2010-07-14 WO PCT/SG2010/000265 patent/WO2011008172A1/en active Application Filing
- 2010-07-14 DK DK10737645.1T patent/DK2454266T3/da active
- 2010-07-14 US US13/384,139 patent/US9062074B2/en active Active
- 2010-07-14 BR BR112012000750-5A patent/BR112012000750B1/pt active IP Right Grant
- 2010-07-14 PL PL10737645T patent/PL2454266T3/pl unknown
- 2010-07-14 MX MX2012000680A patent/MX2012000680A/es active IP Right Grant
- 2010-07-14 PT PT107376451T patent/PT2454266E/pt unknown
- 2010-07-15 TW TW099123331A patent/TWI537276B/zh active
- 2010-07-15 AR ARP100102594A patent/AR077483A1/es not_active Application Discontinuation
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2013
- 2013-04-29 HK HK13105191.1A patent/HK1178159A1/xx unknown
- 2013-10-04 SM SM201300112T patent/SMT201300112B/xx unknown
- 2013-10-07 HR HRP20130941AT patent/HRP20130941T1/hr unknown
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2015
- 2015-05-07 JP JP2015094972A patent/JP2015164941A/ja active Pending
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2019
- 2019-08-05 AR ARP190102219A patent/AR114987A2/es unknown
Also Published As
Publication number | Publication date |
---|---|
US9062074B2 (en) | 2015-06-23 |
HRP20130941T1 (hr) | 2013-11-08 |
SI2454266T1 (sl) | 2013-10-30 |
JP2012533539A (ja) | 2012-12-27 |
CN102762577A (zh) | 2012-10-31 |
JP2015164941A (ja) | 2015-09-17 |
CA2768210A1 (en) | 2011-01-20 |
WO2011008172A1 (en) | 2011-01-20 |
BR112012000750A2 (pt) | 2016-08-09 |
PL2454266T3 (pl) | 2014-01-31 |
ES2429525T3 (es) | 2013-11-15 |
TWI537276B (zh) | 2016-06-11 |
EP2454266A1 (en) | 2012-05-23 |
MX2012000680A (es) | 2012-02-28 |
SMT201300112B (it) | 2013-11-08 |
PT2454266E (pt) | 2013-10-10 |
CA2768210C (en) | 2017-08-15 |
US20120196876A1 (en) | 2012-08-02 |
TW201107336A (en) | 2011-03-01 |
BR112012000750A8 (pt) | 2018-02-06 |
DK2454266T3 (da) | 2013-09-08 |
BR112012000750B1 (pt) | 2021-05-25 |
RU2543721C2 (ru) | 2015-03-10 |
AR077483A1 (es) | 2011-08-31 |
AR114987A2 (es) | 2020-11-11 |
CN102762577B (zh) | 2015-01-07 |
EP2454266B1 (en) | 2013-07-10 |
HK1178159A1 (en) | 2013-09-06 |
RU2012105044A (ru) | 2013-08-20 |
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