JP2006519255A - 17α−アセトキシ−11β−(4−N,N−ジメチルアミノフェニル)−19−ノルプレグナ−4,9−ジエン−3,20−ジオンの製造方法、その中間体及びそのような中間体の製造方法 - Google Patents
17α−アセトキシ−11β−(4−N,N−ジメチルアミノフェニル)−19−ノルプレグナ−4,9−ジエン−3,20−ジオンの製造方法、その中間体及びそのような中間体の製造方法 Download PDFInfo
- Publication number
- JP2006519255A JP2006519255A JP2006508726A JP2006508726A JP2006519255A JP 2006519255 A JP2006519255 A JP 2006519255A JP 2006508726 A JP2006508726 A JP 2006508726A JP 2006508726 A JP2006508726 A JP 2006508726A JP 2006519255 A JP2006519255 A JP 2006519255A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- producing
- norpregna
- molar amount
- 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
Links
- CRODSNSLNRWYAX-GUMHCPJTSA-N C[C@](CC1)(C(CC2)C(CC3)C1=C(CC1)C3=CC1=O)[C@]2(C(C)=O)O Chemical compound C[C@](CC1)(C(CC2)C(CC3)C1=C(CC1)C3=CC1=O)[C@]2(C(C)=O)O CRODSNSLNRWYAX-GUMHCPJTSA-N 0.000 description 2
- SBWHXJADQBBTGY-UJKMTWAASA-N C[C@](CC1)(C(CC2)C(CC3)C1=C(CC1)C3=CC1=O)[C@]2(C(C)=O)OC(C)=O Chemical compound C[C@](CC1)(C(CC2)C(CC3)C1=C(CC1)C3=CC1=O)[C@]2(C(C)=O)OC(C)=O SBWHXJADQBBTGY-UJKMTWAASA-N 0.000 description 1
- OOLLAFOLCSJHRE-BDQXMMFTSA-N C[C@](C[C@@H]1c(cc2)ccc2N(C)C)(C(CC2)C(CC3)C1=C(CC1)C3=CC1=O)[C@]2(C(C)=O)OC(C)=O Chemical compound C[C@](C[C@@H]1c(cc2)ccc2N(C)C)(C(CC2)C(CC3)C1=C(CC1)C3=CC1=O)[C@]2(C(C)=O)OC(C)=O OOLLAFOLCSJHRE-BDQXMMFTSA-N 0.000 description 1
- AZVGVNDMOMRAMV-GCCDOCAJSA-N C[C@](C[C@@H]1c(cc2)ccc2N(C)C)(C(CC2)C(CC3)C1=C(CCC1(C4)OCCO1)[C@@]34O)[C@]2(C(C)=O)OC(C)=O Chemical compound C[C@](C[C@@H]1c(cc2)ccc2N(C)C)(C(CC2)C(CC3)C1=C(CCC1(C4)OCCO1)[C@@]34O)[C@]2(C(C)=O)OC(C)=O AZVGVNDMOMRAMV-GCCDOCAJSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45109603P | 2003-02-28 | 2003-02-28 | |
| PCT/US2004/004246 WO2004078709A2 (en) | 2003-02-28 | 2004-02-13 | METHOD FOR PREPARING 17 α-ACETOXY-11β-(4-N,N-DIMETHYLAMINOPHENYL)-19-NORPREGNA-4,9-DIENE-3,20-DIONE, INTERMEDIATES THEREOF, AND METHODS FOR THE PREPARATION OF SUCH INTERMEDIATES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006519255A true JP2006519255A (ja) | 2006-08-24 |
| JP2006519255A5 JP2006519255A5 (enExample) | 2007-02-15 |
Family
ID=32962558
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006508726A Pending JP2006519255A (ja) | 2003-02-28 | 2004-02-13 | 17α−アセトキシ−11β−(4−N,N−ジメチルアミノフェニル)−19−ノルプレグナ−4,9−ジエン−3,20−ジオンの製造方法、その中間体及びそのような中間体の製造方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20060111577A1 (enExample) |
| EP (1) | EP1613640A4 (enExample) |
| JP (1) | JP2006519255A (enExample) |
| AU (1) | AU2004217988C1 (enExample) |
| CA (1) | CA2516319C (enExample) |
| WO (1) | WO2004078709A2 (enExample) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014050105A1 (en) | 2012-09-28 | 2014-04-03 | Aska Pharmaceutical Co., Ltd. | Amorphous ulipristal acetate |
| WO2014050106A1 (en) | 2012-09-28 | 2014-04-03 | Aska Pharmaceutical Co., Ltd. | Crystalline polymorphic form of ulipristal acetate |
| WO2014050107A1 (en) | 2012-09-28 | 2014-04-03 | Aska Pharmaceutical Co., Ltd. | Crystalline polymorphic form of ulipristal acetate |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2212912B1 (es) * | 2003-01-22 | 2005-10-01 | Crystal Pharma, S.A. | Procedimiento para la obtencion de 17alfa-acetoxi-11beta-(4-n,n-dimetilaminofenil)-19-norpregna-4,9-dien-3,20-diona. |
| HU227112B1 (hu) | 2006-06-14 | 2010-07-28 | Richter Gedeon Nyrt | Ipari eljárás 17-alfa-acetoxi-11-béta-[4-(N,N-dimetil-amino)-fenil]-19-norpregna-4,9-dién-3,20-dion elõállítására és új intermedierek az eljáráshoz |
| EP2211845B1 (en) | 2007-10-17 | 2017-02-22 | Laboratoire HRA Pharma | Glucocorticoid receptor antagonists such as mifepristone for treating cushing's syndrome |
| US8299050B2 (en) | 2008-01-29 | 2012-10-30 | Laboratoire Hra-Pharma | Method for treating uterine fibroids |
| US8512745B2 (en) | 2008-12-08 | 2013-08-20 | Laboratoire Hra Pharma | Ulipristal acetate tablets |
| RU2542779C2 (ru) | 2009-04-14 | 2015-02-27 | Лаборатуар Хра-Фарма | Способ контрацепции, используемый по мере необходимости |
| US8426392B2 (en) | 2009-12-09 | 2013-04-23 | Laboratoire Hra-Pharma | Method for providing emergency contraception |
| WO2011091890A1 (en) | 2010-02-01 | 2011-08-04 | Laboratoire Hra-Pharma | A method for post coital contraception in overweight for obese female subjects using ulipristal acetate |
| WO2011091892A1 (en) | 2010-02-01 | 2011-08-04 | Ulmann Andre | A method for late post coital contraception using ulipristal acetate |
| CN102241722B (zh) * | 2010-05-12 | 2015-11-25 | 杭州容立医药科技有限公司 | 一种合成孕酮受体调节剂优力司特的纯化方法 |
| EP2471537A1 (en) | 2010-12-30 | 2012-07-04 | PregLem S.A. | Treatment of pain associated with dislocation of basal endometrium |
| CN102516345B (zh) * | 2011-11-01 | 2014-11-26 | 上海优拓医药科技有限公司 | 醋酸乌利司他及其关键中间体的制备方法 |
| EP2545922A1 (en) | 2011-07-12 | 2013-01-16 | PregLem S.A. | Treatment of excessive menstrual bleeding associated with uterine fibroids |
| CN102295674B (zh) * | 2011-07-14 | 2013-04-10 | 四川大学 | 获得高纯度17α-乙酰氧基-11β-(4-N,N-二甲氨基苯基)-19-去甲孕甾-4,9-二烯-3,20-二酮的方法 |
| CN102344478B (zh) * | 2011-07-22 | 2013-08-07 | 上海希迈医药科技有限公司 | 一种17α-乙酰氧基-11β-(4-N,N-二甲氨基苯基)-19-去甲孕甾-4,9-二烯-3,20-二酮的结晶物及其制备方法 |
| CN102321141B (zh) * | 2011-07-22 | 2013-05-15 | 上海希迈医药科技有限公司 | 一种17α-乙酰氧基-11β-(4-N,N-二甲氨基苯基)-19-去甲孕甾-4,9-二烯-3,20-二酮的无定形物及其制备方法 |
| FR2987271B1 (fr) | 2012-02-28 | 2017-08-18 | Hra Pharma Lab | Combinaison de modulateurs selectifs du recepteur a la progesterone et d'anti-inflammatoires non steroidiens |
| EP2641602A1 (en) | 2012-03-23 | 2013-09-25 | PregLem S.A. | Method for treating gynecological diseases |
| CN103755765B (zh) * | 2012-04-17 | 2018-01-02 | 常州市第四制药厂有限公司 | 醋酸乌利司他的多晶型及其制备方法 |
| CN102675395B (zh) * | 2012-04-17 | 2014-04-30 | 常州市第四制药厂有限公司 | 醋酸乌利司他的多晶型及其制备方法 |
| WO2013175009A1 (en) | 2012-05-25 | 2013-11-28 | Laboratoire Hra-Pharma | Ulipristal acetate for prevention and treatment of breast tumors |
| CN102702296B (zh) * | 2012-06-19 | 2014-09-03 | 山东诚创医药技术开发有限公司 | 环-3,20-双(1,2-亚乙基缩醛)-17α-羟基-17β-乙酰基-雌甾-5(10),9(11)-二烯-3-酮的制备方法 |
| WO2014060888A1 (en) | 2012-10-18 | 2014-04-24 | Lupin Limited | Novel process and intermediate for preparation of ulipristal |
| CN102942612A (zh) * | 2012-10-30 | 2013-02-27 | 四川大学 | 一种合成醋酸乌利司他的新方法 |
| CN103804456B (zh) * | 2012-11-15 | 2017-08-04 | 上海创诺医药集团有限公司 | 醋酸乌利司他中间体及其制备方法 |
| JP2016516764A (ja) | 2013-04-10 | 2016-06-09 | プレグレム ソシエテ アノニム | 子宮筋腫治療に用いるプロゲステロン受容体調節剤 |
| HU230319B1 (hu) * | 2013-10-01 | 2016-01-28 | Richter Gedeon Nyrt. | Ipari eljárás szteroid hatóanyagok előállítására |
| MX391191B (es) | 2014-11-17 | 2025-03-21 | Context Biopharma Inc | Composiciones de liberación extendida de onapristona y métodos. |
| AU2016326657B2 (en) | 2015-09-25 | 2019-10-24 | Context Biopharma, Inc. | Methods of making onapristone intermediates |
| MX2018007154A (es) | 2015-12-15 | 2019-01-10 | Context Biopharma Inc | Composiciones de onapristona amorfa y metodos para hacer las mismas. |
| US20180148471A1 (en) | 2016-11-30 | 2018-05-31 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
| CN110028543B (zh) * | 2018-01-11 | 2024-04-12 | 上海汇伦医药股份有限公司 | 一种醋酸优力司特的制备方法 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3381003A (en) * | 1965-06-01 | 1968-04-30 | Merck & Co Inc | 3-keto-13beta-alkyl-17beta-acetyl-gona-4-ene-17alpha-ol compounds and processes of preparing them |
| US5929262A (en) * | 1995-03-30 | 1999-07-27 | The United States Of America As Represented By The Department Of Health And Human Services | Method for preparing 17α-acetoxy-11β-(4-N, N-dimethylaminophyl)-19-Norpregna-4,9-diene-3, 20-dione, intermediates useful in the method, and methods for the preparation of such intermediates |
| WO2001018025A2 (en) * | 1999-09-03 | 2001-03-15 | Research Triangle Institute | 17alpha propynyl 11-aryl steroids |
| JP2002505334A (ja) * | 1998-03-06 | 2002-02-19 | リサーチ・トライアングル・インスティチュート | アゴニスト又はアンタゴニストホルモン特性を有する20−ケト−11β−アリールステロイドとその誘導体 |
| JP2006515869A (ja) * | 2003-01-22 | 2006-06-08 | クリスタル、ファーマ、ソシエダッド、アノニマ | 17α−アセトキシ−11β−(4−N,N−ジメチルアミノフェニル)−19−ノルプレグナ−4,9−ジエン−3,20−ジオンを得る方法 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA8231B (en) * | 1981-01-09 | 1982-11-24 | Roussel Uclaf | New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained |
| FR2639045B2 (fr) * | 1982-03-01 | 1994-07-29 | Roussel Uclaf | Nouveaux produits derives de la structure 3-ceto-delta-4,9-19-nor steroides et leur application comme medicaments |
| FR2522328B1 (fr) * | 1982-03-01 | 1986-02-14 | Roussel Uclaf | Nouveaux produits derives de la structure 3-ceto 4,9 19-nor steroides, leur procede de preparation et leur application comme medicaments |
| FR2598421B1 (fr) * | 1986-05-06 | 1988-08-19 | Roussel Uclaf | Nouveaux produits 19-nor ou 19-nor d-homo steroides substitues en position 11b par un radical phenyle portant un radical alkynyle, leur procede de preparation, leur application comme medicaments et les compositions les renfermant |
| DE3761308D1 (de) * | 1986-07-23 | 1990-02-08 | Akzo Nv | 18-phenylestrane-derivate. |
| DE3625315A1 (de) * | 1986-07-25 | 1988-01-28 | Schering Ag | 11ss-(4-isopropenylphenyl)-estra-4,9-diene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| US5272140A (en) * | 1987-01-23 | 1993-12-21 | Akzo N.V. | 11-aryl steroid derivatives |
| FR2618783B1 (fr) * | 1987-07-30 | 1991-02-01 | Roussel Uclaf | Nouveaux 17-aryle steroides, leurs procedes et des intermediaires de preparation comme medicaments et les compositions pharmaceutiques les renfermant |
| ATE85342T1 (de) * | 1987-12-12 | 1993-02-15 | Akzo Nv | 11-arylsteroid-derivate. |
| US4954490A (en) * | 1988-06-23 | 1990-09-04 | Research Triangle Institute | 11 β-substituted progesterone analogs |
| DE3822770A1 (de) * | 1988-07-01 | 1990-01-04 | Schering Ag | 13-alkyl-11ss-phenylgonane |
| US5364847A (en) * | 1989-03-10 | 1994-11-15 | Endorecherche | Inhibitors of sex steroid biosynthesis and methods for their production and use |
| DD289541A5 (de) * | 1989-08-04 | 1991-05-02 | ��@�K@�������������@�K@��������������@��������k�� | Verfahren zur herstellung von 11beta-aryl-16 alpha, 17 alph-cyclohexanoestra-4,9-dienen |
| FR2651435A1 (fr) * | 1989-09-07 | 1991-03-08 | Roussel Uclaf | Nouvelle utilisation de composes anti-progestomimetiques. |
| DE4042004A1 (de) * | 1990-12-22 | 1992-06-25 | Schering Ag | 14(beta)-h-, 14- u. 15-en-11(beta)-aryl-4-estrene |
| DE69413829T2 (de) * | 1993-08-04 | 1999-04-15 | Akzo Nobel N.V., Arnheim/Arnhem | Antiglucocorticoidsteroide zur behandlung von angststörungen |
| US5759577A (en) * | 1995-01-17 | 1998-06-02 | American Home Products Corporation | Controlled release of steroids from sugar coatings |
-
2004
- 2004-02-13 US US10/542,580 patent/US20060111577A1/en not_active Abandoned
- 2004-02-13 CA CA2516319A patent/CA2516319C/en not_active Expired - Fee Related
- 2004-02-13 JP JP2006508726A patent/JP2006519255A/ja active Pending
- 2004-02-13 AU AU2004217988A patent/AU2004217988C1/en not_active Ceased
- 2004-02-13 EP EP04711161A patent/EP1613640A4/en not_active Withdrawn
- 2004-02-13 WO PCT/US2004/004246 patent/WO2004078709A2/en not_active Ceased
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3381003A (en) * | 1965-06-01 | 1968-04-30 | Merck & Co Inc | 3-keto-13beta-alkyl-17beta-acetyl-gona-4-ene-17alpha-ol compounds and processes of preparing them |
| US5929262A (en) * | 1995-03-30 | 1999-07-27 | The United States Of America As Represented By The Department Of Health And Human Services | Method for preparing 17α-acetoxy-11β-(4-N, N-dimethylaminophyl)-19-Norpregna-4,9-diene-3, 20-dione, intermediates useful in the method, and methods for the preparation of such intermediates |
| JP2002505334A (ja) * | 1998-03-06 | 2002-02-19 | リサーチ・トライアングル・インスティチュート | アゴニスト又はアンタゴニストホルモン特性を有する20−ケト−11β−アリールステロイドとその誘導体 |
| WO2001018025A2 (en) * | 1999-09-03 | 2001-03-15 | Research Triangle Institute | 17alpha propynyl 11-aryl steroids |
| JP2006515869A (ja) * | 2003-01-22 | 2006-06-08 | クリスタル、ファーマ、ソシエダッド、アノニマ | 17α−アセトキシ−11β−(4−N,N−ジメチルアミノフェニル)−19−ノルプレグナ−4,9−ジエン−3,20−ジオンを得る方法 |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014050105A1 (en) | 2012-09-28 | 2014-04-03 | Aska Pharmaceutical Co., Ltd. | Amorphous ulipristal acetate |
| WO2014050106A1 (en) | 2012-09-28 | 2014-04-03 | Aska Pharmaceutical Co., Ltd. | Crystalline polymorphic form of ulipristal acetate |
| WO2014050107A1 (en) | 2012-09-28 | 2014-04-03 | Aska Pharmaceutical Co., Ltd. | Crystalline polymorphic form of ulipristal acetate |
| JP2015531339A (ja) * | 2012-09-28 | 2015-11-02 | あすか製薬株式会社 | 無定形ウリプリスタール酢酸エステル |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2004217988C1 (en) | 2010-06-03 |
| WO2004078709A2 (en) | 2004-09-16 |
| EP1613640A4 (en) | 2010-05-19 |
| US20060111577A1 (en) | 2006-05-25 |
| AU2004217988B2 (en) | 2009-12-10 |
| WO2004078709A3 (en) | 2005-02-24 |
| EP1613640A2 (en) | 2006-01-11 |
| AU2004217988A1 (en) | 2004-09-16 |
| CA2516319A1 (en) | 2004-09-16 |
| CA2516319C (en) | 2012-09-18 |
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