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 PDF

Info

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
Application number
JP2006508726A
Other languages
English (en)
Japanese (ja)
Other versions
JP2006519255A5 (enExample
Inventor
ケイ. キム、ヒュン
エヌ. ラオ、ペンマラジュ
シモンズ、アン−マリー
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Government of the United States of America
Original Assignee
Government of the United States of America
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Government of the United States of America filed Critical Government of the United States of America
Publication of JP2006519255A publication Critical patent/JP2006519255A/ja
Publication of JP2006519255A5 publication Critical patent/JP2006519255A5/ja
Pending legal-status Critical Current

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J5/00Normal 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)
JP2006508726A 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 Pending JP2006519255A (ja)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Patent Citations (5)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Similar Documents

Publication Publication Date Title
JP2006519255A (ja) 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
RU2624007C2 (ru) Способ получения улипристала ацетата и его промежуточных продуктов
CA2514169C (en) Process for obtaining 17.alpha.-acetoxy-11.beta.(4-n,n-dimethylaminophenyl-19-norpregna-4,9-diene-3,20-dione
JP5274453B2 (ja) 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−ジオンの合成のための工業的プロセスおよびプロセスの新規中間体
CA2216737A1 (en) Method for preparing 17.alpha.-acetoxy-11.beta.-(4-n,n-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione, intermediates useful in the method, and methods for the preparation of such intermediates
KR20100036218A (ko) 17-아세톡시-11β-[4-(디메틸아미노)-페닐]-21-메톡시-19-노르프레그나-4,9-디엔-3,20-디온의 공업적 합성 방법 및 이 방법의 주요 중간체
JP2721002B2 (ja) アンドロスタ‐1,4‐ジエン‐3,17‐ジオンの6‐メチレン誘導体の合成における改良
AU775831B2 (en) Process for preparing 17alpha-acetoxy-11beta-(4-N,N-(dimethylamino)phenyl)-21- methoxy-19-norpregna-4,9-diene-3,20-dione, intermediates useful in the process, and processes for preparing such intermediates
JP5430603B2 (ja) ググルステロン及びググルステロールの製造方法
RU2099346C1 (ru) Стероиды, способ получения стероидов, способ получения 16-метиленстероидов, соединения
Batist et al. The chemistry of 9α-hydroxysteroids. 3. Methods for selective formation and dehydrations of 17β-cyano-9α, 17α-dihydroxyandrost-4-en-3-one
MX2012009251A (es) Un proceso para introducir un enlace doble en la posicion 15, 16 de un esteroide.
EP0071178B1 (en) Acyloxysteroids and process for producing same
CN118255831A (zh) 屈螺酮中间体的制备方法
US4939247A (en) Gamma-lactone derivatives and process of preparing same
RU2309159C2 (ru) Способ получения 4,17 (20)-z-прегнадиен-3,16-диона, способы получения соединений
RU2480477C1 (ru) СПОСОБ ПОЛУЧЕНИЯ АЦЕТАТА 16α,17α-ЦИКЛОГЕКСАНО-5α,6α-ЭПОКСИПРЕГН-3β-ОЛ-20-ОНА
US4874551A (en) δ-lactone derivatives and process of preparing same
CN118420696A (zh) 一种哈西奈德中间体异构体杂质的制备方法
WO2002101014A2 (en) A process for making estra-4,9(10)-diene steroids
JPH04235997A (ja) 10−(2−プロピニル)エストル−4−エン−3,17−ジオン

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20061219

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20061219

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100427

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20101005