JP2006519255A5 - - Google Patents
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- Publication number
- JP2006519255A5 JP2006519255A5 JP2006508726A JP2006508726A JP2006519255A5 JP 2006519255 A5 JP2006519255 A5 JP 2006519255A5 JP 2006508726 A JP2006508726 A JP 2006508726A JP 2006508726 A JP2006508726 A JP 2006508726A JP 2006519255 A5 JP2006519255 A5 JP 2006519255A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- producing
- norpregna
- dimethylaminophenyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 29
- 238000004519 manufacturing process Methods 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- -1 N, N-dimethylaminophenyl Chemical group 0.000 claims 4
- 239000000376 reactant Substances 0.000 claims 3
- 239000007818 Grignard reagent Substances 0.000 claims 1
- HKDLNTKNLJPAIY-WKWWZUSTSA-N Ulipristal Chemical compound C1=CC(N(C)C)=CC=C1[C@@H]1C2=C3CCC(=O)C=C3CC[C@H]2[C@H](CC[C@]2(O)C(C)=O)[C@]2(C)C1 HKDLNTKNLJPAIY-WKWWZUSTSA-N 0.000 claims 1
- 230000021736 acetylation Effects 0.000 claims 1
- 238000006640 acetylation reaction Methods 0.000 claims 1
- 150000004795 grignard reagents Chemical class 0.000 claims 1
- 150000004820 halides Chemical class 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 238000005907 ketalization reaction Methods 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- ZGGAHACLOAUQSQ-AELPEBTASA-N C[C@]1(C(CC2)C(CCC(C3)=C4CCC33OCCO3)C4=CC1)[C@]2(C(C)=O)OC(C)=O Chemical compound C[C@]1(C(CC2)C(CCC(C3)=C4CCC33OCCO3)C4=CC1)[C@]2(C(C)=O)OC(C)=O ZGGAHACLOAUQSQ-AELPEBTASA-N 0.000 description 1
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 JP2006519255A (ja) | 2006-08-24 |
| JP2006519255A5 true JP2006519255A5 (https=) | 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 (https=) |
| EP (1) | EP1613640A4 (https=) |
| JP (1) | JP2006519255A (https=) |
| AU (1) | AU2004217988C1 (https=) |
| CA (1) | CA2516319C (https=) |
| WO (1) | WO2004078709A2 (https=) |
Families Citing this family (35)
| 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 |
| EP2532350A1 (en) | 2007-10-17 | 2012-12-12 | Laboratoire HRA Pharma | Pharmaceutical combination of a glucocorticoid receptor antagonist and a cortisol synthesis inhibitor 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 |
| BRPI1014035A2 (pt) | 2009-04-14 | 2016-04-12 | Hra Pharma Lab | método para contracepção. |
| US8426392B2 (en) | 2009-12-09 | 2013-04-23 | Laboratoire Hra-Pharma | Method for providing emergency contraception |
| US20130045959A1 (en) | 2010-02-01 | 2013-02-21 | Andre Ulmann | Method for late post coital contraception using ulipristal acetate |
| US8962603B2 (en) | 2010-02-01 | 2015-02-24 | Laboratoire Hra-Pharma | Method for post coital contraception in overweight or obese female subjects 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 |
| ES2672727T3 (es) | 2012-05-25 | 2018-06-15 | Laboratoire Hra Pharma | Acetato de ulipristal para la prevención y el tratamiento de tumores de mama |
| 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 |
| AU2013321890B2 (en) | 2012-09-28 | 2017-05-18 | 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 |
| WO2014050105A1 (en) * | 2012-09-28 | 2014-04-03 | Aska Pharmaceutical Co., Ltd. | Amorphous ulipristal acetate |
| 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 |
| SG11201507260QA (en) | 2013-04-10 | 2015-10-29 | Preglem Sa | Progesteron receptor modulators for use in the therapy of uterine fibroids |
| HU230319B1 (hu) * | 2013-10-01 | 2016-01-28 | Richter Gedeon Nyrt. | Ipari eljárás szteroid hatóanyagok előállítására |
| RU2017112748A (ru) | 2014-11-17 | 2018-12-19 | Арно Терапьютикс, Инк. | Композиции онапристона пролонгированного действия и способы |
| CA2998924A1 (en) * | 2015-09-25 | 2017-03-30 | Context Biopharma Inc. | Methods of making onapristone intermediates |
| CA3008422A1 (en) | 2015-12-15 | 2017-06-22 | Context Biopharma Inc. | Amorphous onapristone compositions and methods of making the same |
| 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 |
Family Cites Families (22)
| 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 |
| 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 |
| ES2053714T3 (es) * | 1987-12-12 | 1994-08-01 | Akzo Nv | Proceso para la preparacion de 11-arilesteroides. |
| 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 |
| JP3828926B2 (ja) * | 1993-08-04 | 2006-10-04 | アクゾ・ノベル・エヌ・ベー | 不安症の治療用抗グルココルチコイドステロイド |
| US5759577A (en) * | 1995-01-17 | 1998-06-02 | American Home Products Corporation | Controlled release of steroids from sugar coatings |
| 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 |
| US6020328A (en) * | 1998-03-06 | 2000-02-01 | Research Triangle Institute | 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
| US6740645B1 (en) * | 1999-09-03 | 2004-05-25 | Research Triangle Institute | 17β-acyl-17α-propynyl-11β-(cyclic amino) aryl steroids and their derivatives having antagonist hormonal properties |
| 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. |
-
2004
- 2004-02-13 AU AU2004217988A patent/AU2004217988C1/en not_active Ceased
- 2004-02-13 CA CA2516319A patent/CA2516319C/en not_active Expired - Fee Related
- 2004-02-13 WO PCT/US2004/004246 patent/WO2004078709A2/en not_active Ceased
- 2004-02-13 JP JP2006508726A patent/JP2006519255A/ja active Pending
- 2004-02-13 US US10/542,580 patent/US20060111577A1/en not_active Abandoned
- 2004-02-13 EP EP04711161A patent/EP1613640A4/en not_active Withdrawn
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