JP2003529604A5 - - Google Patents
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- Publication number
- JP2003529604A5 JP2003529604A5 JP2001572529A JP2001572529A JP2003529604A5 JP 2003529604 A5 JP2003529604 A5 JP 2003529604A5 JP 2001572529 A JP2001572529 A JP 2001572529A JP 2001572529 A JP2001572529 A JP 2001572529A JP 2003529604 A5 JP2003529604 A5 JP 2003529604A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- methyl
- composition
- acetoxy
- methoxy
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 description 61
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 38
- 239000000203 mixture Substances 0.000 description 33
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 description 25
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 22
- 229910052739 hydrogen Inorganic materials 0.000 description 21
- 239000001257 hydrogen Substances 0.000 description 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 18
- 125000000217 alkyl group Chemical group 0.000 description 8
- 125000003545 alkoxy group Chemical group 0.000 description 7
- 125000004423 acyloxy group Chemical group 0.000 description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 2
- 150000002431 hydrogen Chemical class 0.000 description 2
- 230000001939 inductive effect Effects 0.000 description 2
- 208000005171 Dysmenorrhea Diseases 0.000 description 1
- 206010013935 Dysmenorrhoea Diseases 0.000 description 1
- 201000009273 Endometriosis Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 206010046798 Uterine leiomyoma Diseases 0.000 description 1
- 125000002252 acyl group Chemical group 0.000 description 1
- 125000005910 alkyl carbonate group Chemical group 0.000 description 1
- 239000003418 antiprogestin Substances 0.000 description 1
- 125000000131 cyclopropyloxy group Chemical group C1(CC1)O* 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 230000002357 endometrial effect Effects 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 150000002367 halogens Chemical class 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 201000010260 leiomyoma Diseases 0.000 description 1
- 206010027191 meningioma Diseases 0.000 description 1
- 210000004914 menses Anatomy 0.000 description 1
- -1 methoxy, ethoxy, vinyloxy, ethynyloxy Chemical group 0.000 description 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000003623 progesteronic effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/526,855 US6900193B1 (en) | 1996-05-01 | 2000-03-17 | Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents |
| US09/526,855 | 2000-03-17 | ||
| PCT/US2001/008681 WO2001074840A2 (en) | 2000-03-17 | 2001-03-16 | 17-alpha-substituted-11-beta-substituted-4-aryl and 21-substituted 19-norpregna 21-substituted 19-norpregnadienedione as antiprogestational agents |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011244014A Division JP2012051935A (ja) | 2000-03-17 | 2011-11-07 | 抗プロゲステロン剤としての１７−α−置換−１１−β−置換−４−アリールおよび２１−置換１９−ノルプレグナジエンジオン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003529604A JP2003529604A (ja) | 2003-10-07 |
| JP2003529604A5 true JP2003529604A5 (enExample) | 2008-05-01 |
| JP5417562B2 JP5417562B2 (ja) | 2014-02-19 |
Family
ID=24099075
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001572529A Expired - Fee Related JP5417562B2 (ja) | 2000-03-17 | 2001-03-16 | 抗プロゲステロン剤としての１７−α−置換−１１−β−置換−４−アリールおよび２１−置換１９−ノルプレグナジエンジオン |
| JP2011244014A Pending JP2012051935A (ja) | 2000-03-17 | 2011-11-07 | 抗プロゲステロン剤としての１７−α−置換−１１−β−置換−４−アリールおよび２１−置換１９−ノルプレグナジエンジオン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011244014A Pending JP2012051935A (ja) | 2000-03-17 | 2011-11-07 | 抗プロゲステロン剤としての１７−α−置換−１１−β−置換−４−アリールおよび２１−置換１９−ノルプレグナジエンジオン |
Country Status (11)
| Country | Link |
|---|---|
| EP (4) | EP2348030B1 (enExample) |
| JP (2) | JP5417562B2 (enExample) |
| AT (1) | ATE396197T1 (enExample) |
| AU (2) | AU4584901A (enExample) |
| CA (1) | CA2403756C (enExample) |
| CY (1) | CY1108281T1 (enExample) |
| DE (1) | DE60134126D1 (enExample) |
| DK (1) | DK1265911T3 (enExample) |
| ES (3) | ES2546336T3 (enExample) |
| PT (1) | PT1265911E (enExample) |
| WO (1) | WO2001074840A2 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE396197T1 (de) * | 2000-03-17 | 2008-06-15 | Us Gov Health & Human Serv | 17-alpha-substituierte-11-beta-substituierte-4- aryl und 21-substituierte 19-norpregnadienedione mit antigestagener aktivität |
| 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. |
| US8173626B2 (en) * | 2006-03-08 | 2012-05-08 | Danco Laboratories Llc | Methods, dosing regimens and medications using anti-progestational agents for the treatment of disorders |
| MY150763A (en) * | 2006-10-24 | 2014-02-28 | Repros Therapeutics Inc | Compositions and methods for suppressing endometrial proliferation |
| HU228636B1 (en) | 2007-06-27 | 2013-04-29 | Richter Gedeon Nyrt | Industrial method for the synthesis of 17-acetoxy-11betha-4[-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process |
| TWI477276B (zh) * | 2008-04-28 | 2015-03-21 | Repros Therapeutics Inc | 抗黃體素給藥方案 |
| TWI539953B (zh) * | 2008-04-28 | 2016-07-01 | 瑞波若斯治療學公司 | 用於治療乳癌之組成物和方法 |
| TW201002736A (en) * | 2008-04-28 | 2010-01-16 | Repros Therapeutics Inc | Compositions and methods for treating progesterone-dependent conditions |
| HUP0900171A2 (hu) | 2009-03-20 | 2010-12-28 | Richter Gedeon Nyrt | 17-acetoxi-11ß-[4-(dimetil-amino)-fenil]-21-metoxi-19-norpregna-4,9-dién-3,20-dion új kristályos módosulata és eljárás elõállítására |
| WO2010119029A1 (en) * | 2009-04-14 | 2010-10-21 | Laboratoire Hra-Pharma | Method for on-demand contraception |
| HUP0900487A2 (hu) | 2009-08-05 | 2011-03-28 | Richter Gedeon Nyrt | 17-acetoxi-11ß-[4-(dimetil-amino)-fenil]-21-metoxi-19-norpregna-4,9-dién-3,20-dion új kristályos polimorf módosulata és eljárás elõállítására |
| UA113283C2 (xx) * | 2010-12-23 | 2017-01-10 | 19-норстероїди і їх застосування для лікування прогестеронзалежних станів | |
| 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 |
| US9109005B2 (en) * | 2012-02-23 | 2015-08-18 | Boehringer Ingelheim International Gmbh | Method for manufacturing of ciclesonide |
| CA2872644A1 (en) | 2012-05-31 | 2013-12-05 | Allergan Pharmaceuticals International Limited | Formulations and methods for vaginal delivery of antiprogestins |
| 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 |
| 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 |
| US9545411B2 (en) | 2012-11-02 | 2017-01-17 | Repros Therapeutics Inc. | Methods and compositions for treating progesterone-dependent conditions |
| CN103073612B (zh) * | 2013-02-04 | 2015-11-04 | 山东大学 | 醋酸乌利司他关键中间体的制备方法 |
| HU230319B1 (hu) | 2013-10-01 | 2016-01-28 | Richter Gedeon Nyrt. | Ipari eljárás szteroid hatóanyagok előállítására |
| CN104774231A (zh) * | 2014-01-13 | 2015-07-15 | 上海医药工业研究院 | 17α-羟基-19-去甲孕甾-4,9-二烯-3,20-二酮的制备工艺 |
| HU230381B1 (hu) | 2014-02-17 | 2016-03-29 | Richter Gedeon Nyrt | Ipari eljárás szteroid intermedier előállítására |
| CN107840865A (zh) * | 2016-09-20 | 2018-03-27 | 天津金耀集团有限公司 | 一种甲泼尼龙的制备方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS582607B2 (ja) | 1976-03-12 | 1983-01-18 | パイオニア株式会社 | 温度検知回路 |
| 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 |
| DE3321826A1 (de) * | 1983-06-15 | 1984-12-20 | Schering AG, 1000 Berlin und 4709 Bergkamen | 13(alpha)-alkylgonane, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3504421A1 (de) * | 1985-02-07 | 1986-08-07 | Schering AG, 1000 Berlin und 4709 Bergkamen | Neue 11ss-phenyl-gonane, deren herstellung und diese enthaltende pharmazeutische praeparate |
| CA1317283C (en) | 1986-11-05 | 1993-05-04 | Douglas Alan Livingston | Steroidal 17-silyl ethers and process to corticoids and progesterones |
| US4954490A (en) * | 1988-06-23 | 1990-09-04 | Research Triangle Institute | 11 β-substituted progesterone analogs |
| 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 |
| ES2152671T3 (es) * | 1996-05-01 | 2001-02-01 | Us Gov Health & Human Serv | Derivados de progesterona sustituidos en posicion 21 como nuevos agentes antiprogestacionales. |
| US6020328A (en) * | 1998-03-06 | 2000-02-01 | Research Triangle Institute | 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
| US6172052B1 (en) * | 1998-12-04 | 2001-01-09 | Research Triangle Institute | 17β-acyl-17α-propynyl-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 |
| ATE396197T1 (de) * | 2000-03-17 | 2008-06-15 | Us Gov Health & Human Serv | 17-alpha-substituierte-11-beta-substituierte-4- aryl und 21-substituierte 19-norpregnadienedione mit antigestagener aktivität |
| RU38486U1 (ru) | 2003-11-03 | 2004-06-20 | Закрытое акционерное общество "Пермский проектно-конструкторский и экспериментальный институт горного и нефтяного машиностроения" | Гидропривод путеочистительной машины |
-
2001
- 2001-03-16 AT AT01918812T patent/ATE396197T1/de active
- 2001-03-16 ES ES10010647.5T patent/ES2546336T3/es not_active Expired - Lifetime
- 2001-03-16 ES ES01918812T patent/ES2307604T3/es not_active Expired - Lifetime
- 2001-03-16 PT PT01918812T patent/PT1265911E/pt unknown
- 2001-03-16 AU AU4584901A patent/AU4584901A/xx active Pending
- 2001-03-16 DK DK01918812T patent/DK1265911T3/da active
- 2001-03-16 JP JP2001572529A patent/JP5417562B2/ja not_active Expired - Fee Related
- 2001-03-16 EP EP20100010647 patent/EP2348030B1/en not_active Expired - Lifetime
- 2001-03-16 EP EP10010646.7A patent/EP2348031B9/en not_active Expired - Lifetime
- 2001-03-16 DE DE60134126T patent/DE60134126D1/de not_active Expired - Lifetime
- 2001-03-16 CA CA2403756A patent/CA2403756C/en not_active Expired - Lifetime
- 2001-03-16 EP EP01918812A patent/EP1265911B1/en not_active Expired - Lifetime
- 2001-03-16 EP EP08009259A patent/EP2033965A3/en not_active Withdrawn
- 2001-03-16 ES ES10010646.7T patent/ES2546291T3/es not_active Expired - Lifetime
- 2001-03-16 WO PCT/US2001/008681 patent/WO2001074840A2/en not_active Ceased
- 2001-03-16 AU AU2001245849A patent/AU2001245849B2/en not_active Expired
-
2008
- 2008-08-21 CY CY20081100895T patent/CY1108281T1/el unknown
-
2011
- 2011-11-07 JP JP2011244014A patent/JP2012051935A/ja active Pending