KR20090067198A - 자궁내막 증식을 억제하는 조성물과 방법 - Google Patents
자궁내막 증식을 억제하는 조성물과 방법 Download PDFInfo
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- KR20090067198A KR20090067198A KR1020097009508A KR20097009508A KR20090067198A KR 20090067198 A KR20090067198 A KR 20090067198A KR 1020097009508 A KR1020097009508 A KR 1020097009508A KR 20097009508 A KR20097009508 A KR 20097009508A KR 20090067198 A KR20090067198 A KR 20090067198A
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- Prior art keywords
- progesterone
- compound
- administered
- cdb
- estrogen
- 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.)
- Ceased
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/36—Antigestagens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
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- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
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- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Nutrition Science (AREA)
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- Heart & Thoracic Surgery (AREA)
- Pregnancy & Childbirth (AREA)
- Hematology (AREA)
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- Gynecology & Obstetrics (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
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Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US86263206P | 2006-10-24 | 2006-10-24 | |
| US60/862,632 | 2006-10-24 | ||
| US88534807P | 2007-01-17 | 2007-01-17 | |
| US60/885,348 | 2007-01-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20090067198A true KR20090067198A (ko) | 2009-06-24 |
Family
ID=39468586
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020097009508A Ceased KR20090067198A (ko) | 2006-10-24 | 2007-10-24 | 자궁내막 증식을 억제하는 조성물과 방법 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US9283234B2 (enExample) |
| EP (3) | EP3263112B1 (enExample) |
| JP (5) | JP2010507685A (enExample) |
| KR (1) | KR20090067198A (enExample) |
| AU (1) | AU2007327707B2 (enExample) |
| BR (1) | BRPI0717747A2 (enExample) |
| CA (1) | CA2673128C (enExample) |
| CR (1) | CR10826A (enExample) |
| CY (2) | CY1119521T1 (enExample) |
| DK (2) | DK2078032T3 (enExample) |
| EA (1) | EA017227B1 (enExample) |
| EC (1) | ECSP099349A (enExample) |
| ES (2) | ES2814343T3 (enExample) |
| HK (1) | HK1216849A1 (enExample) |
| HU (2) | HUE036870T2 (enExample) |
| IL (2) | IL197893A (enExample) |
| LT (2) | LT2078032T (enExample) |
| MX (2) | MX343130B (enExample) |
| MY (1) | MY150763A (enExample) |
| NO (1) | NO342085B1 (enExample) |
| NZ (1) | NZ576274A (enExample) |
| PL (2) | PL2078032T3 (enExample) |
| PT (2) | PT2078032T (enExample) |
| SI (2) | SI2078032T1 (enExample) |
| WO (1) | WO2008067086A2 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2034984A4 (en) | 2006-06-02 | 2013-03-06 | Pear Tree Women S Health Care | PROCESS FOR TREATING ATROPHIC VAGINITIS |
| MX343130B (es) * | 2006-10-24 | 2016-10-26 | Repros Therapeutics Inc | Composiciones y métodos para suprimir la proliferación endometrial. |
| TW201002736A (en) * | 2008-04-28 | 2010-01-16 | Repros Therapeutics Inc | Compositions and methods for treating progesterone-dependent conditions |
| TWI477276B (zh) | 2008-04-28 | 2015-03-21 | Repros Therapeutics Inc | 抗黃體素給藥方案 |
| RU2373977C1 (ru) * | 2008-08-05 | 2009-11-27 | Государственное образовательное учреждение дополнительного профессионального образования "Новокузнецкий государственный институт усовершенствования врачей Федерального агентства по здравоохранению и социальному развитию" | Способ лечения болевого синдрома при викарном увеличении яичника после односторонней аднексэктомии |
| US8512745B2 (en) | 2008-12-08 | 2013-08-20 | Laboratoire Hra Pharma | Ulipristal acetate tablets |
| UA113283C2 (xx) * | 2010-12-23 | 2017-01-10 | 19-норстероїди і їх застосування для лікування прогестеронзалежних станів | |
| EP2471537A1 (en) * | 2010-12-30 | 2012-07-04 | PregLem S.A. | Treatment of pain associated with dislocation of basal endometrium |
| BR112014029131B1 (pt) | 2012-05-31 | 2021-03-09 | Allergan Pharmaceuticals International Limited | cápsula de mucoadesivo |
| HK1211852A1 (en) | 2012-11-02 | 2016-06-03 | Repros Therapeutics Inc. | Methods and compositions for treating progesterone-dependent conditions |
| FR2997628B1 (fr) * | 2012-11-08 | 2015-01-16 | Hra Pharma Lab | Produit de co-micronisation comprenant un modulateur selectif des recepteurs a la progesterone |
| CN105120874A (zh) | 2013-04-10 | 2015-12-02 | 普雷格莱姆股份有限公司 | 孕酮受体调节剂在子宫肌瘤疗法中的用途 |
| US20190008804A1 (en) * | 2016-01-12 | 2019-01-10 | Repros Therapeutics Inc. | Trans-Clomiphene and Progesterone Receptor Antagonist Combination Therapy for Treating Hormone-Dependent Conditions |
Family Cites Families (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4038389A (en) * | 1975-05-07 | 1977-07-26 | The Upjohn Company | Medroxyprogesterone acetate compositions |
| US4409208A (en) | 1980-04-15 | 1983-10-11 | The Salk Institute For Biological Studies | GnRH antagonists |
| 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 |
| US4619914A (en) | 1983-03-10 | 1986-10-28 | The Salk Institute For Biological Studies | GNRH antagonists IIIB |
| US4780461A (en) | 1983-06-15 | 1988-10-25 | Schering Aktiengesellschaft | 13α-alkyl-gonanes, their production, and pharmaceutical preparations containing same |
| US4547370A (en) | 1983-11-29 | 1985-10-15 | The Salk Institute For Biological Studies | GnRH Antagonists |
| DE3347126A1 (de) | 1983-12-22 | 1985-07-11 | Schering AG, 1000 Berlin und 4709 Bergkamen | 11ss-aryl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| US4569927A (en) | 1984-02-23 | 1986-02-11 | The Salk Institute For Biological Studies | GnRH Antagonists IV |
| US4565804A (en) | 1984-09-07 | 1986-01-21 | The Salk Institute For Biological Studies | GnRH Antagonists VI |
| DE3506785A1 (de) | 1985-02-22 | 1986-08-28 | Schering AG, Berlin und Bergkamen, 1000 Berlin | 11ss-n,n-dimethylaminophenyl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3625315A1 (de) | 1986-07-25 | 1988-01-28 | Schering Ag | 11ss-(4-isopropenylphenyl)-estra-4,9-diene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3708942A1 (de) | 1987-03-18 | 1988-09-29 | Schering Ag | 19,11ss-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate |
| US5446178A (en) | 1987-03-18 | 1995-08-29 | Schering Aktiengesellschaft | Process for preparing 19,11β-bridged steroids |
| ATE69820T1 (de) | 1987-04-24 | 1991-12-15 | Akzo Nv | 11-arylestranderivate und 11-arylpregnanderivate. |
| DE3878198T2 (de) | 1987-12-12 | 1993-06-24 | Akzo Nv | 11-arylsteroid-derivate. |
| DE3820948A1 (de) | 1988-06-16 | 1989-12-21 | Schering Ag | 10ss, 11ss-ueberbrueckte steroide |
| DE3822770A1 (de) | 1988-07-01 | 1990-01-04 | Schering Ag | 13-alkyl-11ss-phenylgonane |
| DE3832303A1 (de) | 1988-09-20 | 1990-04-12 | Schering Ag | 11ss-phenyl-14ssh-steroide |
| DE3917274A1 (de) | 1989-05-24 | 1990-11-29 | Schering Ag | 9(alpha)-hydroxy-19, 11(beta)-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3921059A1 (de) | 1989-06-23 | 1991-01-10 | Schering Ag | 11(beta)-aryl-4-estrene, verfahren zu ihrer herstellung sowie deren verwendung als arzneimittel |
| DE4042007A1 (de) | 1990-12-22 | 1992-06-25 | Schering Ag | 6,7-modifizierte-11(beta)-aryl-4-estrene |
| US5407928A (en) | 1990-08-15 | 1995-04-18 | Schering Aktiengesellschaft | 11β-aryl-gona-4,9-dien-3-ones |
| DE4038128A1 (de) | 1990-11-27 | 1992-06-04 | Schering Ag | 8-en-19, 11(beta)-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate |
| ZA929315B (en) | 1991-12-20 | 1993-05-24 | Akzo Nv | 17-spirofuran-3'-ylidene steroids. |
| DE4216004B4 (de) | 1992-05-12 | 2008-03-27 | Bayer Schering Pharma Akiengesellschaft | Verwendung kompetitiver Progesteronantagonisten |
| US5439913A (en) | 1992-05-12 | 1995-08-08 | Schering Aktiengesellschaft | Contraception method using competitive progesterone antagonists and novel compounds useful therein |
| DE4216003A1 (de) | 1992-05-12 | 1993-11-18 | Schering Ag | Dissoziierte kompetitive Progesteronantagonisten |
| JPH07508987A (ja) | 1992-07-01 | 1995-10-05 | オーソ・フアーマシユーチカル・コーポレーシヨン | １−アリールスルホニル，アリールカルボニルおよび１−アリールホスホニル−３−フェニル−１，４，５，６−テトラヒドロピリダジン |
| US5468736A (en) | 1993-02-25 | 1995-11-21 | The Medical College Of Hampton Road | Hormone replacement therapy |
| DE4332283A1 (de) | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| DE4332284C2 (de) | 1993-09-20 | 1997-05-28 | Jenapharm Gmbh | 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US5681817A (en) | 1994-02-04 | 1997-10-28 | The Medical College Of Hampton Roads | Treatment of ovarian estrogen dependent conditions |
| DE4434488A1 (de) | 1994-09-14 | 1996-03-21 | Schering Ag | Steroidester und -amide, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung |
| US5576310A (en) | 1994-09-20 | 1996-11-19 | Jenapharm Gmbh | 11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds |
| US5521166A (en) * | 1994-12-19 | 1996-05-28 | Ortho Pharmaceitical Corporation | Antiprogestin cyclophasic hormonal regimen |
| US5693647A (en) | 1994-12-22 | 1997-12-02 | Ligand Pharmaceuticals Incorporated | Steroid receptor modulator compounds and methods |
| US5780050A (en) * | 1995-07-20 | 1998-07-14 | Theratech, Inc. | Drug delivery compositions for improved stability of steroids |
| US6900193B1 (en) | 1996-05-01 | 2005-05-31 | The United States Of America As Represented By The Department Of Health And Human Services | Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents |
| JP4260886B2 (ja) | 1996-05-01 | 2009-04-30 | アメリカ合衆国 | 新規の抗プロゲステロンとしての２１―置換プロゲステロン誘導体 |
| US5753655A (en) | 1996-10-10 | 1998-05-19 | Ortho Pharmaceutical Corporation | 1-arylsulphonyl, arylcarbonyl and arylthiocarbonyl pyridazino derivatives and methods of preparation |
| DE19652408C2 (de) | 1996-12-06 | 2002-04-18 | Schering Ag | Steroidester, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Arzneimitteln |
| DE19706061A1 (de) | 1997-02-07 | 1998-08-13 | Schering Ag | Antigestagen wirksame Steroide mit fluorierter 17alpha-Alkylkette |
| DE19809845A1 (de) | 1998-03-03 | 1999-09-09 | Jenapharm Gmbh | S-substituierte 11beta-Benzaldoxim-estra-4,9-dien-kohlensäurethiolester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zubereitungen |
| US6020328A (en) * | 1998-03-06 | 2000-02-01 | Research Triangle Institute | 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
| US6689768B2 (en) * | 1998-04-15 | 2004-02-10 | Jenapharm Gmbh & Co. Kg | Pharmaceutical preparations for treating side effects during and/or after GnRHa therapy |
| US6417214B1 (en) | 1999-05-04 | 2002-07-09 | Wyeth | 3,3-substituted indoline derivatives |
| US6339098B1 (en) | 1999-05-04 | 2002-01-15 | American Home Products Corporation | 2,1-benzisothiazoline 2,2-dioxides |
| US6369056B1 (en) | 1999-05-04 | 2002-04-09 | American Home Products Corporation | Cyclic urea and cyclic amide derivatives |
| US6358948B1 (en) | 1999-05-04 | 2002-03-19 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| US6380235B1 (en) | 1999-05-04 | 2002-04-30 | American Home Products Corporation | Benzimidazolones and analogues |
| US6391907B1 (en) | 1999-05-04 | 2002-05-21 | American Home Products Corporation | Indoline derivatives |
| US6509334B1 (en) | 1999-05-04 | 2003-01-21 | American Home Products Corporation | Cyclocarbamate derivatives as progesterone receptor modulators |
| US6306851B1 (en) | 1999-05-04 | 2001-10-23 | American Home Products Corporation | Cyclocarbamate and cyclic amide derivatives |
| SE514556C2 (sv) | 1999-07-09 | 2001-03-12 | Jema Jori Ab | Metod för hantering av en databas |
| US6768014B2 (en) | 1999-12-29 | 2004-07-27 | The United States Of America As Represented By The Department Of Health And Human Services | PROCESS FOR PREPARING 17α-ACETOXY-11β-[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 |
| US7109171B2 (en) * | 2000-02-28 | 2006-09-19 | Praecis Pharmaceuticals Inc. | Methods for treating FSH related conditions with GnRH antagonists |
| ES2546291T3 (es) * | 2000-03-17 | 2015-09-22 | The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | 17-Alfa-sustituida, 11-beta-sustituida-4-arilo y 21-sustituida 19-norpregnadienodionas como agentes antiprogestacionales |
| WO2006010097A2 (en) * | 2004-07-09 | 2006-01-26 | The Population Council, Inc. | Sustained release compositions containing progesterone receptor modulators |
| MX343130B (es) * | 2006-10-24 | 2016-10-26 | Repros Therapeutics Inc | Composiciones y métodos para suprimir la proliferación endometrial. |
-
2007
- 2007-10-24 MX MX2013010762A patent/MX343130B/es unknown
- 2007-10-24 LT LTEP07871232.0T patent/LT2078032T/lt unknown
- 2007-10-24 LT LTEP17184128.1T patent/LT3263112T/lt unknown
- 2007-10-24 EA EA200970409A patent/EA017227B1/ru unknown
- 2007-10-24 KR KR1020097009508A patent/KR20090067198A/ko not_active Ceased
- 2007-10-24 PL PL07871232T patent/PL2078032T3/pl unknown
- 2007-10-24 BR BRPI0717747-0A2A patent/BRPI0717747A2/pt not_active IP Right Cessation
- 2007-10-24 NZ NZ576274A patent/NZ576274A/en not_active IP Right Cessation
- 2007-10-24 SI SI200731976T patent/SI2078032T1/sl unknown
- 2007-10-24 PT PT78712320T patent/PT2078032T/pt unknown
- 2007-10-24 PT PT171841281T patent/PT3263112T/pt unknown
- 2007-10-24 DK DK07871232.0T patent/DK2078032T3/da active
- 2007-10-24 PL PL17184128T patent/PL3263112T3/pl unknown
- 2007-10-24 ES ES17184128T patent/ES2814343T3/es active Active
- 2007-10-24 EP EP17184128.1A patent/EP3263112B1/en not_active Not-in-force
- 2007-10-24 JP JP2009534845A patent/JP2010507685A/ja active Pending
- 2007-10-24 ES ES07871232.0T patent/ES2643318T3/es active Active
- 2007-10-24 DK DK17184128.1T patent/DK3263112T3/da active
- 2007-10-24 AU AU2007327707A patent/AU2007327707B2/en not_active Ceased
- 2007-10-24 US US12/446,567 patent/US9283234B2/en not_active Expired - Fee Related
- 2007-10-24 HU HUE07871232A patent/HUE036870T2/hu unknown
- 2007-10-24 MX MX2009003953A patent/MX2009003953A/es active IP Right Grant
- 2007-10-24 CA CA2673128A patent/CA2673128C/en not_active Expired - Fee Related
- 2007-10-24 HU HUE17184128A patent/HUE051484T2/hu unknown
- 2007-10-24 WO PCT/US2007/082432 patent/WO2008067086A2/en not_active Ceased
- 2007-10-24 SI SI200732158T patent/SI3263112T1/sl unknown
- 2007-10-24 EP EP20167723.4A patent/EP3693376A1/en not_active Withdrawn
- 2007-10-24 MY MYPI20091368 patent/MY150763A/en unknown
- 2007-10-24 EP EP07871232.0A patent/EP2078032B1/en active Active
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2009
- 2009-04-05 IL IL197893A patent/IL197893A/en active IP Right Grant
- 2009-05-20 EC EC2009009349A patent/ECSP099349A/es unknown
- 2009-05-20 NO NO20091966A patent/NO342085B1/no not_active IP Right Cessation
- 2009-05-22 CR CR10826A patent/CR10826A/es unknown
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2013
- 2013-12-16 JP JP2013259154A patent/JP6175364B2/ja not_active Expired - Fee Related
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2014
- 2014-04-11 US US14/251,192 patent/US9616074B2/en not_active Expired - Fee Related
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2015
- 2015-05-14 IL IL238823A patent/IL238823B/en active IP Right Grant
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2016
- 2016-04-27 HK HK16104781.7A patent/HK1216849A1/zh unknown
- 2016-07-27 JP JP2016147279A patent/JP2016183199A/ja active Pending
-
2017
- 2017-03-21 US US15/464,736 patent/US20170189421A1/en not_active Abandoned
- 2017-08-28 JP JP2017163450A patent/JP2017203049A/ja active Pending
- 2017-10-25 CY CY20171101111T patent/CY1119521T1/el unknown
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2019
- 2019-04-03 JP JP2019071622A patent/JP2019131587A/ja active Pending
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2020
- 2020-08-12 CY CY20201100748T patent/CY1123239T1/el unknown
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| B601 | Maintenance of original decision after re-examination before a trial | ||
| PB0601 | Maintenance of original decision after re-examination before a trial | ||
| J301 | Trial decision |
Free format text: TRIAL DECISION FOR APPEAL AGAINST DECISION TO DECLINE REFUSAL REQUESTED 20121206 Effective date: 20130809 |
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| PJ1301 | Trial decision |
Patent event code: PJ13011S01D Patent event date: 20130809 Comment text: Trial Decision on Objection to Decision on Refusal Appeal kind category: Appeal against decision to decline refusal Request date: 20121206 Decision date: 20130809 Appeal identifier: 2012101010321 |