JP2008512426A5 - - Google Patents
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- Publication number
- JP2008512426A5 JP2008512426A5 JP2007530702A JP2007530702A JP2008512426A5 JP 2008512426 A5 JP2008512426 A5 JP 2008512426A5 JP 2007530702 A JP2007530702 A JP 2007530702A JP 2007530702 A JP2007530702 A JP 2007530702A JP 2008512426 A5 JP2008512426 A5 JP 2008512426A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound according
- compound
- treatment
- medicament
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 102000015694 estrogen receptors Human genes 0.000 claims 2
- 108010038795 estrogen receptors Proteins 0.000 claims 2
- 230000003054 hormonal effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 238000001794 hormone therapy Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000004962 physiological condition Effects 0.000 claims 1
- -1 steroid compounds Chemical class 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60850104P | 2004-09-08 | 2004-09-08 | |
| US60/608,501 | 2004-09-08 | ||
| EP04104334 | 2004-09-08 | ||
| EP04104334.0 | 2004-09-08 | ||
| PCT/EP2005/054368 WO2006027347A1 (en) | 2004-09-08 | 2005-09-05 | 15β-SUBSTITUTED STEROIDS HAVING SELECTIVE ESTROGENIC ACTIVITY |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008512426A JP2008512426A (ja) | 2008-04-24 |
| JP2008512426A5 true JP2008512426A5 (enExample) | 2008-10-02 |
| JP4889644B2 JP4889644B2 (ja) | 2012-03-07 |
Family
ID=34929554
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007530702A Expired - Fee Related JP4889644B2 (ja) | 2004-09-08 | 2005-09-05 | 選択的エストロゲン活性を有する１５β−置換ステロイド |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7838516B2 (enExample) |
| EP (1) | EP1805201B1 (enExample) |
| JP (1) | JP4889644B2 (enExample) |
| AR (1) | AR050732A1 (enExample) |
| AT (1) | ATE414710T1 (enExample) |
| AU (1) | AU2005281705B2 (enExample) |
| BR (1) | BRPI0514976A (enExample) |
| CA (1) | CA2577497C (enExample) |
| DK (1) | DK1805201T3 (enExample) |
| ES (1) | ES2317312T3 (enExample) |
| NZ (1) | NZ553266A (enExample) |
| PE (1) | PE20060590A1 (enExample) |
| PL (1) | PL1805201T3 (enExample) |
| PT (1) | PT1805201E (enExample) |
| RS (1) | RS51640B (enExample) |
| RU (1) | RU2386637C2 (enExample) |
| SI (1) | SI1805201T1 (enExample) |
| TW (1) | TW200621795A (enExample) |
| UA (1) | UA89964C2 (enExample) |
| WO (1) | WO2006027347A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8030298B2 (en) | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
| US8080540B2 (en) | 2006-09-19 | 2011-12-20 | Abbott Products Gmbh | Therapeutically active triazoles and their use |
| US8288367B2 (en) | 2006-11-30 | 2012-10-16 | Solvay Pharmaceuticals Gmbh | Substituted estratriene derivatives as 17BETA HSD inhibitors |
| EP2448910B1 (en) * | 2009-06-29 | 2013-05-15 | Merz Pharma GmbH & Co. KGaA | Method of preparing neramexane |
| BRPI1012669A2 (pt) * | 2009-06-29 | 2016-04-05 | Merz Pharma Gmbh & Co Kgaa | metodo de preparacao de 3,3,5,5-tetrametliciclohexanona, método de preparção de 1-amino-1,3,3,5,5,-pentametilciclohexano ou um sal farmaceuticamente aceitável do mesmo e composto |
| CA2765609A1 (en) * | 2009-06-29 | 2011-01-06 | Merz Pharma Gmbh & Co. Kgaa | Method of preparing neramexane |
| EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| EP2764008B1 (en) * | 2011-10-07 | 2016-08-17 | Estetra S.P.R.L. | Process for the production of estetrol |
| MX2015017879A (es) | 2013-06-25 | 2017-03-01 | Forendo Pharma Ltd | Derivados de estratrientiazol 17-nitrogeno substitutidos terapeuticamente activos como inhibidores de 17.beta-hidroxiestero ide deshidrogenasa. |
| AR096728A1 (es) | 2013-06-25 | 2016-01-27 | Forendo Pharma Ltd | Derivados de estratrieno-tiazol terapéuticamente activos |
| CN105518017B (zh) | 2013-06-25 | 2020-07-14 | 佛恩多制药有限公司 | 治疗活性的作为1型17β-羟基类固醇脱氢酶抑制剂的雌三烯噻唑衍生物 |
| CN107207562B (zh) | 2014-12-23 | 2020-03-06 | 佛恩多制药有限公司 | 17β-HSD1抑制剂的前药 |
| US10413557B2 (en) | 2014-12-23 | 2019-09-17 | Forendo Pharma Ltd. | Prodrugs of 17.BETA.-HSD1-inhibitors |
| RS57328B1 (sr) | 2015-06-18 | 2018-08-31 | Mithra Pharmaceuticals S A | Orodisperzibilna dozna jedinica koja sadrži estetrolsku komponentu |
| WO2016203044A1 (en) | 2015-06-18 | 2016-12-22 | Mithra Pharmaceuticals S.A. | Orodispersible tablet containing estetrol |
| LT3310345T (lt) | 2015-06-18 | 2021-06-25 | Estetra Sprl | Burnoje disperguojama tabletė, turinti estetrolio |
| NZ737945A (en) | 2015-06-18 | 2023-06-30 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
| CA3178291A1 (en) | 2016-08-05 | 2018-04-12 | Estetra Srl | Method for the management of dysmenorrhea and menstrual pain |
| WO2018224736A2 (en) | 2017-06-08 | 2018-12-13 | Forendo Pharma Ltd | Therapeutically active steroidal derivatives |
| CR20200486A (es) | 2018-04-19 | 2021-01-27 | Estetra Sprl | Compuestos y sus usos para aliviar los síntomas asociados a la menopausa |
| TWI801561B (zh) | 2018-04-19 | 2023-05-11 | 比利時商依思特拉私人有限責任公司 | 化合物及其用於緩解絕經相關症狀的用途 |
| MX2021006452A (es) | 2018-12-05 | 2021-09-28 | Forendo Pharma Ltd | Compuestos estra-1,3,5(10)-trieno condensados en posición 16(17) con un anillo de pirazol como inhibidores de 17-hsd1. |
| TWI893101B (zh) | 2020-04-16 | 2025-08-11 | 比利時商埃斯特拉有限責任公司 | 具有降低之副作用之避孕組成物 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL226738A (enExample) | 1957-04-11 | |||
| DE1084261B (de) | 1957-04-11 | 1960-06-30 | Syntex Sa | Verfahren zur Herstellung neuer Cyclopentanophenanthrenderivate |
| US3257429A (en) * | 1957-11-12 | 1966-06-21 | Syntex Corp | 16-methylene derivatives of estrone and estradiol |
| US3007946A (en) | 1958-11-06 | 1961-11-07 | Searle & Co | 3-alkoxy-16-methylene-1, 3, 5(10)-estratrien-17-ones |
| US3049555A (en) | 1959-12-22 | 1962-08-14 | Searle & Co | 3-alkoxy-16-methyl-1, 3, 5 (10)-estratrien-17-ones |
| US3092645A (en) | 1961-12-28 | 1963-06-04 | Searle & Co | Esters of 17alpha-alkynylester-5(10)-ene-3beta, 17beta-diols |
| GB1112840A (en) | 1964-04-07 | 1968-05-08 | Res Inst Medicine Chem | Steroids having pro-oestrogenic activity |
| US3299108A (en) | 1965-10-18 | 1967-01-17 | Searle & Co | 17alpha-alkynyl/alkenyl-13beta-alkyl-11-alkylgona-1, 3, 5 (10)-triene-3, 17beta-diols, ethers and esters thereof and intermediates thereto |
| US3465010A (en) | 1966-11-22 | 1969-09-02 | Searle & Co | 17 - (unsaturated hydrocarbon - substituted) 11,13beta - dialkylgon -4 - ene - 3,17beta-diols and esters thereof |
| US3377366A (en) | 1966-12-02 | 1968-04-09 | Searle & Co | 17alpha-alkynyl/alkenyl-11, 13beta-dialkylgon-5(10)-en-3-ones and esters thereof |
| US3642992A (en) * | 1967-09-08 | 1972-02-15 | Upjohn Co | Organic compounds |
| ZA712312B (en) | 1970-04-28 | 1972-01-26 | Ochsner Med Found Alton | 4,14-estradiene compounds |
| US3652606A (en) | 1970-08-07 | 1972-03-28 | Searle & Co | 3-oxygenated 11beta-methylestr-4-en-17beta-ol and esters thereof |
| US3704253A (en) | 1970-09-23 | 1972-11-28 | American Home Prod | 13 - polycarbonalkyl - 16 - methylgona-1,3,5(10)-trienes and 13-polycarbonalkyl-16-methylgon - 4 - en-3-ones and intermediates for their production |
| US3766224A (en) * | 1971-06-03 | 1973-10-16 | Sandoz Ag | 15-methyl-substituted steroids |
| FR2377419A1 (fr) | 1977-01-13 | 1978-08-11 | Roussel Uclaf | Nouveaux derives steroides 11b-substitues 1,3,5 (10) trieniques, leur procede de preparation et leur application comme medicament |
| DE2757157C3 (de) | 1977-12-19 | 1980-10-09 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | Verfahren zur Herstellung von 16 a -alkylierten Steroiden |
| AU572589B2 (en) | 1983-12-14 | 1988-05-12 | Upjohn Company, The | 11(alpha)-difluoromethyl and (e)-and (z)-11-fluoromethylene steroids |
| US5116830A (en) | 1984-08-17 | 1992-05-26 | Sri International | Stereoisomerically pure 17α-ethynyl-estra-2-en-17β-ol and the 17β esters thereof, methods of preparation and uses |
| US5204337A (en) | 1988-10-31 | 1993-04-20 | Endorecherche Inc. | Estrogen nucleus derivatives for use in inhibition of sex steroid activity |
| ZA94715B (en) | 1993-02-08 | 1994-10-24 | Akzo Nv | Steroids for treating menopausal complaints |
| ZA941464B (en) | 1993-03-05 | 1994-09-27 | Akzo Nv | Use of pregnane derivative |
| CA2200423C (en) | 1996-03-26 | 2006-12-19 | Sietse Mosselman | Novel estrogen receptor |
| IL123195A (en) | 1997-02-21 | 2002-11-10 | Akzo Nobel Nv | Steroid compounds with anti-pregnancy activity and against bone thinning, preparation and pharmaceutical preparations containing them |
| JP2002506014A (ja) | 1998-03-09 | 2002-02-26 | アクゾ・ノベル・エヌ・ベー | 新規な避妊用キット |
| RU2216546C2 (ru) | 1998-06-19 | 2003-11-20 | Акцо Нобель Н.В. | СОЕДИНЕНИЕ (7α,17β)-7-МЕТИЛ-17-[(1-ОКСОУНДЕЦИЛ)ОКСИ]ЭСТР-4-ЕН-3-ОН, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, НАБОР ДЛЯ МУЖСКОЙ КОНТРАЦЕПЦИИ |
| WO2000031112A1 (en) | 1998-11-20 | 2000-06-02 | Akzo Nobel N.V. | Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11 |
| TW548277B (en) | 1999-07-16 | 2003-08-21 | Akzo Nobel Nv | Orally active androgens |
| SK3282002A3 (en) | 1999-09-06 | 2002-06-04 | Akzo Nobel Nv | Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11 |
| EP1226155B1 (de) * | 1999-11-02 | 2007-05-02 | Bayer Schering Pharma AG | 18-nor-steroide als selektiv wirksame estrogene |
| HRP20030060A2 (en) * | 2000-07-28 | 2004-06-30 | Akzo Nobel Nv | 16alpha-methyl or ethyl substituted estrogens |
-
2005
- 2005-05-09 UA UAA200701655A patent/UA89964C2/ru unknown
- 2005-09-02 TW TW094130148A patent/TW200621795A/zh unknown
- 2005-09-05 NZ NZ553266A patent/NZ553266A/en not_active IP Right Cessation
- 2005-09-05 ES ES05794597T patent/ES2317312T3/es not_active Expired - Lifetime
- 2005-09-05 CA CA2577497A patent/CA2577497C/en not_active Expired - Fee Related
- 2005-09-05 BR BRPI0514976-2A patent/BRPI0514976A/pt not_active IP Right Cessation
- 2005-09-05 JP JP2007530702A patent/JP4889644B2/ja not_active Expired - Fee Related
- 2005-09-05 PL PL05794597T patent/PL1805201T3/pl unknown
- 2005-09-05 SI SI200530582T patent/SI1805201T1/sl unknown
- 2005-09-05 US US11/662,166 patent/US7838516B2/en active Active
- 2005-09-05 RS RS20070075A patent/RS51640B/sr unknown
- 2005-09-05 EP EP05794597A patent/EP1805201B1/en not_active Expired - Lifetime
- 2005-09-05 AU AU2005281705A patent/AU2005281705B2/en not_active Ceased
- 2005-09-05 PT PT05794597T patent/PT1805201E/pt unknown
- 2005-09-05 RU RU2007112939/04A patent/RU2386637C2/ru not_active IP Right Cessation
- 2005-09-05 DK DK05794597T patent/DK1805201T3/da active
- 2005-09-05 WO PCT/EP2005/054368 patent/WO2006027347A1/en not_active Ceased
- 2005-09-05 AT AT05794597T patent/ATE414710T1/de active
- 2005-09-06 PE PE2005001026A patent/PE20060590A1/es not_active Application Discontinuation
- 2005-09-08 AR ARP050103745A patent/AR050732A1/es unknown
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