DK2507253T3 - 6-substituted estradiol derivatives and methods of use - Google Patents
6-substituted estradiol derivatives and methods of use Download PDFInfo
- Publication number
- DK2507253T3 DK2507253T3 DK10834033.2T DK10834033T DK2507253T3 DK 2507253 T3 DK2507253 T3 DK 2507253T3 DK 10834033 T DK10834033 T DK 10834033T DK 2507253 T3 DK2507253 T3 DK 2507253T3
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- DK
- Denmark
- Prior art keywords
- compounds
- compound
- estrogen
- mmol
- methyl
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Classifications
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- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
- C07J1/0074—Esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0044—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N5/00—Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
- C12N5/06—Animal cells or tissues; Human cells or tissues
- C12N5/0602—Vertebrate cells
- C12N5/0693—Tumour cells; Cancer cells
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2501/00—Active agents used in cell culture processes, e.g. differentation
- C12N2501/30—Hormones
- C12N2501/38—Hormones with nuclear receptors
- C12N2501/39—Steroid hormones
- C12N2501/392—Sexual steroids
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Wood Science & Technology (AREA)
- Biotechnology (AREA)
- Zoology (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Oncology (AREA)
- General Engineering & Computer Science (AREA)
- Cell Biology (AREA)
- Microbiology (AREA)
- Biochemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12/627,874 US10174070B2 (en) | 2005-09-30 | 2009-11-30 | 6-substituted estradiol derivatives and methods of use |
| PCT/US2010/058342 WO2011066542A2 (en) | 2009-11-30 | 2010-11-30 | 6-substituted estradiol derivatives and methods of use |
Publications (1)
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| DK2507253T3 true DK2507253T3 (en) | 2016-07-04 |
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| DK10834033.2T DK2507253T3 (en) | 2009-11-30 | 2010-11-30 | 6-substituted estradiol derivatives and methods of use |
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| Country | Link |
|---|---|
| US (2) | US10174070B2 (enExample) |
| EP (1) | EP2507253B1 (enExample) |
| JP (1) | JP5898625B2 (enExample) |
| KR (2) | KR20120095461A (enExample) |
| CN (1) | CN102753564B (enExample) |
| AU (3) | AU2010324632A1 (enExample) |
| CA (1) | CA2781627C (enExample) |
| DK (1) | DK2507253T3 (enExample) |
| ES (1) | ES2568941T3 (enExample) |
| MX (1) | MX342436B (enExample) |
| SG (1) | SG181126A1 (enExample) |
| WO (1) | WO2011066542A2 (enExample) |
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| US10174070B2 (en) | 2005-09-30 | 2019-01-08 | Endece Llc | 6-substituted estradiol derivatives and methods of use |
| ES2605960T3 (es) * | 2010-09-14 | 2017-03-17 | Endece, Llc | Derivados de desmetil-estradiol 6-sustituido como agonistas del RE-beta |
| SG193380A1 (en) | 2011-03-21 | 2013-10-30 | Endece Llc | 6-substituted estradiol derivatives for use in remyelination of nerve axons |
| EP2688901B1 (en) * | 2011-03-25 | 2019-05-08 | Université Laval | INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10 |
| CN104936971B (zh) * | 2013-04-18 | 2017-10-13 | 西安力邦医药科技有限责任公司 | 具有抗癌活性的7‑α‑[9‑(4，4，5，5，5‑五氟戊基亚硫酰基)壬基]‑雌甾‑1，3，5(10)‑三烯‑3，17β‑二醇的酯类衍生物及其制备方法 |
| JP2017512769A (ja) * | 2014-03-19 | 2017-05-25 | エンディース エルエルシーＥｎｄｅｃｅ，Ｌｌｃ | アルツハイマー病の治療のための６−置換エストラジオール誘導体 |
| CN114644673B (zh) * | 2020-12-19 | 2023-12-26 | 上海喀露蓝科技有限公司 | 一种雌二醇衍生物、其制备方法及其在医药上的用途 |
| CN113956321B (zh) * | 2021-10-22 | 2023-11-03 | 郑州安图生物工程股份有限公司 | 雌二醇6位葡萄糖醛酸苷及其制备方法和应用 |
| CN115505019B (zh) * | 2022-11-07 | 2024-01-26 | 南宁师范大学 | 7-酰胺取代雌甾类化合物及其制备方法和应用 |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE258820C (enExample) | ||||
| US2867630A (en) | 1958-06-09 | 1959-01-06 | Upjohn Co | 6-fluoro androstenes |
| GB853012A (en) | 1958-06-26 | 1960-11-02 | British Drug Houses Ltd | 1:6-dimethyl aromatic steroids and the preparation thereof |
| US3130210A (en) | 1962-11-14 | 1964-04-21 | Olin Mathieson | Estradiol derivatives |
| NL122154C (enExample) | 1963-10-18 | |||
| US3377363A (en) | 1966-04-13 | 1968-04-09 | Abbott Lab | delta5(10)-6-hydroxymethyl-estrene compounds |
| DE1906716A1 (de) * | 1969-02-06 | 1970-08-20 | Schering Ag | 6,7-Disubstituierte OEstratriene |
| DK290774A (enExample) | 1973-06-08 | 1975-02-03 | Schering Ag | |
| DE2832606A1 (de) | 1978-07-21 | 1980-01-31 | Schering Ag | Verfahren zur herstellung von 7 alpha -methyl-oestrogenen |
| US4732904A (en) | 1984-12-24 | 1988-03-22 | Morgan Lee R | Antiestrogenic hydrazones |
| GB8517360D0 (en) | 1985-07-09 | 1985-08-14 | Erba Farmitalia | Substituted androsta-1,4-diene-3,17-diones |
| DD258820A1 (de) | 1986-06-13 | 1988-08-03 | Adw Ddr | Verfahren zur herstellung von 6beta-hydroxy-methyl-androsta-1,4-dien-3,17-dion |
| GB8615092D0 (en) | 1986-06-20 | 1986-07-23 | Erba Farmitalia | Androst-4-ene-317-diones |
| GB8721383D0 (en) | 1987-09-11 | 1987-10-21 | Erba Farmitalia | Preparation of methylene derivatives |
| GB8801697D0 (en) | 1988-01-26 | 1988-02-24 | Erba Farmitalia | Improvements in synthesis of 6-methylene derivatives of androsta-1 4-diene-3 17-dione |
| US4938763B1 (en) | 1988-10-03 | 1995-07-04 | Atrix Lab Inc | Biodegradable in-situ forming implants and method of producing the same |
| US5504074A (en) | 1993-08-06 | 1996-04-02 | Children's Medical Center Corporation | Estrogenic compounds as anti-angiogenic agents |
| JPH07215992A (ja) | 1993-12-07 | 1995-08-15 | Teikoku Hormone Mfg Co Ltd | ６−又は７−置換アンドロスタ−１，４−ジエン誘導体 |
| DE19633349A1 (de) | 1996-08-19 | 1998-02-26 | Sigma Tau Ind Farmaceuti | Neue 6-Hydroxy- und 6-Oxo-androstan-Derivate, die auf das kardiovaskuläre System wirken und pharmazeutische Zusammensetzungen, die diese enthalten |
| AU764266B2 (en) | 1998-08-11 | 2003-08-14 | Entremed, Inc | Use of estrogenic and anti-estrogenic compounds as anti-fungal compounds |
| WO2001058919A2 (en) | 2000-02-11 | 2001-08-16 | Sri International | Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one |
| IT1317031B1 (it) | 2000-05-17 | 2003-05-26 | Sigma Tau Ind Farmaceuti | Procedimento migliorato per la preparazione di (e,z)3-(2-amminoetossimmino)-androstano-6, 17-dione e di suoi analoghi. |
| WO2002022645A2 (en) | 2000-09-14 | 2002-03-21 | Accelerated Pharmaceuticals, Inc. | Method of making 7alpha-methyl-11beta-methoxy estradiol and related compounds with estrogenic activity |
| AU2004275693A1 (en) | 2003-05-28 | 2005-04-07 | Entremed, Inc. | Antiangiogenic agents |
| US8088758B2 (en) | 2003-11-12 | 2012-01-03 | Abbott Products Gmbh | 17β-hydroxysteroid dehydrogenase type I inhibitors |
| ATE548375T1 (de) | 2004-01-16 | 2012-03-15 | Cedarburg Pharmaceuticals Inc | Exemestan und zwischenprodukte davon und verfahren zu dessen herstellung |
| EP1756139A4 (en) | 2004-03-12 | 2009-07-29 | Entremed Inc | ANTI-ANGIOGENIC AGENTS |
| US7419972B2 (en) | 2004-07-02 | 2008-09-02 | Schering Ag | 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1 |
| US10174070B2 (en) | 2005-09-30 | 2019-01-08 | Endece Llc | 6-substituted estradiol derivatives and methods of use |
| US8168621B2 (en) | 2005-09-30 | 2012-05-01 | Endece, Llc | 6-substituted estradiol derivatives and methods of use |
| US20080119447A1 (en) | 2005-09-30 | 2008-05-22 | James Yarger | 6-alkoxyalkyl estradiol derivatives and methods of use |
| JP5255444B2 (ja) | 2005-09-30 | 2013-08-07 | エンディース エルエルシー | （ｓ）−６−メチルオキサアルキルエキセメスタン化合物および関連する使用方法 |
| TWI392682B (zh) | 2006-04-13 | 2013-04-11 | Sigma Tau Ind Farmaceuti | 作為心血管疾病的治療藥物之雄甾烷和雄甾烯的胺基衍生物 |
| JP5290189B2 (ja) | 2006-11-30 | 2013-09-18 | エンディース エルエルシー | ６−アルコキシアルキルエストラジオール誘導体およびその使用 |
| ES2605960T3 (es) | 2010-09-14 | 2017-03-17 | Endece, Llc | Derivados de desmetil-estradiol 6-sustituido como agonistas del RE-beta |
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2009
- 2009-11-30 US US12/627,874 patent/US10174070B2/en not_active Expired - Fee Related
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2010
- 2010-11-30 MX MX2012006169A patent/MX342436B/es active IP Right Grant
- 2010-11-30 AU AU2010324632A patent/AU2010324632A1/en not_active Abandoned
- 2010-11-30 DK DK10834033.2T patent/DK2507253T3/en active
- 2010-11-30 CN CN201080059521.4A patent/CN102753564B/zh not_active Expired - Fee Related
- 2010-11-30 WO PCT/US2010/058342 patent/WO2011066542A2/en not_active Ceased
- 2010-11-30 CA CA2781627A patent/CA2781627C/en not_active Expired - Fee Related
- 2010-11-30 ES ES10834033.2T patent/ES2568941T3/es active Active
- 2010-11-30 KR KR1020127017044A patent/KR20120095461A/ko not_active Ceased
- 2010-11-30 SG SG2012039608A patent/SG181126A1/en unknown
- 2010-11-30 JP JP2012541227A patent/JP5898625B2/ja not_active Expired - Fee Related
- 2010-11-30 EP EP10834033.2A patent/EP2507253B1/en not_active Not-in-force
- 2010-11-30 KR KR1020187023922A patent/KR102048457B1/ko not_active Expired - Fee Related
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2016
- 2016-10-05 AU AU2016238850A patent/AU2016238850A1/en not_active Abandoned
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2018
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2019
- 2019-01-07 US US16/241,477 patent/US10723757B2/en active Active
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|---|---|
| KR20180095742A (ko) | 2018-08-27 |
| MX342436B (es) | 2016-09-29 |
| CA2781627A1 (en) | 2011-06-03 |
| ES2568941T3 (es) | 2016-05-05 |
| CA2781627C (en) | 2017-02-28 |
| US20100130463A1 (en) | 2010-05-27 |
| CN102753564A (zh) | 2012-10-24 |
| CN102753564B (zh) | 2017-04-05 |
| US10174070B2 (en) | 2019-01-08 |
| WO2011066542A3 (en) | 2011-10-20 |
| MX2012006169A (es) | 2012-11-12 |
| AU2018203658A1 (en) | 2018-06-14 |
| EP2507253B1 (en) | 2016-03-30 |
| EP2507253A2 (en) | 2012-10-10 |
| WO2011066542A2 (en) | 2011-06-03 |
| US10723757B2 (en) | 2020-07-28 |
| EP2507253A4 (en) | 2013-05-22 |
| KR20120095461A (ko) | 2012-08-28 |
| SG181126A1 (en) | 2012-07-30 |
| AU2016238850A1 (en) | 2016-10-20 |
| KR102048457B1 (ko) | 2019-11-25 |
| AU2010324632A1 (en) | 2012-06-14 |
| JP2013512260A (ja) | 2013-04-11 |
| JP5898625B2 (ja) | 2016-04-06 |
| US20190135853A1 (en) | 2019-05-09 |
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