JP5898625B2 - ６−置換エストラジオール誘導体およびその使用方法 - Google Patents
６−置換エストラジオール誘導体およびその使用方法 Download PDFInfo
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- JP5898625B2 JP5898625B2 JP2012541227A JP2012541227A JP5898625B2 JP 5898625 B2 JP5898625 B2 JP 5898625B2 JP 2012541227 A JP2012541227 A JP 2012541227A JP 2012541227 A JP2012541227 A JP 2012541227A JP 5898625 B2 JP5898625 B2 JP 5898625B2
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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)
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- Bioinformatics & Cheminformatics (AREA)
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- 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 (3)
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| US12/627,874 US10174070B2 (en) | 2005-09-30 | 2009-11-30 | 6-substituted estradiol derivatives and methods of use |
| US12/627,874 | 2009-11-30 | ||
| PCT/US2010/058342 WO2011066542A2 (en) | 2009-11-30 | 2010-11-30 | 6-substituted estradiol derivatives and methods of use |
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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 |
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| 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 |
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| 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 |
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| 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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| 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 |
| DK2507253T3 (en) | 2016-07-04 |
| US20190135853A1 (en) | 2019-05-09 |
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