MX342436B - Derivados de estradiol 6-sustituidos y metodos de uso. - Google Patents
Derivados de estradiol 6-sustituidos y metodos de uso.Info
- Publication number
- MX342436B MX342436B MX2012006169A MX2012006169A MX342436B MX 342436 B MX342436 B MX 342436B MX 2012006169 A MX2012006169 A MX 2012006169A MX 2012006169 A MX2012006169 A MX 2012006169A MX 342436 B MX342436 B MX 342436B
- Authority
- MX
- Mexico
- Prior art keywords
- nch3
- group
- alkyl
- alkynyl
- alkenyl
- Prior art date
Links
- 150000002159 estradiols Chemical class 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 abstract 1
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- -1 C1 -C6 alkyl Inorganic materials 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 101100054666 Streptomyces halstedii sch3 gene Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229930182480 glucuronide Natural products 0.000 abstract 1
- 150000008134 glucuronides Chemical class 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 125000000468 ketone group Chemical group 0.000 abstract 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 abstract 1
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical group [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- 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
- C07J1/0059—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 (2)
| Publication Number | Publication Date |
|---|---|
| MX2012006169A MX2012006169A (es) | 2012-11-12 |
| MX342436B true MX342436B (es) | 2016-09-29 |
Family
ID=44067274
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012006169A MX342436B (es) | 2009-11-30 | 2010-11-30 | Derivados de estradiol 6-sustituidos y metodos de uso. |
Country Status (12)
| 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) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
-
2009
- 2009-11-30 US US12/627,874 patent/US10174070B2/en not_active Expired - Fee Related
-
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
-
2016
- 2016-10-05 AU AU2016238850A patent/AU2016238850A1/en not_active Abandoned
-
2018
- 2018-05-24 AU AU2018203658A patent/AU2018203658A1/en not_active Abandoned
-
2019
- 2019-01-07 US US16/241,477 patent/US10723757B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| KR20180095742A (ko) | 2018-08-27 |
| 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 |
| DK2507253T3 (en) | 2016-07-04 |
| US20190135853A1 (en) | 2019-05-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |