JP2013512260A5 - - Google Patents
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- Publication number
- JP2013512260A5 JP2013512260A5 JP2012541227A JP2012541227A JP2013512260A5 JP 2013512260 A5 JP2013512260 A5 JP 2013512260A5 JP 2012541227 A JP2012541227 A JP 2012541227A JP 2012541227 A JP2012541227 A JP 2012541227A JP 2013512260 A5 JP2013512260 A5 JP 2013512260A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- group
- cyclopenta
- alkenyl
- phenanthrene
- 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
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 35
- 150000001875 compounds Chemical class 0.000 claims 24
- 125000001475 halogen functional group Chemical group 0.000 claims 20
- 125000003342 alkenyl group Chemical group 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 14
- -1 (methoxymethyl) amino Chemical group 0.000 claims 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 239000000126 substance Substances 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 4
- 229930182480 glucuronide Natural products 0.000 claims 4
- 150000008134 glucuronides Chemical class 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000007787 solid Substances 0.000 claims 3
- DFCZQECVFFVKDE-UHFFFAOYSA-N 3-phenanthryl hydrogen sulfate Chemical compound C1=CC=C2C3=CC(OS(=O)(=O)O)=CC=C3C=CC2=C1 DFCZQECVFFVKDE-UHFFFAOYSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 230000002759 chromosomal effect Effects 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 210000001672 ovary Anatomy 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 230000010076 replication Effects 0.000 claims 2
- GBAGOJGTNKBYMI-OCJHARCKSA-N (6r,8r,9s,10r,13s,14s)-6-(methoxymethyl)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound C([C@@]12C)CC(O)CC1[C@H](COC)C[C@@H]1[C@@H]2CC[C@]2(C)C(O)CC[C@H]21 GBAGOJGTNKBYMI-OCJHARCKSA-N 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 210000000601 blood cell Anatomy 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 230000005907 cancer growth Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000004696 endometrium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 102000015694 estrogen receptors Human genes 0.000 claims 1
- 108010038795 estrogen receptors Proteins 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000468 ketone group Chemical group 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 210000001165 lymph node Anatomy 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 210000000952 spleen Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
Applications Claiming Priority (3)
| 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 |
| 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013512260A JP2013512260A (ja) | 2013-04-11 |
| JP2013512260A5 true JP2013512260A5 (https=) | 2014-01-23 |
| JP5898625B2 JP5898625B2 (ja) | 2016-04-06 |
Family
ID=44067274
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012541227A Expired - Fee Related JP5898625B2 (ja) | 2009-11-30 | 2010-11-30 | ６−置換エストラジオール誘導体およびその使用方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US10174070B2 (https=) |
| EP (1) | EP2507253B1 (https=) |
| JP (1) | JP5898625B2 (https=) |
| KR (2) | KR102048457B1 (https=) |
| CN (1) | CN102753564B (https=) |
| AU (3) | AU2010324632A1 (https=) |
| CA (1) | CA2781627C (https=) |
| DK (1) | DK2507253T3 (https=) |
| ES (1) | ES2568941T3 (https=) |
| MX (1) | MX342436B (https=) |
| SG (1) | SG181126A1 (https=) |
| WO (1) | WO2011066542A2 (https=) |
Families Citing this family (10)
| 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 |
| BR112013005843A2 (pt) * | 2010-09-14 | 2019-12-10 | Endece Llc | derivativos de er-beta 6-substituído por desmetil-estradiol |
| CN106420767A (zh) * | 2011-03-21 | 2017-02-22 | 安德斯有限责任公司 | 用于神经轴突的髓鞘再生的6‑取代的雌二醇衍生物 |
| EP2688901B1 (en) * | 2011-03-25 | 2019-05-08 | Université Laval | INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10 |
| CA2909418A1 (en) * | 2013-04-18 | 2014-10-23 | Xi'an Libang Pharmaceutical Technology Co., Ltd. | Ester derivative of 7-.alpha.-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)n onyl]-estra-1,3,5(10)-triene-3,17.beta.-diol having anticancer activity and preparation method thereof |
| SG11201607693WA (en) * | 2014-03-19 | 2016-10-28 | Endece Llc | 6-substituted estradiol derivatives for the treatment of alzheimer's disease |
| 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 |
| CN117264008A (zh) * | 2022-06-15 | 2023-12-22 | 中国科学院大连化学物理研究所 | 一种化合物及应用和抑制剂与药物 |
| 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 (https=) | ||||
| 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 (https=) | 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 (https=) | 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 |
| ATE284682T1 (de) | 1998-08-11 | 2005-01-15 | Entremed Inc | Verwendung von 2-methoxyestradiol als fungizide |
| 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 |
| JP2006526025A (ja) | 2003-05-28 | 2006-11-16 | エントレメッド インコーポレイテッド | 抗血管新生剤 |
| 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 |
| US7498322B2 (en) | 2004-03-12 | 2009-03-03 | Entremed, Inc. | Antiangiogenic 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 |
| US20080119447A1 (en) | 2005-09-30 | 2008-05-22 | James Yarger | 6-alkoxyalkyl estradiol derivatives and methods of use |
| BRPI0616639A2 (pt) | 2005-09-30 | 2011-06-28 | Endece Llc | compostos de exemestano de (s)-6-metiloxaalquila e métodos de uso relacionados |
| 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 |
| 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 |
| BR112013005843A2 (pt) | 2010-09-14 | 2019-12-10 | Endece Llc | derivativos de er-beta 6-substituído por desmetil-estradiol |
-
2009
- 2009-11-30 US US12/627,874 patent/US10174070B2/en not_active Expired - Fee Related
-
2010
- 2010-11-30 EP EP10834033.2A patent/EP2507253B1/en not_active Not-in-force
- 2010-11-30 CN CN201080059521.4A patent/CN102753564B/zh not_active Expired - Fee Related
- 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 ES ES10834033.2T patent/ES2568941T3/es active Active
- 2010-11-30 KR KR1020187023922A patent/KR102048457B1/ko not_active Expired - Fee Related
- 2010-11-30 SG SG2012039608A patent/SG181126A1/en unknown
- 2010-11-30 DK DK10834033.2T patent/DK2507253T3/en active
- 2010-11-30 JP JP2012541227A patent/JP5898625B2/ja not_active Expired - Fee Related
- 2010-11-30 CA CA2781627A patent/CA2781627C/en not_active Expired - Fee Related
- 2010-11-30 KR KR1020127017044A patent/KR20120095461A/ko not_active Ceased
- 2010-11-30 WO PCT/US2010/058342 patent/WO2011066542A2/en not_active Ceased
-
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
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