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PE20142461A1 - Moduladores del receptor de estrogeno y sus usos - Google Patents

Moduladores del receptor de estrogeno y sus usos

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Publication number
PE20142461A1
PE20142461A1 PE2014001451A PE2014001451A PE20142461A1 PE 20142461 A1 PE20142461 A1 PE 20142461A1 PE 2014001451 A PE2014001451 A PE 2014001451A PE 2014001451 A PE2014001451 A PE 2014001451A PE 20142461 A1 PE20142461 A1 PE 20142461A1
Authority
PE
Peru
Prior art keywords
halogen
estrogen receptor
receptor modulators
phenyl
ring
Prior art date
Application number
PE2014001451A
Other languages
English (en)
Inventor
Nicholas D Smith
Steven P Govek
Mehmet Kahraman
Jackaline D Julien
Johnny Y Nagasawa
Karensa L Douglas
Celine Bonnefous
Andiliy G Lai
Original Assignee
Seragon Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Seragon Pharmaceuticals Inc filed Critical Seragon Pharmaceuticals Inc
Publication of PE20142461A1 publication Critical patent/PE20142461A1/es

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Abstract

REFERIDA A UN COMPUESTO DE FORMULA (III), DONDEEL ANILLO B ES FENILO, NAFTILO, ENTRE OTROS; EL ANILLO C ES FENILO, HETEROARILO MONOCICLICO DE 5 MIEMBROS, ENTRE OTROS; R1 ES C(=O)-Z, ENTRE OTROS; Z ES OH, NHOH, ENTRE OTROS; Ra ES H, HALOGENO, CN, OH, ENTRE OTROS; Rb ES H, HALOGENO, OH, CN, ENTRE OTROS; Rc ES H, HALOGENO, CN, OH, ENTRE OTROS; R4 ES H, HALOGENO, CN, OH, ENTRE OTROS; R5 Y R6 SON H, ALQUILO C1-C4 O HALOGENO; m Y n SON 0, 1, 2 O 3; p ES 0, 1 O 2; r ES 1, 2, 3 O 4. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE ESTROGENO
PE2014001451A 2012-03-20 2013-03-14 Moduladores del receptor de estrogeno y sus usos PE20142461A1 (es)

Applications Claiming Priority (1)

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US201261613442P 2012-03-20 2012-03-20

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PE20142461A1 true PE20142461A1 (es) 2015-02-05

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PE2014001451A PE20142461A1 (es) 2012-03-20 2013-03-14 Moduladores del receptor de estrogeno y sus usos

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US (1) US9499538B2 (es)
EP (1) EP2828243B1 (es)
JP (1) JP6154887B2 (es)
KR (1) KR20140138296A (es)
CN (1) CN104220426B (es)
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Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2828243B1 (en) 2012-03-20 2018-10-17 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
CN105121413B (zh) 2013-03-14 2018-09-14 赛拉根医药股份有限公司 多环雌激素受体调节剂及其用途
BR112015023267B1 (pt) 2013-03-15 2023-01-31 Epigen Biosciences, Inc Composto, e medicamento para tratar um indivíduo com doença ou condição lisofosfatídica dependente de ácido
JP6389517B2 (ja) 2013-06-19 2018-09-12 セラゴン ファーマシューティカルズ， インク． アゼチジンエストロゲン受容体調節因子及びその使用
JP6576916B2 (ja) 2013-06-19 2019-09-18 セラゴン ファーマシューティカルズ， インク． エストロゲン受容体モジュレーター及びその使用
US9675586B2 (en) 2013-12-06 2017-06-13 Genentech, Inc. Estrogen receptor modulator for the treatment of locally advanced or metastatic estrogen receptor positive breast cancer
CA2941161A1 (en) 2014-03-13 2015-09-17 F.Hoffmann-La Roche Ag Methods and compositions for modulating estrogen receptor mutants
MX2016011636A (es) 2014-03-13 2016-12-12 Hoffmann La Roche Combinaciones terapeuticas con moduladores de receptor de estrogeno.
WO2016023847A1 (en) 2014-08-11 2016-02-18 F. Hoffmann-La Roche Ag Crystalline forms of an estrogen receptor modulator
CN107531722B (zh) 2015-05-26 2020-07-17 豪夫迈·罗氏有限公司 杂环雌激素受体调节剂及其用途
MY186977A (en) * 2015-05-29 2021-08-26 Eisai R&D Man Co Ltd Tetrasubstituted alkene compounds and their use
CN105061316B (zh) * 2015-07-17 2017-12-22 苏州大学 稠环类化合物、制备方法和用途
CN106518768B (zh) * 2015-09-15 2021-07-02 江苏恒瑞医药股份有限公司 丙烯酸类衍生物、其制备方法及其在医药上的应用
JP2018533561A (ja) 2015-10-07 2018-11-15 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト （ｅ）−３−（４−（（ｅ）−２−（２−クロロ−４−フルオロフェニル）−１−（１ｈ−インダゾール−５−イル）ブタ−１−エン−１−イル）フェニル）アクリル酸を調製するためのプロセス
US20170166551A1 (en) 2015-12-09 2017-06-15 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulator compounds
JP6790222B2 (ja) * 2016-03-25 2020-11-25 羅欣薬業（上海）有限公司Ｌｕｏｘｉｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ （Ｓｈａｎｇｈａｉ） Ｃｏ．， Ｌｔｄ． エストロゲン受容体ダウンレギュレーターとしての置換インドール化合物
ES2991862T3 (es) 2016-04-01 2024-12-05 Recurium Ip Holdings Llc Moduladores del receptor de estrógeno
RU2742771C2 (ru) 2016-08-31 2021-02-10 Цзянсу Хэнжуй Медицин Ко., Лтд. Производное оксопиколинамида, способ его получения и его фармацевтическое применение
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
EP3544974A1 (en) * 2016-11-24 2019-10-02 Eisai R&D Management Co., Ltd. Tetrasubstituted alkene compounds and their use for the treatment of breast cancer
KR102425785B1 (ko) 2016-11-28 2022-07-28 에자이 알앤드디 매니지먼트 가부시키가이샤 인다졸 유도체의 염 및 이의 결정
MX2019008158A (es) 2017-01-06 2019-12-09 G1 Therapeutics Inc Terapia de combinacion para el tratamiento del cancer.
KR20190117582A (ko) 2017-02-10 2019-10-16 쥐원 쎄라퓨틱스, 인크. 벤조티오펜 에스트로겐 수용체 조정제
CN108976187B (zh) * 2017-06-02 2021-11-26 上海青东生物科技有限公司 一种取代苯并呋喃衍生物及其制备与在制备抗肿瘤药物中的应用
WO2019225552A1 (en) * 2018-05-22 2019-11-28 Eisai R&D Management Co., Ltd. Salts of indazole derivative and crystals thereof
CN113490850B (zh) 2018-08-17 2024-12-06 基因泰克公司 用于治疗乳腺癌的诊断和治疗方法
AU2019400398B2 (en) * 2018-12-17 2024-10-03 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Estrogen receptor antagonist
CN119320379A (zh) * 2019-06-19 2025-01-17 江苏恒瑞医药股份有限公司 吲唑类衍生物、其制备方法及其在医药上的应用
CA3148221A1 (en) 2019-08-06 2021-02-11 Recurium Ip Holdings, Llc Estrogen receptor modulators for treating mutants
JP2024502270A (ja) 2020-12-23 2024-01-18 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー エストロゲン受容体調節薬
CN115745895A (zh) * 2021-11-13 2023-03-07 温州奥洋科技有限公司 一种紫外线吸收剂二苯嘧啶乙烯的结构与合成路线
CN116239562B (zh) * 2021-12-07 2024-12-31 江苏师范大学 一种以苯并呋喃酮为原料合成盐酸多塞平的方法

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0002097B1 (en) * 1977-08-22 1981-08-05 Imperial Chemical Industries Plc Triphenylalkene derivatives, process for their preparation and pharmaceutical compositions containing them
US4229447A (en) 1979-06-04 1980-10-21 American Home Products Corporation Intraoral methods of using benzodiazepines
US4596795A (en) 1984-04-25 1986-06-24 The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives
US5011692A (en) 1985-12-28 1991-04-30 Sumitomo Pharmaceuticals Company, Limited Sustained pulsewise release pharmaceutical preparation
US4755386A (en) 1986-01-22 1988-07-05 Schering Corporation Buccal formulation
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5739136A (en) 1989-10-17 1998-04-14 Ellinwood, Jr.; Everett H. Intraoral dosing method of administering medicaments
US5017381A (en) 1990-05-02 1991-05-21 Alza Corporation Multi-unit pulsatile delivery system
US5229135A (en) 1991-11-22 1993-07-20 Prographarm Laboratories Sustained release diltiazem formulation
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
JP3409366B2 (ja) 1993-06-18 2003-05-26 東洋インキ製造株式会社 有機エレクトロルミネッセンス素子
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5837284A (en) 1995-12-04 1998-11-17 Mehta; Atul M. Delivery of multiple doses of medications
DE19807760A1 (de) 1997-02-27 1998-09-03 Fuji Electric Co Ltd Elektrofotografischer Fotoleiter
US5840329A (en) 1997-05-15 1998-11-24 Bioadvances Llc Pulsatile drug delivery system
CA2301032C (en) 1997-08-15 2009-01-13 Duke University A method of preventing or treating estrogen-dependent diseases and disorders
DE19801598C2 (de) 1998-01-17 2000-05-11 Aventis Res & Tech Gmbh & Co Katalytische Synthese von N-alkylierten Anilinen aus Olefinen und Anilinen
DE19801597C2 (de) 1998-01-17 2001-05-03 Aventis Res & Tech Gmbh & Co Basenkatalysierte Synthese von 1-Aryl-4-(arylethyl)piperazinen aus aromatischen Olefinen und 1-Arylpiperazinen
TW593256B (en) 1999-11-16 2004-06-21 Hormos Medical Oy Ltd Triphenylalkene derivatives and their use as selective estrogen receptor modulators
GB9929988D0 (en) 1999-12-17 2000-02-09 Celltech Therapeutics Ltd Chemical compounds
US6528681B2 (en) * 2000-04-05 2003-03-04 Bristol-Meyers Squibb Pharma Company Halogenated triphenylethylene derivatives as selective estrogen receptor modulators
EP1417169A2 (en) * 2001-08-11 2004-05-12 Bristol-Myers Squibb Pharma Company Selective estrogen receptor modulators
EP1556059A4 (en) 2002-06-06 2010-06-30 Smithkline Beecham MIMETICS OF THROMBOPOIETINE
WO2005033056A2 (en) 2003-10-08 2005-04-14 Smithkline Beecham Corporation Triphenylethylene compounds as selective estrogen receptor modulators
DE102004028862A1 (de) * 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
US20070292545A1 (en) 2005-10-18 2007-12-20 Aaron Monte Anti-infective agents and methods of use
CN101146796A (zh) * 2005-01-26 2008-03-19 先灵公司 作为蛋白激酶抑制剂用于治疗癌症的3-(吲唑-5-基)-(1,2,4)三嗪衍生物及相关化合物
EP1922381A1 (en) 2005-08-15 2008-05-21 Technion Research And Development Foundation, Ltd. Printable materials
WO2008057857A1 (en) 2006-11-01 2008-05-15 Bristol-Myers Squibb Company MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-ϰB ACTIVITY AND USE THEREOF
JP2008156313A (ja) 2006-12-26 2008-07-10 Fyuuensu:Kk アミロイド疾患の治療およびモニタリングのための薬剤
GB0704407D0 (en) 2007-03-07 2007-04-18 Glaxo Group Ltd Compounds
DE102007049451A1 (de) * 2007-10-16 2009-04-23 Merck Patent Gmbh 5-Cyano-thienopyridine
JP5223362B2 (ja) 2008-02-07 2013-06-26 コニカミノルタビジネステクノロジーズ株式会社 光電変換素子及び太陽電池
WO2009131654A2 (en) 2008-04-21 2009-10-29 North Carolina State University Inhibition and dispersion of bacterial biofilms with imidazole-triazole derivatives
EP2362775B1 (en) 2008-11-20 2015-08-05 GlaxoSmithKline LLC Chemical compounds
US20110294668A1 (en) 2008-12-08 2011-12-01 North Carolina State University Inhibition and dispersion of biofilms in plants with imidazole-triazole derivatives
WO2010107474A1 (en) 2009-03-16 2010-09-23 The Research Foundation Of State University Of New York Antiestrogens for breast cancer therapy
WO2010144959A1 (en) 2009-06-18 2010-12-23 Fibrotech Therapeutics Pty Ltd Analogues of anti-fibrotic agents
GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
EP2828243B1 (en) 2012-03-20 2018-10-17 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
JP6126562B2 (ja) * 2014-08-27 2017-05-10 三星ダイヤモンド工業株式会社 光ファイバ装置

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