JP2013528223A - エストロゲン受容体モジュレーターおよびその用途 - Google Patents

エストロゲン受容体モジュレーターおよびその用途 Download PDF

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JP2013528223A
JP2013528223A JP2013514346A JP2013514346A JP2013528223A JP 2013528223 A JP2013528223 A JP 2013528223A JP 2013514346 A JP2013514346 A JP 2013514346A JP 2013514346 A JP2013514346 A JP 2013514346A JP 2013528223 A JP2013528223 A JP 2013528223A
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substituted
unsubstituted
phenyl
chromene
methyl
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JP2013528223A5 (enExample
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カフラマン，メフメト
ゴベク，スティーブン，ピー．
ナガサワ，ジョニー，ワイ．
スミス，ニコラス，ディー．
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アラゴン ファーマシューティカルズ，インク．
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Publication of JP2013528223A publication Critical patent/JP2013528223A/ja
Publication of JP2013528223A5 publication Critical patent/JP2013528223A5/ja
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017507964A (ja) * 2014-03-13 2017-03-23 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト エストロゲン受容体モジュレーターを用いた治療的組合せ
JP2017509631A (ja) * 2014-03-13 2017-04-06 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト エストロゲン受容体突然変異体を調節する方法及び組成物
JP2018520116A (ja) * 2015-05-26 2018-07-26 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 複素環式エストロゲン受容体モジュレーター及びその使用
JP2018536647A (ja) * 2015-10-27 2018-12-13 スン プハルマ アドバンセド リサーチ カンパニー リミテド 新規ヘテロ環状抗エストロゲン剤

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20170786T1 (hr) 2010-06-10 2017-08-11 Seragon Pharmaceuticals, Inc. Modulatori estrogenskog receptora i njihove uporabe
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
WO2013056178A2 (en) 2011-10-14 2013-04-18 Foundation Medicine, Inc. Novel estrogen receptor mutations and uses thereof
MX357496B (es) 2011-12-14 2018-07-11 Seragon Pharmaceuticals Inc Moduladores del receptor de estrógenos fluorados y sus usos.
AU2012353660A1 (en) 2011-12-16 2014-06-12 Olema Pharmaceuticals, Inc. Novel benzopyran compounds, compositions and uses thereof
WO2014203129A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Combinations of benzopyran compounds, compositions and uses thereof
UA117249C2 (uk) 2013-06-19 2018-07-10 Серагон Фармасьютікалз, Інк. Модулятор рецептора естрогену та його застосування
WO2014203132A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Substituted benzopyran compounds, compositions and uses thereof
CA2915534A1 (en) 2013-06-19 2014-12-24 Seragon Pharmaceuticals, Inc. Azetidine estrogen receptor modulators and uses thereof
EP3233828B1 (en) 2014-12-18 2020-03-04 F. Hoffmann-La Roche AG Estrogen receptor modulators and uses thereof
JP2017538727A (ja) * 2014-12-18 2017-12-28 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 癌の治療に有用な２，３−ジフェニルクロメンの誘導体
EA032311B1 (ru) 2014-12-18 2019-05-31 Ф. Хоффманн-Ля Рош Аг Тетрагидро-пиридо[3,4-b]индоловые модуляторы эстрогеновых рецепторов и их применение
WO2017024319A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Tunable endogenous protein degradation
HUE055321T2 (hu) 2015-10-01 2021-11-29 Olema Pharmaceuticals Inc Tetrahidro-1H-pirido[3,4-b]indol anti-ösztrogén hatóanyagok
WO2017080338A1 (zh) 2015-11-12 2017-05-18 浙江海正药业股份有限公司 丙烯酸类衍生物、其制备方法及其在医药上的用途
CA3008020C (en) 2015-12-09 2024-02-20 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulators
ES2842579T3 (es) 2016-02-05 2021-07-14 Inventisbio Llc Degradadores de los receptores de estrógenos selectivos y sus usos
IL295050A (en) 2016-04-01 2022-09-01 Recurium Ip Holdings Llc Estrogen receptor modulators
US10125135B2 (en) 2016-04-20 2018-11-13 Astrazeneca Ab Chemical compounds
ES2989988T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros heterorocíclicos para la degradación de proteínas diana
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
US20180002344A1 (en) 2016-06-16 2018-01-04 Genentech, Inc. Heteroaryl estrogen receptor modulators and uses thereof
CN109789143A (zh) 2016-07-01 2019-05-21 G1治疗公司 基于嘧啶的抗增殖剂
WO2018019793A1 (en) 2016-07-25 2018-02-01 Astrazeneca Ab N-(2-(4-((1r,3r)-3-methyl-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indol-1-yl)phenoxy)ethyl)propan-1-amine derivatives and related compounds as selective down-regulators of the estrogen receptor for treating cancer
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
JP6744489B2 (ja) 2016-10-24 2020-08-19 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ 癌の治療において有用な６，７，８，９−テトラヒドロ−３Ｈ−ピラゾロ［４，３−ｆ］イソキノリン誘導体
WO2018129419A1 (en) * 2017-01-05 2018-07-12 Radius Pharmaceuticals, Inc. Polymorphic forms of rad1901-2hcl
MX2019008158A (es) 2017-01-06 2019-12-09 G1 Therapeutics Inc Terapia de combinacion para el tratamiento del cancer.
JOP20190183B1 (ar) 2017-01-30 2022-09-15 Astrazeneca Ab معدِلات مستقبلات الاستروجين
EP4119552A1 (en) 2017-02-08 2023-01-18 Dana-Farber Cancer Institute, Inc. Regulating chimeric antigen receptors
US10208011B2 (en) 2017-02-10 2019-02-19 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators
CN118440096A (zh) 2017-06-20 2024-08-06 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
KR102659211B1 (ko) 2017-06-29 2024-04-18 쥐원 쎄라퓨틱스, 인크. G1t38의 형체 형태 및 그의 제조 방법
CN111032627B (zh) * 2017-09-25 2023-10-20 罗欣健康科技发展(北京)有限公司 一种雌激素受体抑制剂的晶型及其制备方法
US11624095B2 (en) 2017-09-27 2023-04-11 Case Western Reserve University Method of quantifying HIV reservoirs by induced transcription based sequencing
CA3079407A1 (en) 2017-10-18 2019-04-25 Novartis Ag Compositions and methods for selective protein degradation
CA3081602A1 (en) 2017-11-16 2019-05-23 Novartis Ag Combination therapies
CN111902141A (zh) 2018-03-26 2020-11-06 C4医药公司 用于ikaros降解的羟脑苷脂结合剂
CN118239948A (zh) 2018-06-21 2024-06-25 豪夫迈·罗氏有限公司 固体形式及制备稠合三环化合物的方法，包括其使用方法
SG11202013177WA (en) 2018-07-04 2021-01-28 Radius Pharmaceuticals Inc Polymorphic forms of rad 1901-2hcl
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
CN108911967A (zh) * 2018-08-03 2018-11-30 上海华堇生物技术有限责任公司 2,5–二甲氧基苯甲酰氯的制备方法
MX2021001857A (es) 2018-08-17 2021-10-13 Genentech Inc Star Metodos de diagnostico y terapeuticos para el tratamiento del cancer de mama.
EP3846800A4 (en) 2018-09-04 2022-08-24 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
CN113453679B (zh) 2018-12-20 2025-07-08 C4医药公司 靶向蛋白降解
EP3897637A1 (en) 2018-12-20 2021-10-27 Novartis AG Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
CN113348163B (zh) 2019-02-12 2024-10-08 雷迪厄斯制药公司 方法和化合物
EP3924054B1 (en) 2019-02-15 2025-04-02 Novartis AG 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CA3123519A1 (en) 2019-02-15 2020-08-20 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CA3252762A1 (en) 2019-04-12 2025-07-08 C4 Therapeutics, Inc. Tricyclic degraders of ikaros and aiolos
WO2020219742A1 (en) 2019-04-24 2020-10-29 Novartis Ag Compositions and methods for selective protein degradation
TW202100184A (zh) 2019-05-20 2021-01-01 瑞士商諾華公司 Mcl-1抑制劑抗體－藥物結合物及使用方法
WO2020238733A1 (zh) 2019-05-24 2020-12-03 浙江海正药业股份有限公司 丙烯酸类衍生物的晶型及其制备方法和用途
CA3144791A1 (en) 2019-07-07 2021-01-14 Olema Pharmaceuticals, Inc. Regimens of estrogen receptor antagonists
US11014915B2 (en) 2019-07-22 2021-05-25 Sun Pharma Advanced Research Company Limited Selective estrogen receptor degrader
CN114269342A (zh) 2019-08-06 2022-04-01 里科瑞尔姆Ip控股有限责任公司 用于治疗突变的雌激素受体调节剂
BR112022011998A2 (pt) 2019-12-20 2022-08-30 Novartis Ag Usos de anticorpos anti-tgfss e inibidores de checkpoint para o tratamento de doenças proliferativas
EP4681715A2 (en) 2019-12-20 2026-01-21 C4 Therapeutics, Inc. Isoindolinone and indazole compounds for the degradation of egfr
AU2021231898A1 (en) 2020-03-05 2022-10-27 C4 Therapeutics, Inc. Compounds for targeted degradation of BRD9
AU2021260829B2 (en) 2020-04-24 2024-01-11 Astrazeneca Ab Dosage regimen for the treatment of cancer
KR20230005270A (ko) 2020-04-24 2023-01-09 아스트라제네카 아베 약학적 제형
EP4652997A2 (en) 2020-05-19 2025-11-26 Pharmacosmos Holding A/s Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders
EP4168007A1 (en) 2020-06-23 2023-04-26 Novartis AG Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
EP4188549A1 (en) 2020-08-03 2023-06-07 Novartis AG Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
EP4192458A4 (en) 2020-08-05 2024-09-04 C4 Therapeutics, Inc. COMPOUNDS FOR TARGETED DEGRADATION OF RET
US20250171423A1 (en) 2020-09-23 2025-05-29 Achillion Pharmaceuticals, Inc. Pharmaceutical compounds for the treatment of complement mediated disorders
KR20230138444A (ko) 2020-11-24 2023-10-05 노파르티스 아게 Mcl-1 억제제 항체-약물 접합체 및 사용 방법
WO2022112942A2 (en) 2020-11-24 2022-06-02 Novartis Ag Anti-cd48 antibodies, antibody drug conjugates, and uses thereof
EP4267578A4 (en) 2020-12-23 2024-11-20 Recurium IP Holdings, LLC ESTROGEN RECEPTOR MODULATORS
IL304891A (en) 2021-02-02 2023-10-01 Servier Lab Selective Protech BCL-XL compounds and methods of use
CN115073273B (zh) * 2021-03-15 2024-09-17 中国医学科学院药物研究所 二苯烷类化合物及其制备方法、药物组合物和用途
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación
CN117940133A (zh) 2021-06-08 2024-04-26 C4医药公司 用于突变braf的降解的治疗剂
CA3256012A1 (en) 2022-05-20 2023-11-23 Les Laboratoires Servier ANTIBODY-DRUG CONJUGATES, MET INHIBITORS BCL-XL, AND THEIR METHODS OF USE
WO2023225320A1 (en) 2022-05-20 2023-11-23 Novartis Ag Epha2 bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
EP4565585A1 (en) 2022-08-03 2025-06-11 Bristol-Myers Squibb Company Compounds for modulating ret protein
WO2024097989A1 (en) 2022-11-04 2024-05-10 Bristol-Myers Squibb Company Ret-ldd protein degraders
EP4611900A1 (en) 2022-11-04 2025-09-10 Bristol-Myers Squibb Company Ret-ldd protein inhibitors
AU2024234194A1 (en) 2023-03-10 2025-08-07 Novartis Ag Panras inhibitor antibody-drug conjugates and methods of use thereof
WO2025006753A2 (en) 2023-06-30 2025-01-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein
TW202540185A (zh) 2023-11-22 2025-10-16 法商施維雅藥廠 抗cd74抗體藥物結合物及其使用方法
WO2025215536A1 (en) 2024-04-10 2025-10-16 Novartis Ag Macrocyclic panras inhibitors for the treatment of cancer

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0470310A1 (en) * 1990-08-09 1992-02-12 Council of Scientific and Industrial Research Novel benzopyrans and process for their production
JPH11500133A (ja) * 1995-02-21 1999-01-06 アンドルシェルシュ・インコーポレイテッド ベンゾピラン含有化合物およびその使用方法
US6262270B1 (en) * 1998-08-14 2001-07-17 Schering Corporation Enantioselective synthesis
WO2001068634A1 (de) * 2000-03-15 2001-09-20 Schering Aktiengesellschaft 4-fluoralkyl-2h-benzopyrane mit antiestrogener wirksamkeit
WO2004091488A2 (en) * 2003-04-14 2004-10-28 Merck & Co., Inc. Estrogen receptor modulators
JP2005513133A (ja) * 2001-12-19 2005-05-12 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド エストロゲン受容体調節剤としての四環状複素化合物
JP2007191484A (ja) * 1998-06-11 2007-08-02 Endorecherche Inc 選択的エストロゲン受容体モジュレーターと性ステロイド前駆体の組合せの医学的使用

Family Cites Families (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP0230654B1 (en) 1985-12-28 1992-03-18 Sumitomo Pharmaceuticals Company, Limited Sustained pulsewise release pharmaceutical preparation
US4755386A (en) 1986-01-22 1988-07-05 Schering Corporation Buccal formulation
US5395842A (en) 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
US5686465A (en) 1988-10-31 1997-11-11 Endorecherche Inc. Sex steroid activity inhibitors
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
US5254568A (en) 1990-08-09 1993-10-19 Council Of Scientific & Industrial Research Benzopyrans as antiestrogenic agents
US5229135A (en) 1991-11-22 1993-07-20 Prographarm Laboratories Sustained release diltiazem formulation
ATE157869T1 (de) 1993-06-24 1997-09-15 Lilly Co Eli Antiöstrogene 2-phenyl-3-aroylbenzothiophene als hypoglykämische mittel
US5407947A (en) * 1993-11-05 1995-04-18 Eli Lilly And Company Methods for inhibiting bone loss using pyrolidine and piperidine substituted benzopyrans
US5446061A (en) 1993-11-05 1995-08-29 Eli Lilly And Company Methods for lowering serum cholesterol
US5416098A (en) 1993-12-30 1995-05-16 Zymogenetics, Inc. Method for treating dermatitis and related conditions
US5389646A (en) 1993-12-30 1995-02-14 Zymogenetics, Inc. Methods for treatment and prevention of bone loss using 2,3-benzopyrans
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
TW398975B (en) 1994-07-22 2000-07-21 Lilly Co Eli Pharmaceutical composition for inhibiting bone loss
US5637598A (en) 1994-11-18 1997-06-10 Eli Lilly And Company Methods of inhibiting bone loss
US5446071A (en) 1994-11-18 1995-08-29 Eli Lilly And Company Methods for lowering serum cholesterol
US5837284A (en) 1995-12-04 1998-11-17 Mehta; Atul M. Delivery of multiple doses of medications
US5980938A (en) 1996-07-15 1999-11-09 Eli Lilly And Company Effect of compounds that suppress induction of plasminogen activator inhibitor 1 (PAI-1)
EP0937060B1 (en) 1996-10-28 2002-12-11 Novo Nordisk A/S Cis-3,4-chroman derivatives useful in the prevention or treatment of estrogen related diseases or syndromes
US5840329A (en) 1997-05-15 1998-11-24 Bioadvances Llc Pulsatile drug delivery system
AU8102398A (en) 1997-07-09 1999-02-08 Central Drug Research Institute (dl)-2,3-diaryl-2h-1-benzopyrans
AU8102498A (en) 1997-07-09 1999-02-08 Central Drug Research Institute Preparation of diaryl-benzopyrans
KR20010022956A (ko) 1997-08-15 2001-03-26 듀크 유니버시티 에스트로겐-의존성 질병 및 장애의 예방방법 또는 치료방법
ID24568A (id) 1997-11-06 2000-07-27 American Home Prod Kontrasepsi oral yang mengandung anti-estrogen plus progestin
US6326392B1 (en) 1997-11-06 2001-12-04 American Home Products Corporation Anti-estrogen plus progestin containing oral contraceptives
WO1999060014A2 (en) 1998-03-30 1999-11-25 The Regents Of The University Of California Methods and compounds for modulating nuclear receptor coactivator binding
AU3457199A (en) 1998-03-30 1999-10-18 Arch Development Corporation Methods and compounds for modulating nuclear receptor activity
US7005428B1 (en) 1998-06-11 2006-02-28 Endorecherche, Inc. Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
WO2000009493A1 (en) 1998-08-14 2000-02-24 Schering Corporation Enantioselective synthesis
WO2000037083A1 (en) 1998-12-18 2000-06-29 Schering Corporation Oral antiestrogen pharmaceutical composition
US6638727B1 (en) 1999-01-26 2003-10-28 Cytyc Health Corporation Methods for identifying treating or monitoring asymptomatic patients for risk reduction or therapeutic treatment of breast cancer
US6716452B1 (en) 2000-08-22 2004-04-06 New River Pharmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
DE19916419B4 (de) 1999-04-08 2005-06-16 Schering Ag Kombinationspräparat aus Vitamin-D-Metaboliten oder Vitamin-D-Analoga und einem Östrogenpartialagonisten zur Behandlung von Osteoporose
BR0012354A (pt) 1999-07-06 2002-04-02 Endorech Inc Compostos e composição farmacêutica e métodos para tratar e/ou suprimir ganho de peso
WO2001026651A2 (en) 1999-10-14 2001-04-19 Endorecherche, Inc. Selective estrogen receptor modulators in the treatment or reduction of the risk of acquiring hypertension, cardiovascular diseases, and insulin resistance
GB0000313D0 (en) 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation
CO5271709A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos
CO5271696A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Procedimiento para reducir la morbilidad y el riesgo de mortalidad
CO5271697A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el tratamiento de afecciones que responden a un aumento de testosterona
CO5251465A1 (es) 2000-01-26 2003-02-28 Pfizer Prod Inc Composiciones y procedimientos para tratar la osteoporosis y reducir el colesterol
IL149990A0 (en) 2000-01-28 2002-12-01 Endorech Inc Selective estrogen receptor modulators in combination with estrogens
AU2001238700A1 (en) 2000-02-22 2001-09-03 Board Of Regents, The University Of Texas System Compositions and methods of use of het, a novel modulator of estrogen action
US6528681B2 (en) 2000-04-05 2003-03-04 Bristol-Meyers Squibb Pharma Company Halogenated triphenylethylene derivatives as selective estrogen receptor modulators
US20020013327A1 (en) 2000-04-18 2002-01-31 Lee Andrew G. Compositions and methods for treating female sexual dysfunction
US7863011B2 (en) 2000-05-10 2011-01-04 Signe Biopharma, Inc. Screening method for predicting susceptibility to breast cancer
US8119138B2 (en) 2000-05-10 2012-02-21 Signe Biopharma Inc. Anti-estrogen and immune modulator combinations for treating breast cancer
EP1177787A3 (en) 2000-07-28 2003-09-10 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating cataracts
ATE278421T1 (de) 2000-08-11 2004-10-15 Wyeth Corp Verfahren zur behandlung eines östrogenrezeptor positives karzinoms
US20020099013A1 (en) 2000-11-14 2002-07-25 Thomas Piccariello Active agent delivery systems and methods for protecting and administering active agents
AU2001289865B2 (en) 2000-09-08 2007-03-01 Pharmacia Italia S.P.A. Exemestane as chemopreventing agent
EP1192945A3 (en) 2000-09-21 2004-03-03 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating osteoarthritis
CA2424299A1 (en) 2000-10-06 2002-04-18 Biomedicines, Inc. Combination therapy for the treatment of estrogen-sensitive disease
IL145838A (en) 2000-10-16 2008-11-03 Pfizer Prod Inc Use of an estrogen agonist/antagonist for the manufacture of a medicament for treating vaginitis
EP1328522A2 (en) 2000-10-19 2003-07-23 Merck & Co., Inc. Estrogen receptor modulators
EP1333827A2 (en) 2000-10-19 2003-08-13 Merck & Co., Inc. Estrogen receptor modulators
US6750213B2 (en) 2000-10-19 2004-06-15 Merck & Co., Inc. Estrogen receptor modulators
AU781168B2 (en) 2001-01-26 2005-05-12 Pfizer Products Inc. Method of treating certain cancers using an estrogen agonist/antagonist
ATE337787T1 (de) 2001-01-26 2006-09-15 Pfizer Italia Srl Exemestan zur behandlung von hormonabhängigen störungen
US20040082557A1 (en) 2001-01-26 2004-04-29 Wajszczuk Charles Paul Methods for treating estrogen-dependent disorders
GB2374412A (en) 2001-04-11 2002-10-16 Karobio Ab Hypertension treatment and assay
WO2003016270A2 (en) 2001-08-11 2003-02-27 Bristol-Myers Squibb Pharma Company Selective estrogen receptor modulators
WO2003026568A2 (en) 2001-09-21 2003-04-03 Merck & Co., Inc. Androstanes as androgen receptor modulators
AU2002331916B2 (en) 2001-10-03 2008-07-24 Merck Sharp & Dohme Corp. Androstane 17-beta-carboxamides as androgen receptor modulators
CA2463142A1 (en) 2001-10-10 2003-04-24 Pharmacia Italia Spa Methods for preventing and treating bone loss with steroid compounds
US7196076B2 (en) 2001-10-19 2007-03-27 Merck & Co., Inc. Androgen receptor modulators and methods of use thereof
US7105679B2 (en) * 2001-12-19 2006-09-12 Kanojia Ramesh M Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
EP1465619A1 (en) 2002-01-14 2004-10-13 Nordic Bioscience A/S Suppression of cartilage degradation via the estrogen receptor
AU2003206442A1 (en) 2002-02-21 2003-09-09 Pantarhei Bioscience B.V. Estrogenic component for treating decreased libido in women
CN1625602A (zh) 2002-03-13 2005-06-08 霍夫曼-拉罗奇有限公司 选择药物敏感性决定因子的方法和利用所选择的因子预测药物敏感性的方法
AU2003218235B2 (en) 2002-03-13 2008-05-15 Merck Sharp & Dohme Corp. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
US20030225132A1 (en) 2002-04-11 2003-12-04 Dininno Frank P. Estrogen receptor modulators
DK1501819T3 (da) * 2002-04-24 2011-01-10 Merck Sharp & Dohme Østrogenreceptormodulatorer
AU2003223754B2 (en) 2002-04-30 2007-08-16 Merck Sharp & Dohme Corp. 4-azasteroid derivatives as androgen receptor modulators
WO2004000225A2 (en) 2002-06-25 2003-12-31 Wyeth Use of thio-oxindole derivatives in treatment of hormone-related conditions
KR20050013247A (ko) 2002-06-25 2005-02-03 와이어쓰 호르몬-관련 병리상태를 치료하기 위한사이클로티오카바메이트 유도체의 용도
US7622592B2 (en) 2002-11-01 2009-11-24 Merck & Co., Inc. Carbonylamino-benzimidazole derivatives as androgen receptor modulators
DK1622630T3 (da) 2003-05-07 2012-12-17 Osteologix As P009368epdk1
AU2004238238C1 (en) 2003-05-07 2010-01-14 Merck Sharp & Dohme Corp. Androgen receptor modulators and methods of use thereof
US20040248989A1 (en) 2003-06-05 2004-12-09 Risto Santti Method for the treatment or prevention of lower urinary tract symptoms
CN1812824A (zh) 2003-06-30 2006-08-02 麦克公司 作为雄激素受体调节剂的17－乙酰氨基－4－氮杂甾体衍生物
CN1816370A (zh) 2003-06-30 2006-08-09 麦克公司 用作雄激素受体调节剂的17－乙酰氨基－4－氮杂甾族化合物衍生物
US20070088028A1 (en) 2003-06-30 2007-04-19 Dankulich William P 17-Acetamido-4-azasteroid derivatives as androgen receptor modulators
CA2530047A1 (en) 2003-06-30 2005-02-03 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
CA2537663A1 (en) 2003-09-10 2005-03-24 Merck & Co., Inc. 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
AU2004272007B2 (en) 2003-09-10 2009-05-28 Merck Sharp & Dohme Corp. 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
US7442833B2 (en) 2003-10-08 2008-10-28 Smithkline Beecham Corporation Triphenylethylene compounds as selective estrogen receptor modulators
US7312229B2 (en) 2003-10-31 2007-12-25 Merck & Co., Inc. 21-Heterocyclic-4-azasteroid derivatives as androgen receptor modulators
WO2005073190A1 (en) 2004-01-29 2005-08-11 Eli Lilly And Company Selective estrogen receptor modulators
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
EP1758653A2 (en) 2004-06-17 2007-03-07 Osteologix A/S Treatments comprising strontium for rheumatic and arthritic diseases and pain
WO2005123130A2 (en) 2004-06-17 2005-12-29 Osteologix A/S Improved treatments of rheumatic and arthritic diseases comprising combinations of a 5-lipoxygenase inhibitor
KR20070059110A (ko) 2004-09-03 2007-06-11 호르모스 메디칼 리미티드 안드로겐 결핍의 치료 또는 예방에 사용하는 제제의 제조를위한 선택적 에스트로겐 수용체 조절자의 용도
SG155258A1 (en) 2004-10-20 2009-09-30 Endorech Inc Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 cgmp phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausa
WO2006084937A1 (en) 2005-02-14 2006-08-17 Leskelae Hannu-Ville Method for diagnosing and treating women with increased response to hormonal replacement therapy
US20070078114A1 (en) 2005-09-02 2007-04-05 Myriad Genetics, Incorporated Combination therapy for alzheimer's disease and other diseases
WO2007098090A2 (en) 2006-02-17 2007-08-30 Novacea, Inc. Treatment of hyperproliferative diseases with n-oxides of estrogen receptor modulators
US20080268041A1 (en) 2007-04-23 2008-10-30 Jens Hoffmann Combination of progesterone-receptor antagonist together with none-steroidal antiestrogen for use in brca mediated diseases
DE102007026877A1 (de) 2007-06-08 2008-12-11 Bayer Schering Pharma Aktiengesellschaft Verwendung des Fibroblastenwachstumsfaktors 7 (Fgf7) und des Rezeptors Fgfr2b als Biomarker
WO2009143309A2 (en) 2008-05-21 2009-11-26 Trustees Of Dartmouth College Female reproductive tract and anal prophylaxes
WO2010107474A1 (en) 2009-03-16 2010-09-23 The Research Foundation Of State University Of New York Antiestrogens for breast cancer therapy
US20100317635A1 (en) 2009-06-16 2010-12-16 Endorecherche, Inc. Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators
HRP20170786T1 (hr) * 2010-06-10 2017-08-11 Seragon Pharmaceuticals, Inc. Modulatori estrogenskog receptora i njihove uporabe
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
DE102010030538A1 (de) 2010-06-25 2011-12-29 Bayer Schering Pharma Aktiengesellschaft 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
GB2483736B (en) * 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
JP5886873B2 (ja) 2010-12-24 2016-03-16 メルク・シャープ・エンド・ドーム・ベー・フェー Ｎ置換アゼチジン誘導体
MX357496B (es) 2011-12-14 2018-07-11 Seragon Pharmaceuticals Inc Moduladores del receptor de estrógenos fluorados y sus usos.
AU2012353660A1 (en) 2011-12-16 2014-06-12 Olema Pharmaceuticals, Inc. Novel benzopyran compounds, compositions and uses thereof

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0470310A1 (en) * 1990-08-09 1992-02-12 Council of Scientific and Industrial Research Novel benzopyrans and process for their production
JPH11500133A (ja) * 1995-02-21 1999-01-06 アンドルシェルシュ・インコーポレイテッド ベンゾピラン含有化合物およびその使用方法
JP2007191484A (ja) * 1998-06-11 2007-08-02 Endorecherche Inc 選択的エストロゲン受容体モジュレーターと性ステロイド前駆体の組合せの医学的使用
US6262270B1 (en) * 1998-08-14 2001-07-17 Schering Corporation Enantioselective synthesis
WO2001068634A1 (de) * 2000-03-15 2001-09-20 Schering Aktiengesellschaft 4-fluoralkyl-2h-benzopyrane mit antiestrogener wirksamkeit
JP2005513133A (ja) * 2001-12-19 2005-05-12 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド エストロゲン受容体調節剤としての四環状複素化合物
WO2004091488A2 (en) * 2003-04-14 2004-10-28 Merck & Co., Inc. Estrogen receptor modulators

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 15, no. 6, JPN6015024818, 2005, pages 1675 - 1681, ISSN: 0003100245 *
CHEMICAL SOCIETY REVIEWS, vol. 37, no. 2, JPN6015024826, 2008, pages 320 - 330, ISSN: 0003100251 *
JOURNAL OF MEDICINAL CHEMISTRY, vol. 33, no. 12, JPN6015024819, 1990, pages 3216 - 3222, ISSN: 0003100246 *
JOURNAL OF MEDICINAL CHEMISTRY, vol. 49, no. 11, JPN6015024821, 2006, pages 3056 - 3059, ISSN: 0003100247 *
JOURNAL OF MEDICINAL CHEMISTRY, vol. 52, no. 23, JPN6015024824, 2009, pages 7544 - 7569, ISSN: 0003100249 *
ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 11, no. 4, JPN6015024825, 2007, pages 731 - 738, ISSN: 0003100250 *
ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 13, no. 1, JPN6015024822, 2009, pages 102 - 105, ISSN: 0003100248 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017507964A (ja) * 2014-03-13 2017-03-23 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト エストロゲン受容体モジュレーターを用いた治療的組合せ
JP2017509631A (ja) * 2014-03-13 2017-04-06 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト エストロゲン受容体突然変異体を調節する方法及び組成物
JP2018520116A (ja) * 2015-05-26 2018-07-26 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 複素環式エストロゲン受容体モジュレーター及びその使用
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JP7052111B2 (ja) 2015-10-27 2022-04-11 スン プハルマ アドバンセド リサーチ カンパニー リミテド 新規ヘテロ環状抗エストロゲン剤

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