ES2627692T3 - Moduladores de receptores de estrógenos y usos de los mismos - Google Patents

Moduladores de receptores de estrógenos y usos de los mismos Download PDF

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Publication number
ES2627692T3
ES2627692T3 ES11793115.4T ES11793115T ES2627692T3 ES 2627692 T3 ES2627692 T3 ES 2627692T3 ES 11793115 T ES11793115 T ES 11793115T ES 2627692 T3 ES2627692 T3 ES 2627692T3
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Spain
Prior art keywords
substituted
unsubstituted
phenyl
methyl
chromen
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ES11793115.4T
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English (en)
Spanish (es)
Inventor
Mehmet Kahraman
Steven P. Govek
Johnny Y. Nagasawa
Nicholas D. Smith
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Aragon Pharmaceuticals Inc
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Aragon Pharmaceuticals Inc
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    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/02—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
    • 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

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  • Urology & Nephrology (AREA)
  • Obesity (AREA)
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  • Gastroenterology & Hepatology (AREA)
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ES11793115.4T 2010-06-10 2011-06-08 Moduladores de receptores de estrógenos y usos de los mismos Active ES2627692T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US35353110P 2010-06-10 2010-06-10
US353531P 2010-06-10
PCT/US2011/039669 WO2011156518A2 (en) 2010-06-10 2011-06-08 Estrogen receptor modulators and uses thereof

Publications (1)

Publication Number Publication Date
ES2627692T3 true ES2627692T3 (es) 2017-07-31

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Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE033581T2 (hu) 2010-06-10 2017-12-28 Seragon Pharmaceuticals Inc Ösztrogén receptor modulátorok és alkalmazásaik
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
JP6112625B2 (ja) * 2011-12-14 2017-04-12 セラゴン ファーマシューティカルズ，インク． フッ素化したエストロゲン受容体モジュレーターおよびその使用
PE20150099A1 (es) 2011-12-16 2015-01-30 Olema Pharmaceuticals Inc Compuestos novedosos de benzopirano, composiciones y usos de los mismos
EA031077B1 (ru) * 2013-06-19 2018-11-30 Серагон Фармасьютикалз, Инк. Модулятор рецептора эстрогена и его применения
BR112015030595A2 (pt) 2013-06-19 2017-07-25 Seragon Pharmaceuticals Inc moduladores de receptor de estrogênio de azetidina e usos dos mesmos
WO2014203129A1 (en) * 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Combinations of benzopyran compounds, compositions and uses thereof
WO2014203132A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Substituted benzopyran compounds, compositions and uses thereof
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
CA2941161A1 (en) 2014-03-13 2015-09-17 F.Hoffmann-La Roche Ag Methods and compositions for modulating estrogen receptor mutants
EP3233818A1 (en) * 2014-12-18 2017-10-25 F. Hoffmann-La Roche AG Derivatives of 2,3-diphenylchromene useful for the treatment of cancer
KR102785474B1 (ko) 2014-12-18 2025-03-26 에프. 호프만-라 로슈 아게 테트라하이드로-피리도[3,4-b]인돌 에스트로겐 수용체 조절제 및 이의 용도
CN107406424B (zh) 2014-12-18 2020-08-25 豪夫迈·罗氏有限公司 雌激素受体调节剂及其用途
EP3303326B1 (en) * 2015-05-26 2020-12-16 H. Hoffnabb-La Roche Ag Heterocyclic estrogen receptor modulators and uses thereof
WO2017024318A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses
KR102710603B1 (ko) 2015-10-01 2024-09-27 올레마 파마슈티컬스 인코포레이티드 테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물
MX385940B (es) 2015-10-27 2025-03-18 Sun Pharma Advanced Res Co Ltd Nuevos antiestrógenos heterocíclicos.
US10519148B2 (en) 2015-11-12 2019-12-31 Zhejiang Hisun Pharmaceutical Co., Ltd. Acrylic acid derivative, preparation method and use in medicine thereof
SMT202300018T1 (it) 2015-12-09 2023-03-17 Univ Illinois Downregolatori del recettore degli estrogeni a base di benzotiofene
CN109362222B (zh) 2016-02-05 2021-03-19 益方生物科技(上海)股份有限公司 选择性雌激素受体降解物及其用途
CN112745316A (zh) 2016-04-01 2021-05-04 里科瑞尔姆Ip控股有限责任公司 雌激素受体调节剂
US10125135B2 (en) 2016-04-20 2018-11-13 Astrazeneca Ab Chemical compounds
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
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
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
EP3454862B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
US20180002344A1 (en) 2016-06-16 2018-01-04 Genentech, Inc. Heteroaryl estrogen receptor modulators and uses thereof
EP3858835A1 (en) 2016-07-01 2021-08-04 G1 Therapeutics, Inc. Pyrimidine-based antiproliferative agents
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
TWI735681B (zh) 2016-10-24 2021-08-11 瑞典商阿斯特捷利康公司 化合物
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
KR102707399B1 (ko) 2017-01-05 2024-09-13 래디어스 파마슈티컬스, 인코포레이티드 Rad1901-2hcl의 다형 형태
EP3565558B1 (en) 2017-01-06 2023-12-06 G1 Therapeutics, Inc. Combination therapy with a serd compound and a cdk4/6 inhibitor for the treatment of cancer
PT3494116T (pt) 2017-01-30 2020-01-28 Astrazeneca Ab Moduladores de recetores de estrogénio
EP3580212A4 (en) 2017-02-08 2021-03-17 Dana Farber Cancer Institute, Inc. REGULATION OF CHEMERIC ANTIGEN RECEPTORS
KR20190117582A (ko) 2017-02-10 2019-10-16 쥐원 쎄라퓨틱스, 인크. 벤조티오펜 에스트로겐 수용체 조정제
EP4717317A2 (en) 2017-06-20 2026-04-01 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
FI3645001T3 (fi) 2017-06-29 2024-09-25 G1 Therapeutics Inc Git38:n morfisia muotoja ja niiden valmistusmenetelmiä
WO2019057201A1 (zh) * 2017-09-25 2019-03-28 罗欣生物科技（上海）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
JP7585034B2 (ja) 2017-10-18 2024-11-18 ノバルティス アーゲー 選択的タンパク質分解のための組成物及び方法
TW201922291A (zh) 2017-11-16 2019-06-16 瑞士商諾華公司 組合療法
JP2021519337A (ja) 2018-03-26 2021-08-10 シー４ セラピューティクス， インコーポレイテッド Ｉｋａｒｏｓの分解のためのセレブロン結合剤
LT3810283T (lt) 2018-06-21 2023-08-25 F. Hoffmann-La Roche Ag 3-((1r,3r)-1-(2,6-difluor-4-((1-(3-fluorpropil)azetidin-3- il)amino) fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)- 2,2- difluorpropan-1-olio tartrato druskos kietosios formos, jų paruošimo procesas ir jų naudojimo būdai vėžiui gydyti
IL279853B2 (en) 2018-07-04 2025-01-01 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
CA3109090A1 (en) 2018-08-17 2020-02-20 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for the treatment of breast cancer
WO2020051235A1 (en) 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
KR20210106437A (ko) 2018-12-20 2021-08-30 노파르티스 아게 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 및 약학적 조합물
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
CN113348163B (zh) 2019-02-12 2024-10-08 雷迪厄斯制药公司 方法和化合物
CN113490528B (zh) 2019-02-15 2024-12-03 诺华股份有限公司 3-(1-氧代-5-(哌啶-4-基)异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途
EP3924055B1 (en) 2019-02-15 2024-04-03 Novartis AG Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CN120172958A (zh) 2019-04-12 2025-06-20 C4医药公司 Ikaros和aiolos的三环降解物
US20220251152A1 (en) 2019-04-24 2022-08-11 Novartis Ag Compositions and methods for selective protein degradation
KR20220024106A (ko) 2019-05-20 2022-03-03 노파르티스 아게 Mcl-1 억제제 항체-약물 접합체 및 사용 방법
CN114929696A (zh) 2019-05-24 2022-08-19 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
MX2022000279A (es) 2019-07-07 2022-02-03 Olema Pharmaceuticals Inc Regimenes de antagonistas del receptor de estrogeno.
US11014915B2 (en) 2019-07-22 2021-05-25 Sun Pharma Advanced Research Company Limited Selective estrogen receptor degrader
CA3148221A1 (en) 2019-08-06 2021-02-11 Recurium Ip Holdings, Llc Estrogen receptor modulators for treating mutants
BR112022011827A2 (pt) 2019-12-20 2022-08-30 C4 Therapeutics Inc Composto, composição farmacêutica, uso de um composto, métodos para tratamento ou profilaxia de câncer e para tratar um paciente com um distúrbio mediado por receptor do fator de crescimento epidérmico, e, invenção
MX2022007759A (es) 2019-12-20 2022-07-19 Novartis Ag Combinacion del anticuerpo anti tim-3 mbg453 y anticuerpo anti tgf-beta nis793, con o sin decitabina o el anticuerpo anti pd-1 spartalizumab, para el tratamiento de mielofibrosis y sindrome mielodisplasico.
AU2021231898A1 (en) 2020-03-05 2022-10-27 C4 Therapeutics, Inc. Compounds for targeted degradation of BRD9
WO2021214253A1 (en) 2020-04-24 2021-10-28 Astrazeneca Ab Dosage regimen for the treatment of cancer
PE20221838A1 (es) 2020-04-24 2022-11-29 Astrazeneca Ab Formulaciones farmaceuticas
ES3048084T3 (en) 2020-05-19 2025-12-09 Pharmacosmos Holding As Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders
CN115916199A (zh) 2020-06-23 2023-04-04 诺华股份有限公司 包含3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物的给药方案
US20230271940A1 (en) 2020-08-03 2023-08-31 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
WO2022066774A1 (en) 2020-09-23 2022-03-31 Achillion Pharmaceuticals, Inc. Pharmaceutical compounds for the treatment of complement mediated disorders
CA3200858A1 (en) 2020-11-24 2022-06-02 Novartis Ag Anti-cd48 antibodies, antibody drug conjugates, and uses thereof
US20240042051A1 (en) 2020-11-24 2024-02-08 Francesca Rocchetti Mcl-1 inhibitor antibody-drug conjugates and methods of use
EP4267578A4 (en) 2020-12-23 2024-11-20 Recurium IP Holdings, LLC ESTROGEN RECEPTOR MODULATORS
CN117794929A (zh) 2021-02-02 2024-03-29 法国施维雅药厂 选择性bcl-xl protac化合物及使用方法
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
WO2022261250A1 (en) 2021-06-08 2022-12-15 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
US20250339547A1 (en) 2022-05-20 2025-11-06 Novartis Ag Met bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
IL317102A (en) 2022-05-20 2025-01-01 Novartis Ag EPHA2 BCL-XL inhibitor antibody-drug conjugates and methods of using them
JP2025525917A (ja) 2022-08-03 2025-08-07 ブリストル－マイヤーズ スクイブ カンパニー Ｒｅｔタンパク質を調節するための化合物
CN120569388A (zh) 2022-11-04 2025-08-29 百时美施贵宝公司 Ret-ldd蛋白降解剂
CN120530116A (zh) 2022-11-04 2025-08-22 百时美施贵宝公司 Ret-ldd蛋白抑制剂
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
PY24103486A (es) 2023-11-22 2025-06-06 Servier Lab Conjugados de anticuerpo anti-cd74-fármaco y métodos de uso de los mismos
TW202543650A (zh) 2024-03-08 2025-11-16 美商海爾達醫療運營公司 異雙官能化合物及其在治療疾病中之用途
WO2025215536A1 (en) 2024-04-10 2025-10-16 Novartis Ag Macrocyclic panras inhibitors for the treatment of cancer

Family Cites Families (118)

* 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
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
US5686465A (en) 1988-10-31 1997-11-11 Endorecherche Inc. Sex steroid activity inhibitors
US5395842A (en) 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
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
EP0470310B1 (en) * 1990-08-09 1995-11-29 Council of Scientific and Industrial Research Novel benzopyrans and process for their production
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
US6060503A (en) 1991-12-02 2000-05-09 Endorecherche, Inc. Benzopyran-containing compounds and method for their use
ES2105525T3 (es) 1993-06-24 1997-10-16 Lilly Co Eli 2-fenil-3-aroilbenzotiofenos antiestrogenicos como agentes hipoglicemicos.
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
UA41909C2 (uk) 1994-07-22 2001-10-15 Елі Ліллі Енд Компані Використання комбінації сполук для інгібірування остеопорозу, фармацевтичний препарат
US5446071A (en) 1994-11-18 1995-08-29 Eli Lilly And Company Methods for lowering serum cholesterol
US5637598A (en) 1994-11-18 1997-06-10 Eli Lilly And Company Methods of inhibiting bone loss
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)
WO1998018776A1 (en) 1996-10-28 1998-05-07 Novo Nordisk A/S Novel 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
WO1999002513A1 (en) 1997-07-09 1999-01-21 Novo Nordisk A/S Preparation of diaryl-benzopyrans
AU8102398A (en) 1997-07-09 1999-02-08 Central Drug Research Institute (dl)-2,3-diaryl-2h-1-benzopyrans
BR9811946A (pt) 1997-08-15 2000-08-22 Univ Duke Método para prevenção ou tratamento de distúrbios e doenças dependentes de estrogênio
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
CA2323575A1 (en) 1998-03-30 1999-11-25 Regents Of The University Of California Methods and compounds for modulating nuclear receptor coactivator binding
KR20010042373A (ko) 1998-03-30 2001-05-25 린다 에스. 스티븐슨 핵 수용체 활성을 조절하는 방법 및 화합물
US6465445B1 (en) 1998-06-11 2002-10-15 Endorecherche, Inc. Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
US7005428B1 (en) 1998-06-11 2006-02-28 Endorecherche, Inc. Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
DE69905376T2 (de) 1998-08-14 2003-10-09 Schering Corp., Kenilworth Enanthioauswählende synthese
US6262270B1 (en) * 1998-08-14 2001-07-17 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
TR200502284T2 (tr) 1999-07-06 2005-08-22 Endorecherche, Inc. Kilo alımını tedavi ve/veya önleme metotları
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
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
CO5271709A1 (es) 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos
CO5251465A1 (es) 2000-01-26 2003-02-28 Pfizer Prod Inc Composiciones y procedimientos para tratar la osteoporosis y reducir el colesterol
CN1400904A (zh) 2000-01-28 2003-03-05 恩多研究公司 与雌激素联合的选择性雌激素受体调节剂
WO2001063292A2 (en) 2000-02-22 2001-08-30 Board Of Regents, The University Of Texas System Compositions and methods of use of het, a novel modulator of estrogen action
DE10013782A1 (de) 2000-03-15 2001-10-18 Schering Ag 4-Fluoralkyl-2H-benzopyrane mit antiestrogener Wirksamkeit, Verfahren zu ihrer Herstellung, pharmazeutische Präparate, die diese enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln
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
US8119138B2 (en) 2000-05-10 2012-02-21 Signe Biopharma Inc. Anti-estrogen and immune modulator combinations for treating breast cancer
US7863011B2 (en) 2000-05-10 2011-01-04 Signe Biopharma, Inc. Screening method for predicting susceptibility to breast cancer
EP1177787A3 (en) 2000-07-28 2003-09-10 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating cataracts
JP2004507465A (ja) 2000-08-11 2004-03-11 ワイス エストロゲン受容体陽性癌腫の治療方法
US20020099013A1 (en) 2000-11-14 2002-07-25 Thomas Piccariello Active agent delivery systems and methods for protecting and administering active agents
CN1729002A (zh) 2000-09-08 2006-02-01 法玛西雅意大利公司 依西美坦作为化学预防剂
EP1192945A3 (en) 2000-09-21 2004-03-03 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating osteoarthritis
PL361874A1 (en) 2000-10-06 2004-10-04 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
AU2002221269A1 (en) 2000-10-19 2002-04-29 Merck & Co., Inc. Estrogen receptor modulators
US6750213B2 (en) 2000-10-19 2004-06-15 Merck & Co., Inc. Estrogen receptor modulators
IL154984A0 (en) 2000-10-19 2003-10-31 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
JP2004519490A (ja) 2001-01-26 2004-07-02 フアルマシア・イタリア・エツセ・ピー・アー エキセメスタンによるホルモン依存性異常症の組合せ治療方法
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
CA2459943A1 (en) 2001-09-21 2003-04-03 Merck & Co., Inc. Androstanes as androgen receptor modulators
WO2003029268A1 (en) 2001-10-03 2003-04-10 Merck & Co., Inc. Androstane 17-beta-carboxamides as androgen receptor modulators
IL161162A0 (en) 2001-10-10 2004-08-31 Pharmacia Italia Spa Methods for preventing and treating bone loss with steroid compounds
JP2005509629A (ja) 2001-10-19 2005-04-14 メルク　エンド　カムパニー　インコーポレーテッド アンドロゲン受容体モジュレーターおよびその使用方法
US7105679B2 (en) * 2001-12-19 2006-09-12 Kanojia Ramesh M Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
IL162295A0 (en) * 2001-12-19 2005-11-20 Ortho Mcneil Pharm Inc Tetracyclic heterocompounds as estrogen receptor modulators
EP1465619A1 (en) 2002-01-14 2004-10-13 Nordic Bioscience A/S Suppression of cartilage degradation via the estrogen receptor
WO2003070253A1 (en) 2002-02-21 2003-08-28 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
HRP20040822A2 (en) 2002-03-13 2005-06-30 Merck & Co. Inc. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
US20030225132A1 (en) 2002-04-11 2003-12-04 Dininno Frank P. Estrogen receptor modulators
ATE481397T1 (de) 2002-04-24 2010-10-15 Merck Sharp & Dohme Modulatoren des östrogenrezeptors
CA2484173A1 (en) 2002-04-30 2003-11-13 Merck & Co., Inc. 4-azasteroid derivatives as androgen receptor modulators
CN1662241A (zh) 2002-06-25 2005-08-31 惠氏公司 环硫代氨基甲酸酯衍生物在治疗与激素有关的病症中的用途
IL165395A0 (en) 2002-06-25 2006-01-15 Wyeth Corp Use of thio-oxubdile derivatives in treatment of hormone-related conditions
EP1581217A4 (en) 2002-11-01 2007-07-11 Merck & Co Inc CARBONYLAMINO-BENZIMIDAZOLE DERIVATIVES AS MODULATORS OF ANDROGENIC RECEPTORS
WO2004091488A2 (en) * 2003-04-14 2004-10-28 Merck & Co., Inc. Estrogen receptor modulators
ES2394782T3 (es) 2003-05-07 2013-02-05 Osteologix A/S Composición con estroncio y vitamina D para la profilaxis y/o tratamiento de afecciones de cartílagos y/o huesos
CA2524409C (en) 2003-05-07 2011-12-20 Merck & Co., Inc. 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
US7329750B2 (en) 2003-06-30 2008-02-12 Merck & Co., Inc. 17-Acetamido-4-azasteroid derivatives as androgen receptor modulators
CA2530025A1 (en) 2003-06-30 2005-01-20 William P. Dankulich 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
AU2004255749B2 (en) 2003-06-30 2008-12-18 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
JP2007521297A (ja) 2003-06-30 2007-08-02 メルク　エンド　カムパニー　インコーポレーテッド アンドロゲン受容体モジュレータとしての１７−アセトアミド−４−アザステロイド誘導体
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
DE602004014806D1 (de) 2003-10-08 2008-08-14 Smithkline Beecham Corp Triphenylethyleneverbindungen als selektive modulatoren des östrogenrezeptors
EP1696925A4 (en) 2003-10-31 2009-11-18 Merck & Co Inc 21-Heterocyclic 4-AZASTEROID DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS
EP1713770A1 (en) 2004-01-29 2006-10-25 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
US20090035315A1 (en) 2004-06-17 2009-02-05 Stephan Christgau Method of Improving Treatments in Rheumatic and Arthritic Diseases
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
EP1786408A4 (en) 2004-09-03 2010-07-28 Hormos Medical Ltd USE OF A SELECTIVE ESTROGEN RECEPTOR MODULATOR IN THE MANUFACTURE OF A PHARMACEUTICAL PREPARATION USED IN A METHOD OF TREATING OR PREVENTING ENDROGENIC INJURIES
US8835413B2 (en) 2004-10-20 2014-09-16 Endorecherche, 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 postmenopausal women
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
HUE033581T2 (hu) 2010-06-10 2017-12-28 Seragon Pharmaceuticals Inc Ösztrogén receptor modulátorok és alkalmazásaik
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
CA2819299A1 (en) 2010-12-24 2012-06-28 Merck Sharp & Dohme B.V. N-substituted azetidine derivatives
JP6112625B2 (ja) 2011-12-14 2017-04-12 セラゴン ファーマシューティカルズ，インク． フッ素化したエストロゲン受容体モジュレーターおよびその使用
PE20150099A1 (es) 2011-12-16 2015-01-30 Olema Pharmaceuticals Inc Compuestos novedosos de benzopirano, composiciones y usos de los mismos

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