KR102785173B1 - 벤조티오펜-기반 선택적 에스트로겐 수용체 하향조절제 - Google Patents

벤조티오펜-기반 선택적 에스트로겐 수용체 하향조절제 Download PDF

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KR102785173B1
KR102785173B1 KR1020187019088A KR20187019088A KR102785173B1 KR 102785173 B1 KR102785173 B1 KR 102785173B1 KR 1020187019088 A KR1020187019088 A KR 1020187019088A KR 20187019088 A KR20187019088 A KR 20187019088A KR 102785173 B1 KR102785173 B1 KR 102785173B1
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KR20180088457A (ko
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그레고리 알. 대처
루이 시옹
지옹 챠오
데브라 에이. 토네티
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더 보드 오브 트러스티즈 오브 더 유니버시티 오브 일리노이
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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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/64—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Steroid Compounds (AREA)
KR1020187019088A 2015-12-09 2016-12-09 벤조티오펜-기반 선택적 에스트로겐 수용체 하향조절제 Active KR102785173B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562264971P 2015-12-09 2015-12-09
US62/264,971 2015-12-09
US201662322878P 2016-04-15 2016-04-15
US62/322,878 2016-04-15
PCT/US2016/066023 WO2017100712A1 (en) 2015-12-09 2016-12-09 Benzothiophene-based selective estrogen receptor downregulators

Publications (2)

Publication Number Publication Date
KR20180088457A KR20180088457A (ko) 2018-08-03
KR102785173B1 true KR102785173B1 (ko) 2025-03-25

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Country Status (25)

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US (7) US10118910B2 (enExample)
EP (2) EP3386968B1 (enExample)
JP (2) JP6920709B2 (enExample)
KR (1) KR102785173B1 (enExample)
CN (2) CN108699024B (enExample)
AU (1) AU2016366680B2 (enExample)
BR (1) BR112018011607B1 (enExample)
CA (1) CA3008020C (enExample)
DK (1) DK3386500T3 (enExample)
EA (1) EA038180B1 (enExample)
ES (1) ES2935125T3 (enExample)
HR (1) HRP20221462T1 (enExample)
HU (1) HUE061065T2 (enExample)
IL (1) IL259566B (enExample)
LT (1) LT3386500T (enExample)
MX (2) MX373946B (enExample)
NZ (1) NZ743651A (enExample)
PL (1) PL3386500T3 (enExample)
PT (1) PT3386500T (enExample)
RS (1) RS63791B1 (enExample)
RU (1) RU2747802C2 (enExample)
SI (1) SI3386500T1 (enExample)
SM (1) SMT202300018T1 (enExample)
WO (2) WO2017100712A1 (enExample)
ZA (2) ZA201803422B (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20221462T1 (hr) * 2015-12-09 2023-01-20 The Board Of Trustees Of The University Of Illinois Selektivni nishodni regulatori receptora estrogena na bazi benzotiofena
US10599150B2 (en) 2016-09-29 2020-03-24 The Charles Stark Kraper Laboratory, Inc. Autonomous vehicle: object-level fusion
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
KR20190117582A (ko) 2017-02-10 2019-10-16 쥐원 쎄라퓨틱스, 인크. 벤조티오펜 에스트로겐 수용체 조정제
WO2019006393A1 (en) 2017-06-29 2019-01-03 G1 Therapeutics, Inc. Morphic forms of git38 and methods of manufacture thereof
CN112041307B (zh) * 2018-02-06 2024-02-09 伊利诺伊大学评议会 作为选择性雌激素受体降解剂的取代的苯并噻吩类似物
CA3109385A1 (en) * 2018-08-16 2020-02-20 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators to treat medical disorders
US10741313B1 (en) 2019-02-06 2020-08-11 Eaton Intelligent Power Limited Bus bar assembly with integrated surge arrestor
US11249184B2 (en) 2019-05-07 2022-02-15 The Charles Stark Draper Laboratory, Inc. Autonomous collision avoidance through physical layer tracking
BR112021022216A2 (pt) * 2019-05-09 2021-12-28 Sanofi Sa Ácido 6-(2,4-diclorofenil)-5-[4-[(3s)-1-(3-fluoropropil)pirrolidin-3-il]oxifenil]-8,9-di-hidro-7h-benzo[7]anuleno-2-carboxílico para uso em pacientes com câncer de mama metastático ou avançado
US20220233534A1 (en) * 2019-07-08 2022-07-28 Dermavant Sciences GmbH Cerdulatinib-containing topical skin pharmaceutical compositions and uses thereof
AU2021273744A1 (en) 2020-05-19 2022-12-08 Pharmacosmos Holding A/S Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders
CN115710248B (zh) * 2022-11-18 2024-06-21 南京中医药大学 新型选择性雌激素受体下调剂化合物、制备方法及用途
CN116574054B (zh) * 2023-05-15 2025-01-28 南京中医药大学 选择性雌激素受体下调剂化合物、制备方法及用途
WO2025147568A1 (en) * 2024-01-05 2025-07-10 Starton Therapeutics, Inc. Solid state active pharmaceutical compositions for transdermal drug delivery

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014066695A1 (en) * 2012-10-24 2014-05-01 The Board Of Trustees Of The University Of Illinois Compositions and methods for treating estrogen-related medical disorders
WO2014130310A1 (en) * 2013-02-19 2014-08-28 Novartis Ag Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders

Family Cites Families (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1947085A (en) 1931-09-22 1934-02-13 Westinghouse Electric & Mfg Co Electrical apparatus
US4133814A (en) 1975-10-28 1979-01-09 Eli Lilly And Company 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents
US4418068A (en) 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
DE4126999A1 (de) 1991-08-16 1993-02-18 Basf Ag Herbizide mittel, enthaltend 3-aminobenzo(b)thiophene als antidots
CA2083891A1 (en) 1991-12-03 1993-06-04 Angus Murray Macleod Heterocyclic compounds, compositions containing them and their use in therapy
JPH05345780A (ja) * 1991-12-24 1993-12-27 Kumiai Chem Ind Co Ltd ピリミジンまたはトリアジン誘導体及び除草剤
SK280617B6 (sk) 1992-01-16 2000-05-16 Hoechst Aktiengesellschaft Arylcykloalkylové deriváty, spôsob ich prípravy, f
TW366342B (en) 1992-07-28 1999-08-11 Lilly Co Eli The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss
EP0622673B1 (en) 1993-04-24 1998-02-04 Kodak Limited Photographic colour couplers and photographic materials containing them
US5478847A (en) 1994-03-02 1995-12-26 Eli Lilly And Company Methods of use for inhibiting bone loss and lowering serum cholesterol
DE69635254T2 (de) 1995-07-07 2006-07-13 Astrazeneca Ab Ortho-substituierte aromatische Verbindungen, die drei (Het)aryl-Ringe enthalten, deren Herstellung und deren Verwendung als Prostaglandin-E2-(PGE2)-Antagonisten
US6458811B1 (en) 1996-03-26 2002-10-01 Eli Lilly And Company Benzothiophenes formulations containing same and methods
US5998402A (en) 1996-04-19 1999-12-07 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
US5880137A (en) 1996-04-19 1999-03-09 American Home Products Corporation 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents
TW397821B (en) 1996-04-19 2000-07-11 American Home Produits Corp 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof
US5780497A (en) 1996-04-19 1998-07-14 American Home Products Corporation 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents
ATE411016T1 (de) * 1997-08-15 2008-10-15 Univ Duke Verfahren zur prophylaxis oder behandlung von östrogen-abhängigen krankheiten
WO1999018101A1 (en) 1997-10-03 1999-04-15 Eli Lilly And Company Benzothiophenes
US6005102A (en) 1997-10-15 1999-12-21 American Home Products Corporation Aryloxy-alkyl-dialkylamines
UA68365C2 (en) 1997-11-06 2004-08-16 Wyeth Corp Peroral contraception by combination of anti-estrogen and progestin
US6326392B1 (en) 1997-11-06 2001-12-04 American Home Products Corporation Anti-estrogen plus progestin containing oral contraceptives
US6479535B1 (en) 1998-05-15 2002-11-12 Wyeth 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations
US6583170B1 (en) 1998-05-15 2003-06-24 Wyeth 2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol and estrogen formulations
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
US7091240B2 (en) 2000-03-10 2006-08-15 Oxigene, Inc. Tubulin binding ligands and corresponding prodrug constructs
US20020013327A1 (en) 2000-04-18 2002-01-31 Lee Andrew G. Compositions and methods for treating female sexual dysfunction
WO2002003990A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted insole compounds for treating excessive intraocular pressure
MXPA02012896A (es) 2000-07-06 2003-10-24 Wyeth Corp Combinaciones de estatinas, agentes estrogenicos y opcionalmente estrogenos.
AU2001271781A1 (en) 2000-07-06 2002-01-21 Wyeth Use of substituted indole compounds for treating sphincter incontinence
WO2002003991A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for increasing nitric oxide synthase activity
US6358991B2 (en) 2000-07-06 2002-03-19 American Home Products Corporation Methods of treating neuropeptide Y-related conditions
BR0112364A (pt) 2000-07-06 2003-07-29 Wyeth Corp Combinações de bisfosfonatos, agentes estrogênicos e opcionalmente estrogênios
WO2002003992A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for treating prosthesis-related bone degeneration
WO2002003986A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for treating breast disorders
EP1311293A2 (en) 2000-07-06 2003-05-21 Wyeth Combinations of ssri and estrogenic agents
AR030064A1 (es) 2000-07-06 2003-08-13 Wyeth Corp Metodos para inhibir los efectos uterotroficos de los agentes estrogenicos
EP1177787A3 (en) 2000-07-28 2003-09-10 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating cataracts
CN100448487C (zh) 2000-08-11 2009-01-07 惠氏公司 治疗雌激素受体阳性癌的方法
EP1192945A3 (en) 2000-09-21 2004-03-03 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating osteoarthritis
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
AU781168B2 (en) 2001-01-26 2005-05-12 Pfizer Products Inc. Method of treating certain cancers using an estrogen agonist/antagonist
JP2005538091A (ja) * 2002-07-24 2005-12-15 イーライ・リリー・アンド・カンパニー ジヒドロ−ベンゾ［ｂ，ｅ］オキセピンに基づく選択的エストロゲン受容体調節物質、組成物および方法
EP1664052B1 (en) 2003-08-15 2009-02-18 AstraZeneca AB Fused heterocycles as inhibitors of glutamate racemase (muri)
JP2005129430A (ja) 2003-10-27 2005-05-19 Konica Minolta Holdings Inc 光電変換材料用半導体、光電変換素子及び太陽電池
FR2862646B1 (fr) 2003-11-20 2006-02-24 Merck Sante Sas Nouveaux composes antidiabetiques contenant des derives benzofuranes, benzothiophenes
TW200533668A (en) 2003-12-15 2005-10-16 Theramex 1-n-phenyl-amino-1h-imidazole derivatives and pharmaceutical compositions containing them
US7399767B2 (en) 2005-01-21 2008-07-15 Ortho-Mcneil Pharmaceutical, Inc. Heterocyclic benzo[c]chromene derivatives useful as modulators of the estrogen receptors
NZ556686A (en) 2005-02-14 2010-01-29 Bionomics Ltd Novel tubulin polymerisation inhibitors
CA2640678C (en) 2006-02-03 2015-03-31 Bionomics Limited Substituted benzofurans, benzothiophenes, benzoselenophenes and indoles and their use as tubulin polymerisation inhibitors
US8933130B2 (en) 2006-06-23 2015-01-13 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
EP1947085A1 (en) 2007-01-19 2008-07-23 Laboratorios del Dr. Esteve S.A. Substituted indole sulfonamide compounds, their preparation and use as medicaments
CA2693207A1 (en) 2007-07-25 2009-01-29 F. Hoffmann-La Roche Ag Benzofuran- and benzo[b]thiophene-2-carboxylic acid amide derivatives and use thereof as histamine 3 receptor modulators
WO2010093578A1 (en) 2009-02-10 2010-08-19 Glaxo Group Limited Indolinyl-, benzofuranyl-, and benzothienyl- amides as modulators of chemokine receptors
WO2010127452A1 (en) 2009-05-04 2010-11-11 The Royal Institution For The Advancement Of Learning/Mcgill University 5-oxo-ete receptor antagonist compounds
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
WO2011136828A1 (en) 2010-04-27 2011-11-03 The Johns Hopkins University Immunogenic compositions and methods for treating neoplasia
MX2012014431A (es) 2010-06-10 2013-02-26 Aragon Pharmaceuticals Inc Modulares del receptor de estrogenos y usos de los mismos.
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
JP5844376B2 (ja) 2010-10-06 2016-01-13 ジェイファーマ株式会社 強力な尿酸トランスポーター阻害剤の開発：それらの尿酸排泄効果のために設計された化合物
ES2586908T3 (es) 2010-12-24 2016-10-19 Merck Sharp & Dohme B.V. Derivados de azetidina N-sustituidos
DE102011087987A1 (de) 2011-12-08 2013-06-13 Bayer Intellectual Property Gmbh 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
MX357496B (es) 2011-12-14 2018-07-11 Seragon Pharmaceuticals Inc Moduladores del receptor de estrógenos fluorados y sus usos.
PE20150099A1 (es) 2011-12-16 2015-01-30 Olema Pharmaceuticals Inc Compuestos novedosos de benzopirano, composiciones y usos de los mismos
BR112014017985A8 (pt) 2012-01-31 2017-07-11 Novartis Ag Combinação de um inibidor de rtk com um antiestrogênio e uso da mesma para o tratamento de cancer
EA201491530A1 (ru) 2012-03-20 2015-07-30 Серагон Фармасьютикалс, Инк. Модуляторы рецепторов эстрогенов и их применение
EP2871891B1 (en) 2012-08-01 2017-03-29 Huawei Technologies Co., Ltd. Synchronization method, apparatus, and system
US20150203285A1 (en) 2012-09-05 2015-07-23 Kjoninklijke Philips N.V. Capsule for the preparation of beverages, device and method
CA2928173C (en) 2012-10-24 2021-10-19 The Board Of Trustees Of The University Of Illinois Compositions comprising benzothiophene derivatives and use thereof for treatment of estrogen-related medical disorders
RU2015138964A (ru) 2013-03-14 2017-04-18 Серагон Фармасьютикалз, Инк. Полициклические модуляторы рецептора эстрогена и их применения
TN2015000516A1 (en) 2013-05-28 2017-04-06 Astrazeneca Ab Chemical compounds
EA031077B1 (ru) 2013-06-19 2018-11-30 Серагон Фармасьютикалз, Инк. Модулятор рецептора эстрогена и его применения
WO2014203129A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Combinations of benzopyran compounds, compositions and uses thereof
CA2915534A1 (en) 2013-06-19 2014-12-24 Seragon Pharmaceuticals, Inc. Azetidine estrogen receptor modulators and uses thereof
WO2014203132A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Substituted benzopyran compounds, compositions and uses thereof
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
WO2015028409A1 (de) 2013-08-27 2015-03-05 Bayer 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
WO2015092634A1 (en) 2013-12-16 2015-06-25 Novartis Ag 1,2,3,4-tetrahydroisoquinoline compounds and compositions as selective estrogen receptor antagonists and degraders
WO2015136017A1 (en) 2014-03-13 2015-09-17 F. Hoffmann-La Roche Ag Methods and compositions for modulating estrogen receptor mutants
EP3116497A2 (en) 2014-03-13 2017-01-18 F. Hoffmann-La Roche AG Therapeutic combinations with estrogen receptor modulators
PT3122426T (pt) 2014-03-28 2023-02-28 Univ Duke Tratamento de cancro da mama utilizando moduladores seletivos do recetor de estrogénio
US20160175284A1 (en) 2014-12-18 2016-06-23 Genentech, Inc. Estrogen receptor modulators and uses thereof
US9845291B2 (en) 2014-12-18 2017-12-19 Genentech, Inc. Estrogen receptor modulators and uses thereof
NZ769496A (en) 2014-12-18 2023-09-29 Hoffmann La Roche Tetrahydro-pyrido[3,4-b]indole estrogen receptor modulators and uses thereof
WO2016174551A1 (en) 2015-04-27 2016-11-03 Pfizer Inc. Anti-estrogenic compounds
US10053451B2 (en) 2015-05-26 2018-08-21 Genentech, Inc. Heterocyclic estrogen receptor modulators and uses thereof
US10087191B2 (en) 2015-06-16 2018-10-02 Jiangsu Hengrui Medicine Co., Ltd. Piperidine derivative and preparation method and pharmaceutical use thereof
IL310489A (en) 2015-10-01 2024-03-01 Olema Pharmaceuticals Inc TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS AND COMPOSITIONS COMPRISING SAME FOR USE IN TREATING CANCER
WO2017056115A1 (en) 2015-10-03 2017-04-06 Sun Pharma Advanced Research Company Limited Novel n-aryl containing fused heterocyclic compounds
WO2017060326A1 (en) 2015-10-07 2017-04-13 F. Hoffmann-La Roche Ag Process for the preparation of (e)-3-(4-((e)-2-(2-chloro-4-fluorophenyl)-1-(1h-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid
DK3368519T3 (da) 2015-10-27 2022-05-23 Sun Pharma Advanced Res Co Ltd Hidtil ukendte, heterocykliske antiøstrogener
EP3374356A1 (en) 2015-11-09 2018-09-19 H. Hoffnabb-La Roche Ag Tetrahydronaphthalene estrogen receptor modulators and uses thereof
US10519148B2 (en) 2015-11-12 2019-12-31 Zhejiang Hisun Pharmaceutical Co., Ltd. Acrylic acid derivative, preparation method and use in medicine thereof
HRP20221462T1 (hr) 2015-12-09 2023-01-20 The Board Of Trustees Of The University Of Illinois Selektivni nishodni regulatori receptora estrogena na bazi benzotiofena
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014066695A1 (en) * 2012-10-24 2014-05-01 The Board Of Trustees Of The University Of Illinois Compositions and methods for treating estrogen-related medical disorders
WO2014130310A1 (en) * 2013-02-19 2014-08-28 Novartis Ag Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders

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