AU2016366680B2 - Benzothiophene-based selective estrogen receptor downregulators - Google Patents

Benzothiophene-based selective estrogen receptor downregulators Download PDF

Info

Publication number
AU2016366680B2
AU2016366680B2 AU2016366680A AU2016366680A AU2016366680B2 AU 2016366680 B2 AU2016366680 B2 AU 2016366680B2 AU 2016366680 A AU2016366680 A AU 2016366680A AU 2016366680 A AU2016366680 A AU 2016366680A AU 2016366680 B2 AU2016366680 B2 AU 2016366680B2
Authority
AU
Australia
Prior art keywords
hooc
compound
cancer
alkyl
pharmaceutically acceptable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
AU2016366680A
Other languages
English (en)
Other versions
AU2016366680A1 (en
Inventor
Gregory R. Thatcher
Debra A. Tonetti
Rui XIONG
Jiong ZHAO
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Illinois System
Original Assignee
University of Illinois at Urbana Champaign
University of Illinois System
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 University of Illinois at Urbana Champaign, University of Illinois System filed Critical University of Illinois at Urbana Champaign
Publication of AU2016366680A1 publication Critical patent/AU2016366680A1/en
Application granted granted Critical
Publication of AU2016366680B2 publication Critical patent/AU2016366680B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2016366680A 2015-12-09 2016-12-09 Benzothiophene-based selective estrogen receptor downregulators Active AU2016366680B2 (en)

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
AU2016366680A1 AU2016366680A1 (en) 2018-07-12
AU2016366680B2 true AU2016366680B2 (en) 2021-06-24

Family

ID=59013340

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2016366680A Active AU2016366680B2 (en) 2015-12-09 2016-12-09 Benzothiophene-based selective estrogen receptor downregulators

Country Status (26)

Country Link
US (7) US20170166551A1 (OSRAM)
EP (2) EP3386500B1 (OSRAM)
JP (2) JP6920709B2 (OSRAM)
KR (1) KR102785173B1 (OSRAM)
CN (2) CN108699024B (OSRAM)
AU (1) AU2016366680B2 (OSRAM)
BR (1) BR112018011607B1 (OSRAM)
CA (1) CA3008020C (OSRAM)
CY (1) CY1125767T1 (OSRAM)
DK (1) DK3386500T3 (OSRAM)
EA (1) EA038180B1 (OSRAM)
ES (1) ES2935125T3 (OSRAM)
HR (1) HRP20221462T1 (OSRAM)
HU (1) HUE061065T2 (OSRAM)
IL (1) IL259566B (OSRAM)
LT (1) LT3386500T (OSRAM)
MX (2) MX393926B (OSRAM)
NZ (1) NZ743651A (OSRAM)
PL (1) PL3386500T3 (OSRAM)
PT (1) PT3386500T (OSRAM)
RS (1) RS63791B1 (OSRAM)
RU (1) RU2747802C2 (OSRAM)
SI (1) SI3386500T1 (OSRAM)
SM (1) SMT202300018T1 (OSRAM)
WO (2) WO2017100715A1 (OSRAM)
ZA (2) ZA201803422B (OSRAM)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2935125T3 (es) 2015-12-09 2023-03-01 Univ Illinois Reguladores a la baja selectivos de los receptores de estrógenos con base en benzotiofeno
US10599150B2 (en) 2016-09-29 2020-03-24 The Charles Stark Kraper Laboratory, Inc. Autonomous vehicle: object-level fusion
AR110728A1 (es) * 2017-01-06 2019-04-24 G1 Therapeutics Inc Terapia combinada para el tratamiento del cáncer
TW201835064A (zh) 2017-02-10 2018-10-01 美商G1治療公司 苯并噻吩雌激素受體調節劑
CA3067873A1 (en) 2017-06-29 2019-01-03 G1 Therapeutics, Inc. Morphic forms of g1t38 and methods of manufacture thereof
WO2019157020A1 (en) 2018-02-06 2019-08-15 The Board Of Trustees Of The University Of Illinois Substituted benzothiophene analogs as selective estrogen receptor degraders
CN112839646A (zh) * 2018-08-16 2021-05-25 G1治疗公司 用于治疗医学疾病的苯并噻吩雌激素受体调节剂
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
AU2020268762A1 (en) * 2019-05-09 2021-12-02 Sanofi 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid for use in metastatic or advanced breast cancer patients
US20220233534A1 (en) * 2019-07-08 2022-07-28 Dermavant Sciences GmbH Cerdulatinib-containing topical skin pharmaceutical compositions and uses thereof
CA3173678A1 (en) 2020-05-19 2021-11-25 Jay Copeland Strum 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
AU2025206255A1 (en) * 2024-01-05 2026-05-14 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
EP0545478A1 (en) 1991-12-03 1993-06-09 MERCK SHARP & DOHME LTD. Heterocyclic compounds as tachykinin antagonists
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
US5834468A (en) 1995-07-07 1998-11-10 Zeneca Limited Substituted aryl and heteroaryl compounds as E-type prostaglandin antagonists
US6458811B1 (en) 1996-03-26 2002-10-01 Eli Lilly And Company Benzothiophenes formulations containing same and methods
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
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
US5998402A (en) 1996-04-19 1999-12-07 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
HUP0002852A3 (en) * 1997-08-15 2001-11-28 Univ Durham A method of preventing or treating estrogen-dependent diseases and disorders using triphenil-ethylene derivatives
ATE263164T1 (de) 1997-10-03 2004-04-15 Lilly Co Eli Bentzothiophene
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
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
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
WO2002003976A2 (en) 2000-07-06 2002-01-17 Wyeth Combinations of bisphosphonates, estrogenic agents and optionally estrogens
CN1635885A (zh) 2000-07-06 2005-07-06 惠氏公司 应用取代吲哚化合物增强一氧化氮合酶活性
AU2001271781A1 (en) 2000-07-06 2002-01-21 Wyeth Use of substituted indole compounds for treating sphincter incontinence
MXPA03000170A (es) 2000-07-06 2003-05-27 Wyeth Corp Combinaciones de un inhibidor de recaptacion de serotonina selectivo y agentes estrogenicos.
WO2002003986A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for treating breast disorders
BR0112365A (pt) 2000-07-06 2003-05-13 Wyeth Corp Combinações de estatinas, agentes estrogênicos e opcionalmente estrogênios
AR030064A1 (es) 2000-07-06 2003-08-13 Wyeth Corp Metodos para inhibir los efectos uterotroficos de los agentes estrogenicos
WO2002003992A2 (en) 2000-07-06 2002-01-17 Wyeth Use of substituted indole compounds for treating prosthesis-related bone degeneration
US6509332B2 (en) 2000-07-06 2003-01-21 Wyeth Methods of treating excessive intraocular pressure
US6358991B2 (en) 2000-07-06 2002-03-19 American Home Products Corporation Methods of treating neuropeptide Y-related conditions
EP1177787A3 (en) 2000-07-28 2003-09-10 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating cataracts
ES2228932T3 (es) 2000-08-11 2005-04-16 Wyeth Procedimiento de tratamiento del carcinoma positivo de estrogenos.
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
WO2004009603A1 (en) * 2002-07-24 2004-01-29 Eli Lilly And Company Dihydro-dibenzo[b,e]oxepine based selective estrogen receptor modulators, compositions and methods
DE602004019548D1 (de) 2003-08-15 2009-04-02 Astrazeneca Ab Kondensierte heterocyclen als inhibitoren von glutamatracemase (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
WO2005058842A1 (en) 2003-12-15 2005-06-30 Laboratoire Theramex 1-n-phenyl-amino-1h-imidazole derivatives and pharmaceutical compositions containing them
AU2006206446A1 (en) 2005-01-21 2006-07-27 Janssen Pharmaceutica N.V. Novel heterocyclic benzo[c]chromene derivatives useful as modulators of the estrogen receptors
EP1848704A4 (en) 2005-02-14 2011-05-11 Bionomics Ltd Novel tubulin polymerisation inhibitors
PT1984333E (pt) 2006-02-03 2012-07-16 Bionomics Ltd Benzofuranos, benzotiofenos, benzoselenofenos e indóis substituídos e sua utilização como inibidores da polimerização da tubulina
ES2436028T3 (es) 2006-06-23 2013-12-26 Radius Health, Inc. Tratamiento de síntomas vasomotores con moduladores selectivos de receptores de estrógeno
EP1947085A1 (en) 2007-01-19 2008-07-23 Laboratorios del Dr. Esteve S.A. Substituted indole sulfonamide compounds, their preparation and use as medicaments
EP2183237A1 (en) 2007-07-25 2010-05-12 F. Hoffmann-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
EP2427430B1 (en) 2009-05-04 2014-09-10 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
BR112012027745A2 (pt) 2010-04-27 2017-01-10 Univ Johns Hopkins método e composição imunogênica para tratamento de neoplásia
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
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
US9540361B2 (en) 2010-12-24 2017-01-10 Merck Sharp & Dohme B.V. N-substituted azetidine derivatives
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
SG11201403002RA (en) 2011-12-14 2014-07-30 Seragon Pharmaceuticals Inc Fluorinated estrogen receptor modulators and uses thereof
EP2791128A4 (en) 2011-12-16 2015-04-22 Olema Pharmaceuticals Inc NOVEL BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF
KR20140117457A (ko) * 2012-01-31 2014-10-07 노파르티스 아게 Rtk 억제제와 항에스트로겐의 조합물 및 암의 치료를 위한 그의 용도
MX2014011217A (es) 2012-03-20 2015-03-10 Seragon Pharmaceuticals Inc Moduladores del receptor de estrogeno y sus usos.
WO2014019176A1 (zh) 2012-08-01 2014-02-06 华为技术有限公司 用于同步的方法、装置及系统
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
EP2970130A4 (en) 2013-03-14 2016-08-03 Seragon Pharmaceuticals Inc POLYCYCLIC ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
PE20160874A1 (es) 2013-05-28 2016-09-04 Astrazeneca Ab Compuestos quimicos
MX2015016171A (es) 2013-06-19 2016-08-08 Seragon Pharmaceuticals Inc Moduladores del receptor de estrogeno de azetidina y usos de los mismos.
WO2014205138A1 (en) 2013-06-19 2014-12-24 Seragon Pharmaceuticals, Inc. Estrogen receptor modulator and uses thereof
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
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
AU2015228859A1 (en) 2014-03-13 2016-07-07 F. Hoffmann-La Roche Ag Therapeutic combinations with estrogen receptor modulators
US9855270B2 (en) 2014-03-13 2018-01-02 Genentech, Inc. Methods and compositions for modulating estrogen receptor mutants
RS67458B1 (sr) 2014-03-28 2025-12-31 Univ Duke Lečenje kancera dojke pozitivnog na receptor estrogena upotrebom selektivnih modulatora receptora estrogena
CN117865872A (zh) 2014-12-18 2024-04-12 豪夫迈·罗氏有限公司 四氢-吡啶并[3,4-b]吲哚雌激素受体调节剂及其用途
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
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
WO2016174551A1 (en) 2015-04-27 2016-11-03 Pfizer Inc. Anti-estrogenic compounds
EP3303326B1 (en) 2015-05-26 2020-12-16 H. Hoffnabb-La Roche Ag Heterocyclic estrogen receptor modulators and uses thereof
KR20180012853A (ko) 2015-06-16 2018-02-06 지앙수 헨그루이 메디슨 컴퍼니 리미티드 피페리딘 유도체 및 이의 제조 방법 및 약학적 용도
DK3355884T3 (da) 2015-10-01 2021-08-02 Olema Pharmaceuticals Inc Tetrahydro-1h-pyrido[3,4-b]indol-antiøstrogenlægemidler
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
HRP20220640T1 (hr) 2015-10-27 2022-07-08 Sun Pharma Advanced Research Company Limited Novi heterociklični antiestrogeni
CN108349952A (zh) 2015-11-09 2018-07-31 豪夫迈·罗氏有限公司 四氢萘雌激素受体调节剂及其用途
CA3011391C (en) 2015-11-12 2021-02-09 Zhejiang Hisun Pharmaceutical Co., Ltd. Acrylic acid derivative, preparation method and use in medicine thereof
ES2935125T3 (es) 2015-12-09 2023-03-01 Univ Illinois Reguladores a la baja selectivos de los receptores de estrógenos con base en benzotiofeno
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
AR110728A1 (es) 2017-01-06 2019-04-24 G1 Therapeutics Inc Terapia combinada para el tratamiento del cáncer

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

Also Published As

Publication number Publication date
ZA202003023B (en) 2022-12-21
EP3386500A4 (en) 2019-05-22
SMT202300018T1 (it) 2023-03-17
IL259566B (en) 2021-09-30
CN108495628A (zh) 2018-09-04
EP3386500B1 (en) 2022-09-07
EP3386500A1 (en) 2018-10-17
EP3386968B1 (en) 2025-04-02
US12054469B2 (en) 2024-08-06
PT3386500T (pt) 2023-01-06
DK3386500T3 (da) 2022-12-12
IL259566A (en) 2018-07-31
US10807964B2 (en) 2020-10-20
WO2017100715A1 (en) 2017-06-15
LT3386500T (lt) 2022-12-27
US20200079752A1 (en) 2020-03-12
US20170166550A1 (en) 2017-06-15
US20200123126A1 (en) 2020-04-23
BR112018011607B1 (pt) 2024-01-30
EA038180B1 (ru) 2021-07-20
US10118910B2 (en) 2018-11-06
CN108699024A (zh) 2018-10-23
JP2019502675A (ja) 2019-01-31
KR20180088457A (ko) 2018-08-03
MX373946B (es) 2020-07-13
US20210047286A1 (en) 2021-02-18
MX2020006991A (es) 2022-07-14
PL3386500T3 (pl) 2023-03-13
RU2747802C2 (ru) 2021-05-14
US20220194917A1 (en) 2022-06-23
RU2018125046A3 (OSRAM) 2020-02-10
US11072595B2 (en) 2021-07-27
EP3386968A1 (en) 2018-10-17
RU2018125046A (ru) 2020-01-09
JP2021169498A (ja) 2021-10-28
CA3008020A1 (en) 2017-06-15
CN108495628B (zh) 2022-01-11
ES2935125T3 (es) 2023-03-01
CA3008020C (en) 2024-02-20
NZ743651A (en) 2023-07-28
US11447461B2 (en) 2022-09-20
KR102785173B1 (ko) 2025-03-25
AU2016366680A1 (en) 2018-07-12
BR112018011607A2 (pt) 2018-11-27
EP3386968A4 (en) 2019-09-25
US20190055209A1 (en) 2019-02-21
CN108699024B (zh) 2022-03-11
EA201891376A1 (ru) 2019-02-28
ZA201803422B (en) 2020-08-26
JP6920709B2 (ja) 2021-08-18
RS63791B1 (sr) 2022-12-30
US20170166551A1 (en) 2017-06-15
MX393926B (es) 2025-03-24
US10377735B2 (en) 2019-08-13
WO2017100712A1 (en) 2017-06-15
HUE061065T2 (hu) 2023-05-28
HRP20221462T1 (hr) 2023-01-20
MX2018007079A (es) 2018-11-12
SI3386500T1 (sl) 2023-01-31
CY1125767T1 (el) 2026-02-25

Similar Documents

Publication Publication Date Title
US11447461B2 (en) Benzothiophene-based selective estrogen receptor downregulators
AU2018217809A1 (en) Benzothiophene estrogen receptor modulators
WO2020037251A1 (en) Benzothiophene estrogen receptor modulators to treat medical disorders
US10703747B2 (en) Benzothiophene-based selective mixed estrogen receptor downregulators
HK1262188B (en) Benzothiophene-based selective estrogen receptor downregulators
HK1262188A1 (en) Benzothiophene-based selective estrogen receptor downregulators

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)