CN109415388A - 选择性雌激素受体下调剂(serds) - Google Patents

选择性雌激素受体下调剂(serds) Download PDF

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Publication number
CN109415388A
CN109415388A CN201780027863.XA CN201780027863A CN109415388A CN 109415388 A CN109415388 A CN 109415388A CN 201780027863 A CN201780027863 A CN 201780027863A CN 109415388 A CN109415388 A CN 109415388A
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CN
China
Prior art keywords
compound
salt
serd
ome
formula
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.)
Pending
Application number
CN201780027863.XA
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English (en)
Chinese (zh)
Inventor
王光迪
刘佳望
郑时龙
钟秋
郭山春
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.)
Xavier University of Louisiana
Original Assignee
Xavier University of Louisiana
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 Xavier University of Louisiana filed Critical Xavier University of Louisiana
Publication of CN109415388A publication Critical patent/CN109415388A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/30—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings
    • C07C57/42—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings having unsaturation outside the rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/52—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing halogen
    • C07C57/58—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing halogen containing six-membered aromatic rings
    • C07C57/60—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing halogen containing six-membered aromatic rings having unsaturation outside the rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/42—Unsaturated compounds containing hydroxy or O-metal groups
    • C07C59/52—Unsaturated compounds containing hydroxy or O-metal groups a hydroxy or O-metal group being bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/42—Unsaturated compounds containing hydroxy or O-metal groups
    • C07C59/56—Unsaturated compounds containing hydroxy or O-metal groups containing halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • C07C59/66—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings
    • C07C59/68—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CN201780027863.XA 2016-05-06 2017-05-05 选择性雌激素受体下调剂(serds) Pending CN109415388A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662332541P 2016-05-06 2016-05-06
US62/332,541 2016-05-06
PCT/US2017/031297 WO2017192991A1 (en) 2016-05-06 2017-05-05 Selective estrogen receptor down-regulators (serds)

Publications (1)

Publication Number Publication Date
CN109415388A true CN109415388A (zh) 2019-03-01

Family

ID=60203671

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780027863.XA Pending CN109415388A (zh) 2016-05-06 2017-05-05 选择性雌激素受体下调剂(serds)

Country Status (5)

Country Link
US (1) US20190233442A1 (https=)
EP (1) EP3452486A4 (https=)
JP (1) JP7064772B2 (https=)
CN (1) CN109415388A (https=)
WO (1) WO2017192991A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113439086A (zh) * 2019-03-20 2021-09-24 法玛比奥斯股份有限公司 用于制备氟维司群3-硼酸的方法
CN113444134A (zh) * 2021-07-22 2021-09-28 中国药科大学 雌甾-1,3,5(10)-三烯类化合物其制备方法和医药用途
WO2021213358A1 (zh) * 2020-04-21 2021-10-28 江苏先声药业有限公司 含硼化合物及其应用

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10125135B2 (en) 2016-04-20 2018-11-13 Astrazeneca Ab Chemical compounds
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
PT3494116T (pt) 2017-01-30 2020-01-28 Astrazeneca Ab Moduladores de recetores de estrogénio
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
IT202100008066A1 (it) * 2021-03-31 2022-10-01 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI ACIDO B-[(7α,17β)-17-IDROSSI-7-[9-[(4,4,5,5,5-PENTAFLUOROPENTIL)SULFINIL]NONIL]ESTRA-1,3,5(10)-TRIEN-3-IL]-BORONICO E INTERMEDI DEL PROCESSO
IT202100012062A1 (it) * 2021-05-11 2022-11-11 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI ACIDO B-[(7α,17β)-17-IDROSSI-7-[9-[(4,4,5,5,5-PENTAFLUOROPENTIL)SULFINIL]NONIL]ESTRA-1,3,5(10)-TRIEN-3-IL]-BORONICO E INTERMEDI DEL PROCESSO
CH720542B1 (it) * 2021-10-29 2025-09-15 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI ACIDO Beta-[(7alpha,17beta)-17-IDROSSI-7-[9-[(4,4,5,5,5-PENTAFLUOROPENTIL)SULFINIL]NONIL]ESTRA-1,3,5(10)-TRIEN-3-IL]-BORONICO E INTERMEDI DEL PROCESSO

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999020646A1 (en) * 1997-10-23 1999-04-29 American Home Products Corporation Estra-1,3,5(10)-triene-7alpha-thioethers
CN101076538A (zh) * 2004-02-13 2007-11-21 因诺文图斯设计有限公司 用于癌症治疗的类固醇
WO2010107474A1 (en) * 2009-03-16 2010-09-23 The Research Foundation Of State University Of New York Antiestrogens for breast cancer therapy
WO2016004166A1 (en) * 2014-07-02 2016-01-07 Xavier University Of Louisiana Boron-based prodrug strategy for increased bioavailability and lower-dosage requirements for drug molecules containing at least one phenol (or aromatic hydroxyl) group

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999020646A1 (en) * 1997-10-23 1999-04-29 American Home Products Corporation Estra-1,3,5(10)-triene-7alpha-thioethers
CN101076538A (zh) * 2004-02-13 2007-11-21 因诺文图斯设计有限公司 用于癌症治疗的类固醇
WO2010107474A1 (en) * 2009-03-16 2010-09-23 The Research Foundation Of State University Of New York Antiestrogens for breast cancer therapy
WO2016004166A1 (en) * 2014-07-02 2016-01-07 Xavier University Of Louisiana Boron-based prodrug strategy for increased bioavailability and lower-dosage requirements for drug molecules containing at least one phenol (or aromatic hydroxyl) group

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DEGORCE, SEBASTIEN L.ET AL.: "Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators", 《JOURNAL OF MEDICINAL CHEMISTRY》 *
LIU, JIAWANG ET AL.: "Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD)", 《JOURNAL OF MEDICINAL CHEMISTRY》 *
QIU ZHONG ET AL.: "Boronic prodrug of 4-hydroxytamoxifen is more efficacious than tamoxifen with enhanced bioavailability independent of CYP2D6 status", 《BMC CANCER》 *
SUZUKI, NAOMI ET AL.: "Anti-breast cancer potential of SS5020, a novel benzopyran antiestrogen", 《INTERNATIONAL JOURNAL OF CANCER》 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113439086A (zh) * 2019-03-20 2021-09-24 法玛比奥斯股份有限公司 用于制备氟维司群3-硼酸的方法
CN113439086B (zh) * 2019-03-20 2024-03-01 法玛比奥斯股份有限公司 用于制备氟维司群3-硼酸的方法
WO2021213358A1 (zh) * 2020-04-21 2021-10-28 江苏先声药业有限公司 含硼化合物及其应用
CN115667275A (zh) * 2020-04-21 2023-01-31 先声药业有限公司 含硼化合物及其应用
CN115667275B (zh) * 2020-04-21 2024-02-23 南京再明医药有限公司 含硼化合物及其应用
CN113444134A (zh) * 2021-07-22 2021-09-28 中国药科大学 雌甾-1,3,5(10)-三烯类化合物其制备方法和医药用途

Also Published As

Publication number Publication date
JP2019514955A (ja) 2019-06-06
JP7064772B2 (ja) 2022-05-11
EP3452486A4 (en) 2020-03-04
WO2017192991A1 (en) 2017-11-09
EP3452486A1 (en) 2019-03-13
US20190233442A1 (en) 2019-08-01

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Application publication date: 20190301