JP2024501471A - エストロゲン受容体分解剤としてのテトラヒドロナフタレン誘導体を用いる乳がんを治療する方法 - Google Patents

エストロゲン受容体分解剤としてのテトラヒドロナフタレン誘導体を用いる乳がんを治療する方法 Download PDF

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JP2024501471A
JP2024501471A JP2023535799A JP2023535799A JP2024501471A JP 2024501471 A JP2024501471 A JP 2024501471A JP 2023535799 A JP2023535799 A JP 2023535799A JP 2023535799 A JP2023535799 A JP 2023535799A JP 2024501471 A JP2024501471 A JP 2024501471A
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compound
formula
inhibitor
breast cancer
subject
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JP2024501471A5 (https=
JPWO2022132652A5 (https=
Inventor
チェン，シン
ピー． クルー，アンドリュー
フラナガン，ジョン
マキシン ゴフ，シェリル
サード，ロイヤル ジェイ． ハスケル，ザ
ドゥーガン ムーア，マルシア
キアン，イミン
チャールズ アンソニー テイラー，イアン
ワン，ジン
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Arvinas Operations Inc
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Arvinas Operations Inc
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Publication of JPWO2022132652A5 publication Critical patent/JPWO2022132652A5/ja
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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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61K31/395—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
    • A61K31/403—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
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods

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  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2023535799A 2020-12-14 2021-12-13 エストロゲン受容体分解剤としてのテトラヒドロナフタレン誘導体を用いる乳がんを治療する方法 Pending JP2024501471A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063125371P 2020-12-14 2020-12-14
US63/125,371 2020-12-14
PCT/US2021/063130 WO2022132652A1 (en) 2020-12-14 2021-12-13 Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders

Publications (3)

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JP2024501471A true JP2024501471A (ja) 2024-01-12
JP2024501471A5 JP2024501471A5 (https=) 2024-12-23
JPWO2022132652A5 JPWO2022132652A5 (https=) 2024-12-23

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JP2023535799A Pending JP2024501471A (ja) 2020-12-14 2021-12-13 エストロゲン受容体分解剤としてのテトラヒドロナフタレン誘導体を用いる乳がんを治療する方法

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Country Link
US (1) US20220193072A1 (https=)
EP (1) EP4259137A1 (https=)
JP (1) JP2024501471A (https=)
KR (1) KR20230121801A (https=)
CN (1) CN116744925A (https=)
AU (1) AU2021401580A1 (https=)
CA (1) CA3202592A1 (https=)
IL (1) IL303143A (https=)
MX (1) MX2023007058A (https=)
TW (1) TW202237117A (https=)
WO (1) WO2022132652A1 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102674902B1 (ko) 2016-12-01 2024-06-14 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
IL320609A (en) 2019-08-26 2025-07-01 Arvinas Operations Inc Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents
CN115746058A (zh) * 2021-09-03 2023-03-07 南京知和医药科技有限公司 一种多环化合物在制备抗肿瘤药物方面的用途
KR20250047743A (ko) * 2022-07-12 2025-04-04 리젠츠 오브 더 유니버시티 오브 미시간 에스트로겐 수용체 분해제로서의 테트라하이드로나프탈렌 유도체
WO2024049926A1 (en) * 2022-08-31 2024-03-07 Arvinas Operations, Inc. Dosage regimens of estrogen receptor degraders
WO2024196053A1 (ko) * 2023-03-17 2024-09-26 재단법인 대구경북첨단의료산업진흥재단 에스트로겐-연관 수용체 감마 억제제 및 항암제의 병용요법용 조성물
TW202440096A (zh) * 2023-03-24 2024-10-16 美商亞文納營運公司 雌激素受體降解劑之給藥方案
CN121368483A (zh) * 2023-06-02 2026-01-20 辉瑞公司 雌激素受体降解剂与cdk4抑制剂的组合
EP4719399A1 (en) * 2023-06-02 2026-04-08 Arvinas Operations, Inc. Combinations of estrogen receptor degraders and akt inhibitors
WO2025122502A1 (en) * 2023-12-04 2025-06-12 Foundation Medicine, Inc. Methods for treating hr-positive her2-negative breast cancer
CN121646481A (zh) * 2024-07-04 2026-03-10 海创药业股份有限公司 一种雌激素受体降解剂和akt抑制剂联合用药物及其用途

Citations (5)

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Publication number Priority date Publication date Assignee Title
JP2017507964A (ja) * 2014-03-13 2017-03-23 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト エストロゲン受容体モジュレーターを用いた治療的組合せ
JP2018518529A (ja) * 2015-04-29 2018-07-12 ラジウス ファーマシューティカルズ，インコーポレイテッド 癌を治療するための方法
WO2019199816A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
JP2020504089A (ja) * 2016-12-01 2020-02-06 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． エストロゲン受容体分解物質としてのテトラヒドロナフタレン誘導体およびテトラヒドロイソキノリン誘導体
WO2020118213A1 (en) * 2018-12-06 2020-06-11 Radius Pharmaceuticals, Inc. Methods for treating cancer resistant to cdk4/6 inhibitors

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US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
IL320609A (en) * 2019-08-26 2025-07-01 Arvinas Operations Inc Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents

Patent Citations (5)

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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
JP2018518529A (ja) * 2015-04-29 2018-07-12 ラジウス ファーマシューティカルズ，インコーポレイテッド 癌を治療するための方法
JP2020504089A (ja) * 2016-12-01 2020-02-06 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． エストロゲン受容体分解物質としてのテトラヒドロナフタレン誘導体およびテトラヒドロイソキノリン誘導体
WO2019199816A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2020118213A1 (en) * 2018-12-06 2020-06-11 Radius Pharmaceuticals, Inc. Methods for treating cancer resistant to cdk4/6 inhibitors

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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. Vol.206, No.15, Article No.112689, JPN6025046594, 2 August 2020 (2020-08-02), pages 1 - 19, ISSN: 0005733116 *
MOLECULAR CANCER THERAPEUTICS, vol. 19, JPN6025046593, 8 May 2020 (2020-05-08), pages 1395 - 1405, ISSN: 0005733117 *

Also Published As

Publication number Publication date
CA3202592A1 (en) 2022-06-23
EP4259137A1 (en) 2023-10-18
WO2022132652A1 (en) 2022-06-23
CN116744925A (zh) 2023-09-12
MX2023007058A (es) 2023-06-23
US20220193072A1 (en) 2022-06-23
AU2021401580A1 (en) 2023-06-22
IL303143A (en) 2023-07-01
TW202237117A (zh) 2022-10-01
KR20230121801A (ko) 2023-08-21

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