CN116744925A - 用四氢萘衍生物作为雌激素受体降解剂治疗乳腺癌的方法 - Google Patents

用四氢萘衍生物作为雌激素受体降解剂治疗乳腺癌的方法 Download PDF

Info

Publication number
CN116744925A
CN116744925A CN202180092119.4A CN202180092119A CN116744925A CN 116744925 A CN116744925 A CN 116744925A CN 202180092119 A CN202180092119 A CN 202180092119A CN 116744925 A CN116744925 A CN 116744925A
Authority
CN
China
Prior art keywords
compound
formula
inhibitors
breast cancer
subject
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
CN202180092119.4A
Other languages
English (en)
Chinese (zh)
Inventor
陈昕
A·P·克鲁
J·弗拉纳根
S·M·高夫
R·J·哈斯克尔三世
M·D·穆尔
钱义民
I·C·A·泰勒
王警
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.)
Arvinas Inc
Original Assignee
Arvinas Inc
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 Arvinas Inc filed Critical Arvinas Inc
Publication of CN116744925A publication Critical patent/CN116744925A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • 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)
CN202180092119.4A 2020-12-14 2021-12-13 用四氢萘衍生物作为雌激素受体降解剂治疗乳腺癌的方法 Pending CN116744925A (zh)

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 (1)

Publication Number Publication Date
CN116744925A true CN116744925A (zh) 2023-09-12

Family

ID=79288002

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180092119.4A Pending CN116744925A (zh) 2020-12-14 2021-12-13 用四氢萘衍生物作为雌激素受体降解剂治疗乳腺癌的方法

Country Status (11)

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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2026007884A1 (zh) * 2024-07-04 2026-01-08 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

Families Citing this family (10)

* 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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108024540A (zh) * 2015-04-29 2018-05-11 雷迪厄斯制药公司 用于治疗癌症的方法
WO2018102725A1 (en) * 2016-12-01 2018-06-07 Arvinas, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
WO2020118213A1 (en) * 2018-12-06 2020-06-11 Radius Pharmaceuticals, Inc. Methods for treating cancer resistant to cdk4/6 inhibitors
WO2021041348A1 (en) * 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
CA3095912A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108024540A (zh) * 2015-04-29 2018-05-11 雷迪厄斯制药公司 用于治疗癌症的方法
WO2018102725A1 (en) * 2016-12-01 2018-06-07 Arvinas, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
WO2020118213A1 (en) * 2018-12-06 2020-06-11 Radius Pharmaceuticals, Inc. Methods for treating cancer resistant to cdk4/6 inhibitors
WO2021041348A1 (en) * 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
HITISHA K. PATEL 等: "Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors", BREAST CANCER RESEARCH, vol. 21, no. 146, 31 December 2019 (2019-12-31), pages 1 - 17 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2026007884A1 (zh) * 2024-07-04 2026-01-08 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

Also Published As

Publication number Publication date
CA3202592A1 (en) 2022-06-23
EP4259137A1 (en) 2023-10-18
WO2022132652A1 (en) 2022-06-23
JP2024501471A (ja) 2024-01-12
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

Similar Documents

Publication Publication Date Title
CN114667147B (zh) 用四氢萘衍生物作为雌激素受体降解剂的治疗乳腺癌的方法
CN116744925A (zh) 用四氢萘衍生物作为雌激素受体降解剂治疗乳腺癌的方法
US20240066032A1 (en) Methods of treating prostate cancer
CN107406424B (zh) 雌激素受体调节剂及其用途
CN115135313A (zh) 治疗前列腺癌的方法
JP2001302547A (ja) 女性の性機能不全を処置するための組成物および方法
EP2694073B1 (en) Combinations of akt and mek inhibitors for treating cancer
US20210353621A1 (en) Methods of treating prostate cancer
CN116761607A (zh) 治疗前列腺癌的方法
EP3953342B1 (en) Improved inhibitors of the notch transcriptional activation complex and methods for use of the same
HK40119356A (zh) 用四氢萘衍生物作为雌激素受体降解剂的治疗乳腺癌的方法
TW202540098A (zh) Ｃｄｋ抑制劑的鹽型及固態型
HK1247199B (zh) 雌激素受体调节剂及其用途

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination