JP2025524557A - 二官能性化合物、該二官能性化合物を含む医薬組成物、およびこれらを使用したアンドロゲン受容体関連疾患の治療方法 - Google Patents

二官能性化合物、該二官能性化合物を含む医薬組成物、およびこれらを使用したアンドロゲン受容体関連疾患の治療方法

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Publication number
JP2025524557A
JP2025524557A JP2024577399A JP2024577399A JP2025524557A JP 2025524557 A JP2025524557 A JP 2025524557A JP 2024577399 A JP2024577399 A JP 2024577399A JP 2024577399 A JP2024577399 A JP 2024577399A JP 2025524557 A JP2025524557 A JP 2025524557A
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substituted
unsubstituted
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compound
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JP2025524557A5 (https=
Inventor
リン，チュ－チャン
チェン，フン－チュァン
チェン，ペイ－チン
チョウ，チ－チャン
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Anhorn Medicines Co Ltd
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Anhorn Medicines Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/496—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
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
JP2024577399A 2022-06-30 2023-06-29 二官能性化合物、該二官能性化合物を含む医薬組成物、およびこれらを使用したアンドロゲン受容体関連疾患の治療方法 Pending JP2025524557A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202263357054P 2022-06-30 2022-06-30
US63/357,054 2022-06-30
PCT/CN2023/103576 WO2024002206A1 (en) 2022-06-30 2023-06-29 Bifunctional compound and pharmaceutical composition comprising the bifunctional compound, and method for treating androgen receptor related diseases by using the same

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JP2025524557A true JP2025524557A (ja) 2025-07-30
JP2025524557A5 JP2025524557A5 (https=) 2025-12-16

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JP2024577399A Pending JP2025524557A (ja) 2022-06-30 2023-06-29 二官能性化合物、該二官能性化合物を含む医薬組成物、およびこれらを使用したアンドロゲン受容体関連疾患の治療方法
JP2024577397A Pending JP2025520909A (ja) 2022-06-30 2023-06-29 二官能性化合物、該二官能性化合物を含む医薬組成物、およびこれらを使用したアンドロゲン受容体関連疾患の治療方法

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Country Link
US (3) US20250197409A1 (https=)
EP (2) EP4547667A1 (https=)
JP (2) JP2025524557A (https=)
KR (2) KR20250027728A (https=)
CN (2) CN119487035A (https=)
AU (2) AU2023300784A1 (https=)
CA (2) CA3259653A1 (https=)
IL (1) IL318001A (https=)
MX (2) MX2024015832A (https=)
TW (2) TWI893405B (https=)
WO (3) WO2024002289A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118955474A (zh) * 2024-07-29 2024-11-15 浙江爱索拓标记医药科技有限公司 一种放射性同位素碳-14标记的巴德卡鲁胺及其制备方法和应用

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JP2020506922A (ja) * 2017-01-31 2020-03-05 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． セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物
JP2021521192A (ja) * 2018-04-13 2021-08-26 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． セレブロンリガンドおよび同リガンドを含む二機能性化合物
WO2021231927A1 (en) * 2020-05-14 2021-11-18 The Regents Of The University Of Michigan Androgen receptor protein degraders with a tricyclic cereblon ligand
CN114163444A (zh) * 2020-09-11 2022-03-11 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
JP2022529339A (ja) * 2019-04-18 2022-06-21 ヒノバ ファーマシューティカルズ インコーポレイテッド アンドロゲン受容体を標的に分解する二官能性キメラ複素環式化合物及びその使用

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RU2738833C9 (ru) * 2014-04-14 2022-02-28 Арвинас, Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения
CA2988414C (en) * 2015-06-04 2023-09-26 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
CN110506039A (zh) * 2016-10-11 2019-11-26 阿尔维纳斯股份有限公司 用于雄激素受体靶向降解的化合物和方法
EP3658548A1 (en) * 2017-07-28 2020-06-03 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
CN114829342A (zh) * 2019-12-23 2022-07-29 上海济煜医药科技有限公司 一种蛋白降解剂化合物的制备方法和应用
WO2021143816A1 (zh) * 2020-01-16 2021-07-22 江苏恒瑞医药股份有限公司 稠合酰亚胺类衍生物、其制备方法及其在医药上的应用
WO2022011205A1 (en) * 2020-07-10 2022-01-13 The Regents Of The University Of Michigan Androgen receptor protein degraders
KR20220014952A (ko) * 2020-07-29 2022-02-08 한국화학연구원 안드로겐 수용체의 저해 또는 분해용 화합물 및 이들의 의약 용도
JP2023547084A (ja) * 2020-10-21 2023-11-09 アルビナス・オペレーションズ・インコーポレイテッド アンドロゲン受容体タンパク質の標的分解のための化合物および方法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020506922A (ja) * 2017-01-31 2020-03-05 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． セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物
JP2021521192A (ja) * 2018-04-13 2021-08-26 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． セレブロンリガンドおよび同リガンドを含む二機能性化合物
JP2022529339A (ja) * 2019-04-18 2022-06-21 ヒノバ ファーマシューティカルズ インコーポレイテッド アンドロゲン受容体を標的に分解する二官能性キメラ複素環式化合物及びその使用
WO2021231927A1 (en) * 2020-05-14 2021-11-18 The Regents Of The University Of Michigan Androgen receptor protein degraders with a tricyclic cereblon ligand
CN114163444A (zh) * 2020-09-11 2022-03-11 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用

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CN119487035A (zh) 2025-02-18
AU2023296682A1 (en) 2025-01-02
IL318001A (en) 2025-02-01
EP4547668A1 (en) 2025-05-07
MX2024015833A (es) 2025-04-02
TWI893404B (zh) 2025-08-11
US20240018149A1 (en) 2024-01-18
EP4547667A1 (en) 2025-05-07
KR20250028370A (ko) 2025-02-28
CA3259653A1 (en) 2024-01-04
TW202404976A (zh) 2024-02-01
US20240336620A1 (en) 2024-10-10
WO2024002205A1 (en) 2024-01-04
JP2025520909A (ja) 2025-07-03
WO2024002206A1 (en) 2024-01-04
TWI893405B (zh) 2025-08-11
US20250197409A1 (en) 2025-06-19
MX2024015832A (es) 2025-04-02
CN119487034A (zh) 2025-02-18
TW202408505A (zh) 2024-03-01
WO2024002289A1 (en) 2024-01-04
AU2023300784A1 (en) 2025-01-02
KR20250027728A (ko) 2025-02-27
CA3259652A1 (en) 2024-01-04

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