JP7555938B2 - アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法 - Google Patents

アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法 Download PDF

Info

Publication number
JP7555938B2
JP7555938B2 JP2021544763A JP2021544763A JP7555938B2 JP 7555938 B2 JP7555938 B2 JP 7555938B2 JP 2021544763 A JP2021544763 A JP 2021544763A JP 2021544763 A JP2021544763 A JP 2021544763A JP 7555938 B2 JP7555938 B2 JP 7555938B2
Authority
JP
Japan
Prior art keywords
alkyl
halo
optionally substituted
mmol
morpholinothiazol
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
JP2021544763A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022523916A (ja
JP2022523916A5 (https=
JPWO2020160295A5 (https=
Inventor
デサンティス，ジェニー
ジョセフ バズ，ロイ
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.)
Montelino Therapeutics Inc
Original Assignee
Montelino Therapeutics 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 Montelino Therapeutics Inc filed Critical Montelino Therapeutics Inc
Publication of JP2022523916A publication Critical patent/JP2022523916A/ja
Publication of JP2022523916A5 publication Critical patent/JP2022523916A5/ja
Publication of JPWO2020160295A5 publication Critical patent/JPWO2020160295A5/ja
Application granted granted Critical
Publication of JP7555938B2 publication Critical patent/JP7555938B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2021544763A 2019-01-30 2020-01-30 アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法 Active JP7555938B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962798554P 2019-01-30 2019-01-30
US62/798,554 2019-01-30
PCT/US2020/015922 WO2020160295A1 (en) 2019-01-30 2020-01-30 Bi-functional compounds and methods for targeted ubiquitination of androgen receptor

Publications (4)

Publication Number Publication Date
JP2022523916A JP2022523916A (ja) 2022-04-27
JP2022523916A5 JP2022523916A5 (https=) 2023-02-06
JPWO2020160295A5 JPWO2020160295A5 (https=) 2023-02-06
JP7555938B2 true JP7555938B2 (ja) 2024-09-25

Family

ID=71733785

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021544763A Active JP7555938B2 (ja) 2019-01-30 2020-01-30 アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法

Country Status (5)

Country Link
US (3) US11098025B2 (https=)
EP (1) EP3917916A4 (https=)
JP (1) JP7555938B2 (https=)
CN (1) CN113677668B (https=)
WO (1) WO2020160295A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7555938B2 (ja) 2019-01-30 2024-09-25 モンテリノ・セラピューティクス・インコーポレイテッド アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法
CA3165168A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
CN115996918A (zh) 2020-05-09 2023-04-21 阿尔维纳斯运营股份有限公司 制造双官能团化合物的方法、双官能团化合物的超纯形式以及包括所述双官能团化合物的剂型
WO2021236695A1 (en) * 2020-05-18 2021-11-25 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
CN114262319B (zh) * 2020-12-01 2023-05-05 南昌奥瑞药业有限公司 一类双功能分子、其制备方法及其应用
JP2024508841A (ja) * 2021-02-25 2024-02-28 メイヨ・ファウンデーション・フォー・メディカル・エデュケーション・アンド・リサーチ プログラム可能なタンパク質分解のための化合物及び疾患処置のための使用方法
WO2023039601A1 (en) * 2021-09-13 2023-03-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US11981672B2 (en) 2021-09-13 2024-05-14 Montelino Therapeutics Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US20240376118A1 (en) * 2021-09-13 2024-11-14 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2023039603A2 (en) * 2021-09-13 2023-03-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US20240382603A1 (en) * 2021-09-13 2024-11-21 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
EP4426286A4 (en) * 2021-11-03 2025-12-24 Relay Therapeutics Inc Bifunctional PI3K-Alpha Inhibitors and Their Uses
AU2022424178A1 (en) 2021-12-30 2024-07-11 Beone Medicines I Gmbh Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
CN119301111A (zh) 2022-03-24 2025-01-10 葛兰素史密斯克莱知识产权发展有限公司 作为protac中的降解决定子的2,4-二氧代四氢嘧啶基衍生物
CN114890989B (zh) * 2022-05-25 2024-03-22 广东晨康生物科技有限公司 一种含氮衍生物为Linker的HDAC8降解剂其制备方法和应用
US20240207415A1 (en) * 2022-11-08 2024-06-27 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
KR20250047848A (ko) * 2023-09-27 2025-04-07 강원대학교산학협력단 Kras의 g12v 돌연변이체 단백질의 특이적 분해 방법 및 그 조성물
US12496301B2 (en) 2023-12-08 2025-12-16 Arvinas Operations, Inc. Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013056837A (ja) 2011-09-07 2013-03-28 Japan Health Science Foundation アポトーシス阻害タンパク質リガンド−エストロゲン受容体リガンドハイブリッド化合物並びにそれを利用したエストロゲン受容体分解誘導剤及び乳癌、子宮頚癌又は卵巣癌の予防及び治療剤
WO2017011590A1 (en) 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
JP2017505787A (ja) 2014-02-14 2017-02-23 ザ ユニバーシティ オブ ブリティッシュ コロンビア 治療薬としてのヒトアンドロゲン受容体ｄｎａ結合ドメイン（ｄｂｄ）化合物およびそれらを使用する方法
JP2017513862A (ja) 2014-04-14 2017-06-01 アルビナス インコーポレイテッド イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2018502925A (ja) 2015-01-20 2018-02-01 アルビナス インコーポレイテッド ターゲティングされたアンドロゲン受容体分解のための化合物および方法
WO2018071606A1 (en) 2016-10-11 2018-04-19 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2018114781A1 (en) 2016-12-19 2018-06-28 F. Hoffmann-La Roche Ag Ar-v7 inhibitors
WO2018144649A1 (en) 2017-01-31 2018-08-09 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
JP2018526430A (ja) 2015-07-10 2018-09-13 アルヴィナス・インコーポレイテッド タンパク質分解のｍｄｍ２系修飾因子および関連の使用方法
WO2020010210A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Mertk degraders and uses thereof

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9817224D0 (en) 1998-08-08 1998-10-07 Univ Nottingham Ocular surface infection
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
EP1087334B1 (fr) 1999-09-15 2007-12-19 European Community Scellé multi-usage électronique à transpondeur passif
CN102186836A (zh) 2008-10-17 2011-09-14 雅培制药有限公司 Trpv1拮抗剂
EP2519664A4 (en) 2009-12-30 2014-03-12 Avila Therapeutics Inc LIGAND-RELATED COVALENTS MODIFYING A PROTEIN
WO2011098904A1 (en) 2010-02-12 2011-08-18 Aegera Therapeutics, Inc. Iap bir domain binding compounds
CA2861066C (en) 2012-01-12 2024-01-02 Yale University Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase
US20150284422A1 (en) 2012-08-10 2015-10-08 Epizyme, Inc. Inhibitors of protein methyltransferase dot1l and methods of use thereof
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
JP6815318B2 (ja) 2014-12-23 2021-01-20 ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド 二官能性分子によって標的化タンパク質分解を誘導する方法
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
AU2017246452C1 (en) 2016-04-06 2021-06-03 The Regents Of The University Of Michigan MDM2 protein degraders
WO2017197056A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting degronimers for target protein degradation
US20200172927A1 (en) 2017-05-15 2020-06-04 The Trustees Of Columbia University In The City Of New York Reprogramming metabolism by inhibiting vhl for treatment of neurodegeneration
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
KR102596354B1 (ko) 2018-11-05 2023-10-31 삼성디스플레이 주식회사 액정 표시 장치 및 그 제조 방법
WO2020102575A1 (en) 2018-11-16 2020-05-22 Inception Ibd, Inc. Heterocyclic aminothiazoles and uses thereof
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
JP7555938B2 (ja) 2019-01-30 2024-09-25 モンテリノ・セラピューティクス・インコーポレイテッド アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法
JP2022549222A (ja) 2019-09-23 2022-11-24 アキュター バイオテクノロジー インコーポレイテッド アンドロゲン受容体分解活性を有する新規尿素およびその使用
US11820781B2 (en) 2019-12-04 2023-11-21 Nurix Therapeutics, Inc. Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway
WO2021236695A1 (en) 2020-05-18 2021-11-25 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013056837A (ja) 2011-09-07 2013-03-28 Japan Health Science Foundation アポトーシス阻害タンパク質リガンド−エストロゲン受容体リガンドハイブリッド化合物並びにそれを利用したエストロゲン受容体分解誘導剤及び乳癌、子宮頚癌又は卵巣癌の予防及び治療剤
JP2017505787A (ja) 2014-02-14 2017-02-23 ザ ユニバーシティ オブ ブリティッシュ コロンビア 治療薬としてのヒトアンドロゲン受容体ｄｎａ結合ドメイン（ｄｂｄ）化合物およびそれらを使用する方法
JP2017513862A (ja) 2014-04-14 2017-06-01 アルビナス インコーポレイテッド イミド系タンパク質分解モジュレーター及び関連する使用方法
JP2018502925A (ja) 2015-01-20 2018-02-01 アルビナス インコーポレイテッド ターゲティングされたアンドロゲン受容体分解のための化合物および方法
JP2018526430A (ja) 2015-07-10 2018-09-13 アルヴィナス・インコーポレイテッド タンパク質分解のｍｄｍ２系修飾因子および関連の使用方法
WO2017011590A1 (en) 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
WO2018071606A1 (en) 2016-10-11 2018-04-19 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2018114781A1 (en) 2016-12-19 2018-06-28 F. Hoffmann-La Roche Ag Ar-v7 inhibitors
WO2018144649A1 (en) 2017-01-31 2018-08-09 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2020010210A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Mertk degraders and uses thereof

Also Published As

Publication number Publication date
WO2020160295A1 (en) 2020-08-06
EP3917916A1 (en) 2021-12-08
CN113677668A (zh) 2021-11-19
CN113677668B (zh) 2024-09-27
US11098025B2 (en) 2021-08-24
JP2022523916A (ja) 2022-04-27
US11787778B2 (en) 2023-10-17
US20210292298A1 (en) 2021-09-23
US20200239430A1 (en) 2020-07-30
EP3917916A4 (en) 2022-12-14
US20240002360A1 (en) 2024-01-04

Similar Documents

Publication Publication Date Title
JP7555938B2 (ja) アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法
US20250223265A1 (en) Compounds and methods for the targeted degradation of androgen receptor
US20240059686A1 (en) Compounds and methods for the targeted degradation of the androgen receptor
US11547759B2 (en) Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
BR112020001825A2 (pt) compostos e métodos para a degradação direcionada de receptor de androgênio
US20230132823A1 (en) Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
JP2023541522A (ja) 低分子量タンパク質分解物質及びその適用
TW202317521A (zh) 化合物
EP4648777A1 (en) Modulators of bcl6 proteolysis and associated methods of use
WO2023039601A1 (en) Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
HK40062040A (en) Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
RU2774863C2 (ru) Соединения и способы для таргетной деградации андрогенового рецептора
AU2023262617A1 (en) Prep binding ligands

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230127

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20230127

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240116

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20240415

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240614

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20240813

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20240911

R150 Certificate of patent or registration of utility model

Ref document number: 7555938

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150