JP7472026B2 - 選択的なタンパク質分解を誘導するための低分子およびその使用法 - Google Patents

選択的なタンパク質分解を誘導するための低分子およびその使用法 Download PDF

Info

Publication number
JP7472026B2
JP7472026B2 JP2020544488A JP2020544488A JP7472026B2 JP 7472026 B2 JP7472026 B2 JP 7472026B2 JP 2020544488 A JP2020544488 A JP 2020544488A JP 2020544488 A JP2020544488 A JP 2020544488A JP 7472026 B2 JP7472026 B2 JP 7472026B2
Authority
JP
Japan
Prior art keywords
optionally substituted
alkyl
heteroaryl
certain embodiments
aryl
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
JP2020544488A
Other languages
English (en)
Japanese (ja)
Other versions
JP2021514958A5 (https=
JP2021514958A (ja
Inventor
ジュン チー
レイ ウー
ヤン ソン
ポール パーク
ケネス シー. アンダーソン
ダーミンダー チャウハン
Original Assignee
デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド
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 デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド filed Critical デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド
Publication of JP2021514958A publication Critical patent/JP2021514958A/ja
Publication of JP2021514958A5 publication Critical patent/JP2021514958A5/ja
Priority to JP2024016079A priority Critical patent/JP7820423B2/ja
Application granted granted Critical
Publication of JP7472026B2 publication Critical patent/JP7472026B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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 three hetero rings
    • C07D495/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020544488A 2018-02-23 2019-02-22 選択的なタンパク質分解を誘導するための低分子およびその使用法 Active JP7472026B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024016079A JP7820423B2 (ja) 2018-02-23 2024-02-06 選択的なタンパク質分解を誘導するための低分子およびその使用法

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862634679P 2018-02-23 2018-02-23
US62/634,679 2018-02-23
PCT/US2019/019180 WO2019165229A1 (en) 2018-02-23 2019-02-22 Small molecules for inducing selective protein degradation and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2024016079A Division JP7820423B2 (ja) 2018-02-23 2024-02-06 選択的なタンパク質分解を誘導するための低分子およびその使用法

Publications (3)

Publication Number Publication Date
JP2021514958A JP2021514958A (ja) 2021-06-17
JP2021514958A5 JP2021514958A5 (https=) 2023-07-24
JP7472026B2 true JP7472026B2 (ja) 2024-04-22

Family

ID=67687887

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2020544488A Active JP7472026B2 (ja) 2018-02-23 2019-02-22 選択的なタンパク質分解を誘導するための低分子およびその使用法
JP2024016079A Active JP7820423B2 (ja) 2018-02-23 2024-02-06 選択的なタンパク質分解を誘導するための低分子およびその使用法

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2024016079A Active JP7820423B2 (ja) 2018-02-23 2024-02-06 選択的なタンパク質分解を誘導するための低分子およびその使用法

Country Status (7)

Country Link
US (1) US11802132B2 (https=)
EP (1) EP3755325A4 (https=)
JP (2) JP7472026B2 (https=)
CN (1) CN112020358A (https=)
AU (1) AU2019225166B2 (https=)
CA (1) CA3090417A1 (https=)
WO (1) WO2019165229A1 (https=)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102455171B1 (ko) 2013-12-18 2022-10-14 더 스크립스 리서치 인스티튜트 변형된 치료제, 스테이플드 펩티드 지질 접합체, 및 이의 조성물
US10254389B2 (en) 2015-11-06 2019-04-09 Artilux Corporation High-speed light sensing apparatus
US10886309B2 (en) 2015-11-06 2021-01-05 Artilux, Inc. High-speed light sensing apparatus II
US10418407B2 (en) 2015-11-06 2019-09-17 Artilux, Inc. High-speed light sensing apparatus III
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
WO2019060742A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc AGENTS FOR DEGRADING PROTEINS AND USES THEREOF
US11358948B2 (en) 2017-09-22 2022-06-14 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
US11105928B2 (en) 2018-02-23 2021-08-31 Artilux, Inc. Light-sensing apparatus and light-sensing method thereof
US11482553B2 (en) 2018-02-23 2022-10-25 Artilux, Inc. Photo-detecting apparatus with subpixels
EP3773576A4 (en) 2018-03-26 2021-12-29 C4 Therapeutics, Inc. Cereblon binders for the degradation of ikaros
US10886311B2 (en) 2018-04-08 2021-01-05 Artilux, Inc. Photo-detecting apparatus
EP3781156A4 (en) 2018-04-16 2022-05-18 C4 Therapeutics, Inc. SPIROCYCLIC COMPOUNDS
EP3807272A1 (en) 2018-06-13 2021-04-21 Amphista Therapeutics Ltd Bifunctional molecules for targeting rpn11
WO2020010177A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Tricyclic crbn ligands and uses thereof
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11691984B2 (en) 2018-10-12 2023-07-04 The Scripps Research Institute Compounds and methods for DCAF-mediated protein degradation
CA3119773A1 (en) 2018-11-30 2020-06-04 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
EP3917517A4 (en) 2019-01-29 2023-01-25 Foghorn Therapeutics Inc. CONNECTIONS AND USES THEREOF
US12384776B2 (en) 2019-01-29 2025-08-12 Foghorn Therapeutics Inc. Compounds and uses thereof
CN120574283A (zh) 2019-04-05 2025-09-02 凯麦拉医疗公司 Stat降解剂和其用途
WO2020210630A1 (en) 2019-04-12 2020-10-15 C4 Therapeutics, Inc. Tricyclic degraders of ikaros and aiolos
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
MX2022006861A (es) 2019-12-04 2022-07-11 Scripps Research Inst Agonistas del receptor glp2 y metodos de uso.
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
WO2021126973A1 (en) * 2019-12-17 2021-06-24 Orionis Biosciences, Inc. Compounds modulating protein recruitment and/or degradation
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
KR20220119415A (ko) 2019-12-20 2022-08-29 씨4 테라퓨틱스, 인코포레이티드 Egfr 분해를 위한 이소인돌리논 및 인다졸 화합물
EP4081308A4 (en) 2019-12-23 2024-01-24 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
KR20230005160A (ko) 2020-03-19 2023-01-09 카이메라 쎄라퓨틱스 인코포레이티드 Mdm2 분해제 및 이의 용도
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
WO2022120355A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead degraders and uses thereof
EP4259144A4 (en) 2020-12-09 2025-08-20 Kymera Therapeutics Inc SMARCA DEGRADING AGENTS AND THEIR USES
CN116867758A (zh) 2020-12-30 2023-10-10 凯麦拉医疗公司 Irak降解剂和其用途
US12171768B2 (en) 2021-02-15 2024-12-24 Kymera Therapeutics, Inc. IRAK4 degraders and uses thereof
JP2024513566A (ja) * 2021-04-09 2024-03-26 ザ・ブロード・インスティテュート・インコーポレイテッド 標的基質の選択的修飾のための二官能性分子
US20240245787A1 (en) 2021-04-13 2024-07-25 President And Fellows Of Harvard College E3 ligase binders and uses thereof
KR20240020735A (ko) 2021-05-07 2024-02-15 카이메라 쎄라퓨틱스 인코포레이티드 Cdk2 분해제 및 그 용도
KR20240032010A (ko) 2021-06-09 2024-03-08 더 스크립스 리서치 인스티튜트 장기 지속형 이중 gip/glp-1 펩타이드 접합체 및 사용 방법
WO2023283130A1 (en) 2021-07-04 2023-01-12 Newave Pharmaceutical Inc. Isoquinoline derivatives as mutant egfr modulators and uses thereof
EP4423086A1 (en) 2021-10-25 2024-09-04 Kymera Therapeutics, Inc. Tyk2 degraders and uses thereof
CA3236265A1 (en) 2021-10-29 2023-05-04 William Leong Irak4 degraders and synthesis thereof
CA3243560A1 (en) 2022-01-31 2023-08-03 Kymera Therapeutics, Inc. Iraqi Degradation Agents and Their Uses
CA3249074A1 (en) 2022-06-06 2023-12-14 C4 Therapeutics, Inc. BICYCLIC SUBSTITUTION GLUTARIMIDE CEREBLON BINDERS
EP4735438A2 (en) 2023-06-30 2026-05-06 Merck Patent GmbH Heterobifunctional compounds for the degradation of kras
EP4735452A2 (en) 2023-06-30 2026-05-06 Merck Patent GmbH Heterobifunctional compounds for the degradation of kras protein

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090053245A1 (en) 2007-05-29 2009-02-26 Mutz Mitchell W Pharmacokinetics and Efficacy of Anti-Angiogenic Drugs and Drugs Treating Diseases of the Blood
WO2014182744A1 (en) 2013-05-08 2014-11-13 The Johns Hopkins University Novel bis-benzylidine piperidone proteasome inhibitor with anticancer activity
WO2017024317A2 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
JP2018502097A (ja) 2014-12-23 2018-01-25 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

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2667196A1 (en) 2012-05-26 2013-11-27 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Bioorthogonal chemical inducers of reversible dimerization for control of protein interactions in cells
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
GB201506871D0 (en) * 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
EP4242304A3 (en) 2015-10-01 2024-02-07 Revolution Medicines, Inc. Methods and reagents for analyzing protein-protein interfaces

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090053245A1 (en) 2007-05-29 2009-02-26 Mutz Mitchell W Pharmacokinetics and Efficacy of Anti-Angiogenic Drugs and Drugs Treating Diseases of the Blood
WO2014182744A1 (en) 2013-05-08 2014-11-13 The Johns Hopkins University Novel bis-benzylidine piperidone proteasome inhibitor with anticancer activity
JP2018502097A (ja) 2014-12-23 2018-01-25 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
WO2017024317A2 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Chemistry & Biology,2006年,Vol.13, No.7,pp.711-722

Also Published As

Publication number Publication date
AU2019225166B2 (en) 2024-10-31
EP3755325A4 (en) 2022-03-02
JP7820423B2 (ja) 2026-02-25
US11802132B2 (en) 2023-10-31
CA3090417A1 (en) 2019-08-29
AU2019225166A1 (en) 2020-08-06
JP2021514958A (ja) 2021-06-17
JP2024054209A (ja) 2024-04-16
CN112020358A (zh) 2020-12-01
WO2019165229A1 (en) 2019-08-29
EP3755325A1 (en) 2020-12-30
US20200407371A1 (en) 2020-12-31

Similar Documents

Publication Publication Date Title
JP7820423B2 (ja) 選択的なタンパク質分解を誘導するための低分子およびその使用法
AU2017363313B2 (en) Inhibitors of interleukin-1 receptor-associated kinases and uses thereof
US12187701B2 (en) Taire family kinase inhibitors and uses thereof
JP7675070B2 (ja) 治療、特にmyd88変異疾患における使用のためのhck阻害剤としてのピラゾロピリミジン誘導体
AU2020301399B2 (en) HCK degraders and uses thereof
AU2019224089B2 (en) Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof
AU2023356963A1 (en) Cereblon-recruiting bcl-xl/bcl-2 dual degraders
US20240376074A1 (en) Nampt inhibitors and uses thereof
US20220348590A1 (en) Cyclooxygenase-2 inhibitors and uses thereof
US20230117680A1 (en) Cyclophilin d inhibitors and uses thereof
AU2020362194B2 (en) A pyrazolopyrimidine derivative as a HCK inhibitor for use in therapy, in particular MYD88 mutated diseases
US20250109165A1 (en) Cyclophilin inhibitors and uses thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200930

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20210127

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220216

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20220216

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20230123

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20230125

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20230421

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230712

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20230712

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20231010

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240206

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20240215

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: 20240328

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20240410

R150 Certificate of patent or registration of utility model

Ref document number: 7472026

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150