CN112020358A - 诱导蛋白质选择性降解的小分子及其用途 - Google Patents

诱导蛋白质选择性降解的小分子及其用途 Download PDF

Info

Publication number
CN112020358A
CN112020358A CN201980027535.9A CN201980027535A CN112020358A CN 112020358 A CN112020358 A CN 112020358A CN 201980027535 A CN201980027535 A CN 201980027535A CN 112020358 A CN112020358 A CN 112020358A
Authority
CN
China
Prior art keywords
optionally substituted
certain embodiments
alkyl
heteroaryl
compound
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
CN201980027535.9A
Other languages
English (en)
Chinese (zh)
Inventor
K·C·安德森
L·吴
J·齐
Y·宋
P·朴
D·察哈恩
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.)
Dana Farber Cancer Institute Inc
Original Assignee
Dana Farber Cancer Institute 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 Dana Farber Cancer Institute Inc filed Critical Dana Farber Cancer Institute Inc
Publication of CN112020358A publication Critical patent/CN112020358A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • C07D495/12—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 three hetero rings
    • C07D495/14—Ortho-condensed systems
    • 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
    • A61K47/545—Heterocyclic compounds
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/12—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 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)
CN201980027535.9A 2018-02-23 2019-02-22 诱导蛋白质选择性降解的小分子及其用途 Pending CN112020358A (zh)

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

Publications (1)

Publication Number Publication Date
CN112020358A true CN112020358A (zh) 2020-12-01

Family

ID=67687887

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980027535.9A Pending CN112020358A (zh) 2018-02-23 2019-02-22 诱导蛋白质选择性降解的小分子及其用途

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

Family Cites Families (8)

* 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
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
WO2014182744A1 (en) 2013-05-08 2014-11-13 The Johns Hopkins University Novel bis-benzylidine piperidone proteasome inhibitor with anticancer activity
WO2016105518A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
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
WO2017024317A2 (en) * 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP4242304A3 (en) 2015-10-01 2024-02-07 Revolution Medicines, Inc. Methods and reagents for analyzing protein-protein interfaces

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
WO2019165229A1 (en) 2019-08-29
JP7472026B2 (ja) 2024-04-22
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
AU2015371251B2 (en) Inhibitors of cyclin-dependent kinase 7 (CDK7)
JP7660063B2 (ja) サイクリン依存性キナーゼ７のインヒビターおよびそれらの使用
US10711036B2 (en) MALT1 inhibitors and uses thereof
JP7680999B2 (ja) サイクリン依存性キナーゼ７のインヒビターおよびそれらの使用
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
AU2019224089B2 (en) Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof
US20230058545A1 (en) Hck as a therapeutic target in myd88 mutated diseases
CA2972239C (en) Inhibitors of cyclin-dependent kinase 7 (cdk7)

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20201201

WD01 Invention patent application deemed withdrawn after publication