KR20230106637A - 빈혈 및 암 치료용 vhl 억제제로서의 1-(2-(4-시클로프로필-1h-1,2,3-트리아졸-1-일)아세틸)-4-히드록시-n-(벤질)피롤리딘 e-2-카르복사미드 유도체 - Google Patents

빈혈 및 암 치료용 vhl 억제제로서의 1-(2-(4-시클로프로필-1h-1,2,3-트리아졸-1-일)아세틸)-4-히드록시-n-(벤질)피롤리딘 e-2-카르복사미드 유도체 Download PDF

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Publication number
KR20230106637A
KR20230106637A KR1020237018547A KR20237018547A KR20230106637A KR 20230106637 A KR20230106637 A KR 20230106637A KR 1020237018547 A KR1020237018547 A KR 1020237018547A KR 20237018547 A KR20237018547 A KR 20237018547A KR 20230106637 A KR20230106637 A KR 20230106637A
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alkyl
independently
pharmaceutically acceptable
tautomer
foregoing
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English (en)
Korean (ko)
Inventor
자코브 퍼만
하오 우
웨인 제이. 페어브라더
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제넨테크, 인크.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020237018547A 2020-11-11 2020-11-30 빈혈 및 암 치료용 vhl 억제제로서의 1-(2-(4-시클로프로필-1h-1,2,3-트리아졸-1-일)아세틸)-4-히드록시-n-(벤질)피롤리딘 e-2-카르복사미드 유도체 Pending KR20230106637A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063112609P 2020-11-11 2020-11-11
US63/112,609 2020-11-11
PCT/US2020/062627 WO2022103411A1 (en) 2020-11-11 2020-11-30 1-(2-(4-cyclopropyl-1h-1,2,3-triazol-1-yl)acetyl)-4-hydroxy-n-(benzyl)pyrrolidin e-2-carboxamide derivatives as vhl inhibitors for the treatment of anemia and cancer

Publications (1)

Publication Number Publication Date
KR20230106637A true KR20230106637A (ko) 2023-07-13

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020237018547A Pending KR20230106637A (ko) 2020-11-11 2020-11-30 빈혈 및 암 치료용 vhl 억제제로서의 1-(2-(4-시클로프로필-1h-1,2,3-트리아졸-1-일)아세틸)-4-히드록시-n-(벤질)피롤리딘 e-2-카르복사미드 유도체

Country Status (10)

Country Link
US (1) US20230391766A1 (https=)
EP (1) EP4244218A1 (https=)
JP (2) JP7654075B2 (https=)
KR (1) KR20230106637A (https=)
CN (1) CN116783183B (https=)
AU (1) AU2020476996A1 (https=)
CA (1) CA3197092A1 (https=)
IL (1) IL302678A (https=)
MX (1) MX2023005305A (https=)
WO (1) WO2022103411A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119677735A (zh) * 2022-05-11 2025-03-21 基因泰克公司 作为vhl配体的苯并噻唑化合物
WO2025162250A1 (zh) * 2024-02-04 2025-08-07 贝达药业股份有限公司 取代的三环化合物及其用途
WO2025228305A1 (zh) * 2024-04-28 2025-11-06 中国科学院上海药物研究所 一种蛋白降解剂缀合物及其偶联物
WO2026012475A1 (en) * 2024-07-12 2026-01-15 Ascentage Pharma (Suzhou) Co., Ltd. Vhl ligands and uses thereof

Family Cites Families (6)

* 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
WO2013106646A2 (en) * 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
KR102668696B1 (ko) * 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
GB2554071A (en) * 2016-09-14 2018-03-28 Univ Dundee Small molecules
CN110573507B (zh) * 2017-04-14 2023-11-14 邓迪大学 小分子
US11547759B2 (en) * 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor

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Publication number Publication date
MX2023005305A (es) 2023-05-25
WO2022103411A1 (en) 2022-05-19
US20230391766A1 (en) 2023-12-07
AU2020476996A1 (en) 2023-06-29
CN116783183A (zh) 2023-09-19
CA3197092A1 (en) 2022-05-19
CN116783183B (zh) 2026-03-20
JP7654075B2 (ja) 2025-03-31
IL302678A (en) 2023-07-01
JP2023549187A (ja) 2023-11-22
EP4244218A1 (en) 2023-09-20
JP2025063287A (ja) 2025-04-15

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