KR20210122165A - Plk1의 선택적 분해를 유도하는 바닐린 유도체 화합물 - Google Patents

Plk1의 선택적 분해를 유도하는 바닐린 유도체 화합물 Download PDF

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KR20210122165A
KR20210122165A KR1020210040038D KR20210040038D KR20210122165A KR 20210122165 A KR20210122165 A KR 20210122165A KR 1020210040038 D KR1020210040038 D KR 1020210040038D KR 20210040038 D KR20210040038 D KR 20210040038D KR 20210122165 A KR20210122165 A KR 20210122165A
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South Korea
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plk1
formula
compound
mmol
cancer
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Korean (ko)
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최시우
류수희
류지훈
손산하
이화진
김성훈
남보아스
민임숙
류혜국
강금영
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(주) 업테라
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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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pain & Pain Management (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
KR1020210040038D 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 바닐린 유도체 화합물 Granted KR20210122165A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020200037875 2020-03-27
KR20200037875 2020-03-27

Publications (1)

Publication Number Publication Date
KR20210122165A true KR20210122165A (ko) 2021-10-08

Family

ID=77892014

Family Applications (8)

Application Number Title Priority Date Filing Date
KR1020210040038D Granted KR20210122165A (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 바닐린 유도체 화합물
KR1020210040036D Granted KR20210122163A (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 피라졸로퀴나졸린 유도체 화합물
KR1020210040037A Active KR102319264B1 (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 벤즈이미다졸 티오펜 유도체 화합물
KR1020210040038A Active KR102313753B1 (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 바닐린 유도체 화합물
KR1020210040035A Active KR102337029B1 (ko) 2020-03-27 2021-03-27 Plk1 선택적 분해 유도 화합물
KR1020210040037D Granted KR20210122164A (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 벤즈이미다졸 티오펜 유도체 화합물
KR1020210040036A Active KR102313752B1 (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 피라졸로퀴나졸린 유도체 화합물
KR1020210171223A Active KR102529222B1 (ko) 2020-03-27 2021-12-02 Plk1 선택적 분해 유도 화합물

Family Applications After (7)

Application Number Title Priority Date Filing Date
KR1020210040036D Granted KR20210122163A (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 피라졸로퀴나졸린 유도체 화합물
KR1020210040037A Active KR102319264B1 (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 벤즈이미다졸 티오펜 유도체 화합물
KR1020210040038A Active KR102313753B1 (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 바닐린 유도체 화합물
KR1020210040035A Active KR102337029B1 (ko) 2020-03-27 2021-03-27 Plk1 선택적 분해 유도 화합물
KR1020210040037D Granted KR20210122164A (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 벤즈이미다졸 티오펜 유도체 화합물
KR1020210040036A Active KR102313752B1 (ko) 2020-03-27 2021-03-27 Plk1의 선택적 분해를 유도하는 피라졸로퀴나졸린 유도체 화합물
KR1020210171223A Active KR102529222B1 (ko) 2020-03-27 2021-12-02 Plk1 선택적 분해 유도 화합물

Country Status (6)

Country Link
US (5) US20230158158A1 (https=)
EP (1) EP3911654A4 (https=)
JP (2) JP7440940B2 (https=)
KR (8) KR20210122165A (https=)
CN (1) CN113784969A (https=)
WO (4) WO2021194318A1 (https=)

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EP4157849A4 (en) * 2021-08-10 2024-12-11 Uppthera, Inc. NOVEL PLK1 DEGRADATION-INDUCING COMPOUND
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CN118339161B (zh) * 2021-12-10 2025-12-09 正大天晴药业集团股份有限公司 一种异噻唑并[5,4-d]嘧啶类IRAK4抑制剂的制备方法
CN118382626A (zh) * 2021-12-10 2024-07-23 山东绿叶制药有限公司 蛋白激酶抑制剂及其制备方法和应用
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CN120603831A (zh) * 2022-11-29 2025-09-05 厄普特拉株式会社 具有增加的刚性的plk1降解诱导化合物
CN120530121A (zh) * 2023-01-17 2025-08-22 北京哲源科技有限责任公司 吡唑并喹唑啉类化合物的立体异构体和氘代衍生物及应用
KR20250037591A (ko) * 2023-02-02 2025-03-17 (주) 업테라 신규 plk1 분해 유도 화합물
CN116554044A (zh) * 2023-05-16 2023-08-08 上海师范大学 一种无氨基保护的2,6-二异丙基-4-羧基苯胺及其合成方法
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WO2025239662A1 (ko) * 2024-05-13 2025-11-20 (주) 업테라 분해 약물-항체 접합체용 plk1 분해 유도 화합물
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EP4157849A4 (en) * 2021-08-10 2024-12-11 Uppthera, Inc. NOVEL PLK1 DEGRADATION-INDUCING COMPOUND

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KR102319264B1 (ko) 2021-11-01
KR20210122163A (ko) 2021-10-08
JP2022539579A (ja) 2022-09-12
US12403198B2 (en) 2025-09-02
KR102313752B1 (ko) 2021-10-19
WO2021194321A1 (en) 2021-09-30
KR102337029B1 (ko) 2021-12-09
JP2023171659A (ja) 2023-12-01
WO2021194320A1 (en) 2021-09-30
WO2021194318A1 (en) 2021-09-30
US20230159515A1 (en) 2023-05-25
US20230203006A1 (en) 2023-06-29
EP3911654A4 (en) 2022-05-11
KR20210122162A (ko) 2021-10-08
KR102313753B1 (ko) 2021-10-19
KR20210150341A (ko) 2021-12-10
US20230372498A1 (en) 2023-11-23
EP3911654A1 (en) 2021-11-24
US11833208B2 (en) 2023-12-05
US20230104076A1 (en) 2023-04-06
WO2021194319A1 (en) 2021-09-30
KR20210122164A (ko) 2021-10-08
KR102529222B1 (ko) 2023-05-08
JP7440940B2 (ja) 2024-02-29
US20230158158A1 (en) 2023-05-25
CN113784969A (zh) 2021-12-10

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