CN117295523A - 靶向pxr的双官能protac型化合物、其制备方法及其治疗用途 - Google Patents

靶向pxr的双官能protac型化合物、其制备方法及其治疗用途 Download PDF

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Publication number
CN117295523A
CN117295523A CN202280035417.4A CN202280035417A CN117295523A CN 117295523 A CN117295523 A CN 117295523A CN 202280035417 A CN202280035417 A CN 202280035417A CN 117295523 A CN117295523 A CN 117295523A
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CN
China
Prior art keywords
compound
pxr
group
ligase
formula
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
CN202280035417.4A
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English (en)
Chinese (zh)
Inventor
吉恩-马克·帕斯库西
J·帕内坎
M·安布拉尔-科西
G·拉孔达
萨比尼·格尔巴尔-查洛因
阿兰·查瓦尼尤
威廉·布尔盖特
凡妮莎·德尔福斯
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.)
Centre National de la Recherche Scientifique CNRS
Institut National de la Sante et de la Recherche Medicale INSERM
Ecole Nationale Superieure de Chimie de Montpellier ENSCM
Universite de Montpellier
Original Assignee
Centre National de la Recherche Scientifique CNRS
Institut National de la Sante et de la Recherche Medicale INSERM
Ecole Nationale Superieure de Chimie de Montpellier ENSCM
Universite de Montpellier
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 Centre National de la Recherche Scientifique CNRS, Institut National de la Sante et de la Recherche Medicale INSERM, Ecole Nationale Superieure de Chimie de Montpellier ENSCM, Universite de Montpellier filed Critical Centre National de la Recherche Scientifique CNRS
Publication of CN117295523A publication Critical patent/CN117295523A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14—Radicals substituted by nitrogen atoms
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
CN202280035417.4A 2021-05-19 2022-05-18 靶向pxr的双官能protac型化合物、其制备方法及其治疗用途 Pending CN117295523A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR2105217 2021-05-19
FR2105217A FR3122989B1 (fr) 2021-05-19 2021-05-19 Nouveaux composes bifonctionnels de type protac ciblant pxr, leur procede de preparation et leur utilisation en therapeutique
PCT/EP2022/063422 WO2022243365A1 (fr) 2021-05-19 2022-05-18 Composés bifonctionnels de type protac ciblant pxr, leur procédé de préparation et leur utilisation en thérapeutique

Publications (1)

Publication Number Publication Date
CN117295523A true CN117295523A (zh) 2023-12-26

Family

ID=76284058

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280035417.4A Pending CN117295523A (zh) 2021-05-19 2022-05-18 靶向pxr的双官能protac型化合物、其制备方法及其治疗用途

Country Status (7)

Country Link
US (1) US20240252658A1 (https=)
EP (1) EP4340887A1 (https=)
JP (1) JP2024519536A (https=)
CN (1) CN117295523A (https=)
CA (1) CA3218875A1 (https=)
FR (1) FR3122989B1 (https=)
WO (1) WO2022243365A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118344284A (zh) * 2024-03-06 2024-07-16 杭州医学院 一种具有苯甲酰胺结构的化合物及其制备方法和应用
CN121735909A (zh) * 2024-09-27 2026-03-27 上海交通大学医学院附属瑞金医院 多价分子胶类化合物及其制备和应用
US20260092058A1 (en) 2024-09-30 2026-04-02 St. Jude Children's Research Hospital, Inc. Small Molecule Degraders and Fluorescent Probes of PXR

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017223415A1 (en) * 2016-06-23 2017-12-28 Dana-Farber Cancer Institute, Inc. Degradation of tripartite motif-containing protein 24 (trim24) by conjugation of trim24 inhibitors with e3 ligase ligand and methods of use

Also Published As

Publication number Publication date
US20240252658A1 (en) 2024-08-01
FR3122989B1 (fr) 2024-03-29
EP4340887A1 (fr) 2024-03-27
JP2024519536A (ja) 2024-05-15
FR3122989A1 (fr) 2022-11-25
WO2022243365A1 (fr) 2022-11-24
CA3218875A1 (fr) 2022-11-24

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