FR3122989B1 - Nouveaux composes bifonctionnels de type protac ciblant pxr, leur procede de preparation et leur utilisation en therapeutique - Google Patents

Nouveaux composes bifonctionnels de type protac ciblant pxr, leur procede de preparation et leur utilisation en therapeutique Download PDF

Info

Publication number
FR3122989B1
FR3122989B1 FR2105217A FR2105217A FR3122989B1 FR 3122989 B1 FR3122989 B1 FR 3122989B1 FR 2105217 A FR2105217 A FR 2105217A FR 2105217 A FR2105217 A FR 2105217A FR 3122989 B1 FR3122989 B1 FR 3122989B1
Authority
FR
France
Prior art keywords
pxr
preparation
protac
therapeutics
new
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
FR2105217A
Other languages
English (en)
French (fr)
Other versions
FR3122989A1 (fr
Inventor
Julie Pannequin
Jean-Marc Pascussi
Muriel Amblard-Caussil
Guillaume Laconde
Sabine Gerbal-Chaloin
Alain Chavanieu
William Bourguet
Vanessa Delfosse
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
Priority to FR2105217A priority Critical patent/FR3122989B1/fr
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
Priority to EP22733859.7A priority patent/EP4340887A1/fr
Priority to JP2023572137A priority patent/JP2024519536A/ja
Priority to US18/562,251 priority patent/US20240252658A1/en
Priority to CA3218875A priority patent/CA3218875A1/fr
Priority to CN202280035417.4A priority patent/CN117295523A/zh
Priority to PCT/EP2022/063422 priority patent/WO2022243365A1/fr
Publication of FR3122989A1 publication Critical patent/FR3122989A1/fr
Application granted granted Critical
Publication of FR3122989B1 publication Critical patent/FR3122989B1/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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)
FR2105217A 2021-05-19 2021-05-19 Nouveaux composes bifonctionnels de type protac ciblant pxr, leur procede de preparation et leur utilisation en therapeutique Active FR3122989B1 (fr)

Priority Applications (7)

Application Number Priority Date Filing Date Title
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
JP2023572137A JP2024519536A (ja) 2021-05-19 2022-05-18 Ｐｘｒを標的とする二官能性ｐｒｏｔａｃ型化合物、同化合物を調製するための方法、及びその治療的使用
US18/562,251 US20240252658A1 (en) 2021-05-19 2022-05-18 Bifunctional protac-type compounds targeting pxr, method for preparing same and therapeutic use thereof
CA3218875A CA3218875A1 (fr) 2021-05-19 2022-05-18 Composes bifonctionnels de type protac ciblant pxr, leur procede de preparation et leur utilisation en therapeutique
EP22733859.7A EP4340887A1 (fr) 2021-05-19 2022-05-18 Composés bifonctionnels de type protac ciblant pxr, leur procédé de préparation et leur utilisation en thérapeutique
CN202280035417.4A 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
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

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
FR3122989A1 FR3122989A1 (fr) 2022-11-25
FR3122989B1 true FR3122989B1 (fr) 2024-03-29

Family

ID=76284058

Family Applications (1)

Application Number Title Priority Date Filing Date
FR2105217A Active 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

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
CN117295523A (zh) 2023-12-26
US20240252658A1 (en) 2024-08-01
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

Similar Documents

Publication Publication Date Title
FR3122989B1 (fr) Nouveaux composes bifonctionnels de type protac ciblant pxr, leur procede de preparation et leur utilisation en therapeutique
MX2023002034A (es) Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas.
EP0656790A4 (en) COMPOSITIONS AND METHODS FOR MODULATING RNA.
NO880705D0 (no) Fremgangsmaate til fremstilling av makromolekylare platinaforbindelser med virkning mot kreft.
Rousso-Noori et al. P32-specific CAR T cells with dual antitumor and antiangiogenic therapeutic potential in gliomas
EP0396387A3 (en) A novel antibody delivery system for biological response modifiers
MX2023005081A (es) Anticuerpos multiespecificos para dirigirse a cd28 y pd-l1 y metodos de uso de los mismos.
FI941572L (fi) Anti-erbB-2-monoklonaalisten vasta-aineiden yhdistelmä ja käyttömenetelmä
BRPI0411526A (pt) vìrus de vaccinia e outros microrganismos recombinates modificados e usos dos mesmos
WO2005000901A3 (en) Cd20-specific antibodies and methods of employing same
MA44547B1 (fr) Anticorps anti-pd-1,procédé de leur production et de leur utilisation
WO2006096754A3 (en) Stabilized aptamers to psma and their use as prostate cancer therapeutics
CA3016333A1 (en) Nanoliposomal targeting of ephrin receptor a2 (epha2) and related diagnostics
WO2001064751A3 (en) High potency recombinant antibodies and method for producing them
PT920623E (pt) Terapia de captura neutronica do bono utilizando metodo de pre-direccionamento
EP0954334A4 (en) Use of macrophage migration inhibitory factor antagonists for cancer therapy
Stepanov et al. Control of the antitumour activity and specificity of CAR T cells via organic adapters covalently tethering the CAR to tumour cells
WO2022084331A3 (en) Novel ligands for asialoglycoprotein receptor
TW200833699A (en) P-toluene sulfonic acid salt of 5-amino-3-(2'-O-acetyl-3'-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidine-2-one and methods for preparation
Zhang et al. CircRNA circ_0006892 regulates miR‐24/PHLPP2 axis to mitigate cigarette smoke extract‐induced bronchial epithelial cell injury
WO2024178202A3 (en) Anti-cd3 antibodies and methods for their use
BRPI0409575A (pt) anticorpos especìficos às células endoteliais e usos dos mesmos
Wei et al. Anticancer activity of a thymidine quinoxaline conjugate is modulated by cytosolic thymidine pathways
Pastore et al. Adenosine receptor antagonists A2AR (TT-10) and A2BR (TT-4) demonstrate anti-tumor activity in 4T1-induced syngeneic breast cancer mouse model
Rothenberg et al. Phase I dose-escalation study of the anti-IGF-IR recombinant human IgG1 monoclonal antibody (Mab) IMC-A12, administered every other week to patients with advanced solid tumors

Legal Events

Date Code Title Description
PLFP Fee payment

Year of fee payment: 2

PLSC Publication of the preliminary search report

Effective date: 20221125

PLFP Fee payment

Year of fee payment: 3

PLFP Fee payment

Year of fee payment: 4

PLFP Fee payment

Year of fee payment: 5