MX2020010420A - Moduladores de la proteólisis y métodos asociados de uso. - Google Patents

Moduladores de la proteólisis y métodos asociados de uso.

Info

Publication number
MX2020010420A
MX2020010420A MX2020010420A MX2020010420A MX2020010420A MX 2020010420 A MX2020010420 A MX 2020010420A MX 2020010420 A MX2020010420 A MX 2020010420A MX 2020010420 A MX2020010420 A MX 2020010420A MX 2020010420 A MX2020010420 A MX 2020010420A
Authority
MX
Mexico
Prior art keywords
target protein
present disclosure
modulators
binds
inhibition
Prior art date
Application number
MX2020010420A
Other languages
English (en)
Inventor
Craig M Crews
Andrew P Crew
Hanqing Dong
Keith R Hornberger
Michael Berlin
Jing Wang
Original Assignee
Arvinas Operations 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 Arvinas Operations Inc filed Critical Arvinas Operations Inc
Publication of MX2020010420A publication Critical patent/MX2020010420A/es

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Classifications

    • 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
    • C07K5/10—Tetrapeptides
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • 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
    • 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

La presente descripción hace referencia a compuestos bifuncionales, que son útiles como moduladores de la proteína de sarcoma de rata Kirsten (proteína diana). En particular, la presente descripción se dirige a compuestos bifuncionales, que contienen en un extremo un ligando de Von Hippel-Lindau, cereblon, inhibidores de las proteínas de apoptosis u homólogo diminuto doble de ratón 2 que se une a la ubiquitina ligasa E3 respectiva y en el otro extremo un resto que se une a una proteína diana, de forma tal que la proteína diana se ubique cerca de la ubiquitina ligasa para efectuar la degradación (e inhibición) de la proteína diana. La presente descripción presenta una amplia variedad de actividades farmacológicas asociadas a la degradación/inhibición de la proteína diana. Las enfermedades o los trastornos que resultan de la agregación, acumulación y/o sobreactivación de la proteína diana se tratan o previenen con compuestos y composiciones de la presente descripción.
MX2020010420A 2018-04-04 2019-04-04 Moduladores de la proteólisis y métodos asociados de uso. MX2020010420A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862652676P 2018-04-04 2018-04-04
PCT/US2019/025878 WO2019195609A2 (en) 2018-04-04 2019-04-04 Modulators of proteolysis and associated methods of use

Publications (1)

Publication Number Publication Date
MX2020010420A true MX2020010420A (es) 2020-12-11

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
MX2020010420A MX2020010420A (es) 2018-04-04 2019-04-04 Moduladores de la proteólisis y métodos asociados de uso.
MX2023010341A MX2023010341A (es) 2018-04-04 2020-10-02 Moduladores de la proteolisis y metodos asociados de uso.

Family Applications After (1)

Application Number Title Priority Date Filing Date
MX2023010341A MX2023010341A (es) 2018-04-04 2020-10-02 Moduladores de la proteolisis y metodos asociados de uso.

Country Status (12)

Country Link
US (2) US11161841B2 (es)
EP (1) EP3774777A2 (es)
JP (1) JP2021521112A (es)
KR (2) KR20210006356A (es)
CN (1) CN112218859A (es)
AU (2) AU2019249231B2 (es)
BR (1) BR112020020307A2 (es)
CA (1) CA3095494C (es)
CO (1) CO2020013864A2 (es)
IL (1) IL277729A (es)
MX (2) MX2020010420A (es)
WO (1) WO2019195609A2 (es)

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