MX2019007646A - Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso. - Google Patents

Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.

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Publication number
MX2019007646A
MX2019007646A MX2019007646A MX2019007646A MX2019007646A MX 2019007646 A MX2019007646 A MX 2019007646A MX 2019007646 A MX2019007646 A MX 2019007646A MX 2019007646 A MX2019007646 A MX 2019007646A MX 2019007646 A MX2019007646 A MX 2019007646A
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MX
Mexico
Prior art keywords
target protein
present disclosure
egfr
associated methods
chimeric molecules
Prior art date
Application number
MX2019007646A
Other languages
English (en)
Inventor
Qian Yimin
Jaime-Figueroa Saul
M Crews Craig
Zimmermann Kurt
P Crew Andrew
Dong Hanqing
Berlin Michael
Wang Jing
Ishchenko Alexey
Burslem George
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 MX2019007646A publication Critical patent/MX2019007646A/es

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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • 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
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    • 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente descripción se refiere a compuestos bifuncionales, que encuentran utilidad como moduladores de las proteínas del receptor tirosina quinasa (RTK). En particular, la presente descripción se dirige a compuestos bifuncionales, que contienen en un extremo un ligando que se une a una ligasa de ubiquitina E3, y en el otro extremo una porción que se une a la proteína diana, de manera que la proteína diana se ubica en la proximidad de la ligasa de ubiquitina para efectuar la ubiquitinación, y por lo tanto la degradación (e inhibición) de la proteína diana. La presente descripción exhibe una amplia gama de actividades farmacológicas, asociadas con la degradación/inhibición de la proteína diana. Las enfermedades o trastornos que resultan de la agregación o acumulación de la proteína diana, se tratan o se previenen con los compuestos y composiciones de la presente descripción.YY.
MX2019007646A 2016-12-23 2017-12-22 Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso. MX2019007646A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662438901P 2016-12-23 2016-12-23
US201762563494P 2017-09-26 2017-09-26
PCT/US2017/068308 WO2018119441A1 (en) 2016-12-23 2017-12-22 Egfr proteolysis targeting chimeric molecules and associated methods of use

Publications (1)

Publication Number Publication Date
MX2019007646A true MX2019007646A (es) 2019-09-06

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MX2019007646A MX2019007646A (es) 2016-12-23 2017-12-22 Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso.

Country Status (13)

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US (2) US10994015B2 (es)
EP (1) EP3559002A4 (es)
JP (1) JP2020505327A (es)
KR (1) KR20190101406A (es)
CN (1) CN110753693A (es)
AU (1) AU2017382406A1 (es)
BR (1) BR112019012682A2 (es)
CA (1) CA3047586A1 (es)
CO (1) CO2019007892A2 (es)
IL (1) IL267398A (es)
MX (1) MX2019007646A (es)
RU (1) RU2019121527A (es)
WO (1) WO2018119441A1 (es)

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