MX2024000329A - Compuestos bifuncionales que comprenden una molecula que contiene una porcion dirigida a la proteina smarca (ptm) enlazada a una porcion de una molecula de union de ligasa de ubiquitina e3 (ulm), y su uso como moduladores de la ubiquitinacion dirigidos al tratamiento del cancer. - Google Patents

Compuestos bifuncionales que comprenden una molecula que contiene una porcion dirigida a la proteina smarca (ptm) enlazada a una porcion de una molecula de union de ligasa de ubiquitina e3 (ulm), y su uso como moduladores de la ubiquitinacion dirigidos al tratamiento del cancer.

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Publication number
MX2024000329A
MX2024000329A MX2024000329A MX2024000329A MX2024000329A MX 2024000329 A MX2024000329 A MX 2024000329A MX 2024000329 A MX2024000329 A MX 2024000329A MX 2024000329 A MX2024000329 A MX 2024000329A MX 2024000329 A MX2024000329 A MX 2024000329A
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Mexico
Prior art keywords
target protein
present disclosure
compounds
brm
associated methods
Prior art date
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MX2024000329A
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English (en)
Inventor
Peter DRAGOVICH
Leanna Staben
Huifen Chen
Andrew P Crew
Michael Berlin
Jing Wang
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Arvinas Operations Inc
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Publication date
Application filed by Arvinas Operations Inc filed Critical Arvinas Operations Inc
Publication of MX2024000329A publication Critical patent/MX2024000329A/es

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    • 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
    • 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
    • A61K31/41—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
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active 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
    • 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
    • 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
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente descripción se refiere a compuestos bifuncionales, que son útiles como moduladores de SMARCA2 o BRM (proteína diana). En particular, la presente descripción se refiere a compuestos bifuncionales, que contienen en un extremo un ligando que se une a la ligasa de ubiquitina E3 de Von Hippel-Lindau, y en el otro extremo una porción que se une a la proteína diana, de manera que la proteína diana se coloca en la proximidad de la ligasa de ubiquitina para efectuar la degradación (e inhibición) de la proteína diana. La presente descripción exhibe un amplio intervalo 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.
MX2024000329A 2018-04-01 2020-10-01 Compuestos bifuncionales que comprenden una molecula que contiene una porcion dirigida a la proteina smarca (ptm) enlazada a una porcion de una molecula de union de ligasa de ubiquitina e3 (ulm), y su uso como moduladores de la ubiquitinacion dirigidos al tratamiento del cancer. MX2024000329A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862651186P 2018-04-01 2018-04-01
US201962797754P 2019-01-28 2019-01-28

Publications (1)

Publication Number Publication Date
MX2024000329A true MX2024000329A (es) 2024-01-25

Family

ID=66175525

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2020010368A MX2020010368A (es) 2018-04-01 2019-04-01 Compuestos dirigidos a brm y métodos de uso asociados.
MX2024000329A MX2024000329A (es) 2018-04-01 2020-10-01 Compuestos bifuncionales que comprenden una molecula que contiene una porcion dirigida a la proteina smarca (ptm) enlazada a una porcion de una molecula de union de ligasa de ubiquitina e3 (ulm), y su uso como moduladores de la ubiquitinacion dirigidos al tratamiento del cancer.

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MX2020010368A MX2020010368A (es) 2018-04-01 2019-04-01 Compuestos dirigidos a brm y métodos de uso asociados.

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US (2) US20190300521A1 (es)
EP (1) EP3774789A1 (es)
JP (2) JP2021520350A (es)
KR (2) KR20240130153A (es)
CN (1) CN112166114A (es)
AU (3) AU2019249849C1 (es)
BR (1) BR112020020196A2 (es)
CA (1) CA3094305A1 (es)
CL (1) CL2020002546A1 (es)
CO (1) CO2020013762A2 (es)
CR (1) CR20200527A (es)
IL (1) IL277677A (es)
MX (2) MX2020010368A (es)
PE (1) PE20212108A1 (es)
PH (1) PH12020500663A1 (es)
SG (1) SG11202008898UA (es)
WO (1) WO2019195201A1 (es)

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BR112020020196A2 (pt) 2021-01-26
IL277677A (en) 2020-11-30
EP3774789A1 (en) 2021-02-17
SG11202008898UA (en) 2020-10-29
US20240076295A1 (en) 2024-03-07
WO2019195201A1 (en) 2019-10-10
US20190300521A1 (en) 2019-10-03
KR102697733B1 (ko) 2024-08-26
JP2021520350A (ja) 2021-08-19
AU2019249849B2 (en) 2022-03-17
MX2020010368A (es) 2021-01-08
PH12020500663A1 (en) 2021-06-07
KR20240130153A (ko) 2024-08-28
PE20212108A1 (es) 2021-11-04
RU2020135754A (ru) 2022-05-04
CO2020013762A2 (es) 2021-01-18
CL2020002546A1 (es) 2021-01-29
AU2024203058A1 (en) 2024-05-30
KR20210005037A (ko) 2021-01-13
RU2020135754A3 (es) 2022-05-04
JP2023071767A (ja) 2023-05-23
AU2019249849C1 (en) 2022-09-29
CA3094305A1 (en) 2019-10-10
CN112166114A (zh) 2021-01-01
AU2019249849A1 (en) 2020-10-01
CR20200527A (es) 2021-04-09
AU2022204042A1 (en) 2022-06-30

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