RS64976B1 - Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora - Google Patents

Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora

Info

Publication number
RS64976B1
RS64976B1 RS20231227A RSP20231227A RS64976B1 RS 64976 B1 RS64976 B1 RS 64976B1 RS 20231227 A RS20231227 A RS 20231227A RS P20231227 A RSP20231227 A RS P20231227A RS 64976 B1 RS64976 B1 RS 64976B1
Authority
RS
Serbia
Prior art keywords
inhibitor
compound
cancer
group
mmol
Prior art date
Application number
RS20231227A
Other languages
English (en)
Serbian (sr)
Inventor
Andrew P Crew
Yimin Qian
Hanqing Dong
Jing Wang
Keith R Hornberger
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 RS64976B1 publication Critical patent/RS64976B1/sr

Links

Classifications

    • 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
    • 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
    • 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
    • A61K31/435—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
    • 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
    • A61K31/435—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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • 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
    • A61K38/05—Dipeptides
    • 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
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • C07D401/02—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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14—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 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
    • C07D417/14—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
    • 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
    • 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
    • C07D487/04—Ortho-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
    • 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
    • C07D487/10—Spiro-condensed 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
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
RS20231227A 2016-12-01 2017-12-01 Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora RS64976B1 (sr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662429041P 2016-12-01 2016-12-01
US201762540049P 2017-08-01 2017-08-01
EP20150584.9A EP3689868B1 (en) 2016-12-01 2017-12-01 Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders

Publications (1)

Publication Number Publication Date
RS64976B1 true RS64976B1 (sr) 2024-01-31

Family

ID=62240410

Family Applications (1)

Application Number Title Priority Date Filing Date
RS20231227A RS64976B1 (sr) 2016-12-01 2017-12-01 Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora

Country Status (24)

Country Link
US (7) US10647698B2 (enExample)
EP (2) EP3689868B1 (enExample)
JP (7) JP6957620B2 (enExample)
KR (3) KR102674902B1 (enExample)
CN (4) CN110291087B (enExample)
AU (5) AU2017366693B2 (enExample)
BR (1) BR112019011200B1 (enExample)
CA (1) CA3042968C (enExample)
CO (1) CO2019007091A2 (enExample)
DK (1) DK3689868T3 (enExample)
ES (1) ES2967404T3 (enExample)
FI (1) FI3689868T3 (enExample)
HR (1) HRP20231537T1 (enExample)
HU (1) HUE064609T2 (enExample)
IL (5) IL316544A (enExample)
LT (1) LT3689868T (enExample)
MX (2) MX2019006402A (enExample)
PL (1) PL3689868T3 (enExample)
PT (1) PT3689868T (enExample)
RS (1) RS64976B1 (enExample)
RU (1) RU2750484C2 (enExample)
SI (1) SI3689868T1 (enExample)
SM (1) SMT202300483T1 (enExample)
WO (1) WO2018102725A1 (enExample)

Families Citing this family (156)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
HK1245791A1 (zh) 2015-01-20 2018-08-31 阿尔维纳斯运营股份有限公司 用於雄激素受体的靶向降解的化合物和方法
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
CN108137507A (zh) 2015-07-10 2018-06-08 阿尔维纳斯股份有限公司 基于mdm2的蛋白水解调节剂和相关的使用方法
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
EP4483875A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
ES2975558T3 (es) 2016-09-15 2024-07-09 Arvinas Inc Derivados de indol como degradantes de receptor de estrógeno
WO2018067702A1 (en) 2016-10-04 2018-04-12 Massachusetts Institute Of Technology Bottlebrush copolymers and uses thereof
EP3535265A4 (en) 2016-11-01 2020-07-08 Arvinas, Inc. PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE
WO2018102725A1 (en) * 2016-12-01 2018-06-07 Arvinas, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
RU2019121527A (ru) 2016-12-23 2021-01-15 Эрвинэс Оперейшнс, Инк. Химерные молекулы, нацеливающиеся на протеолиз egfr, и связанные с ними способы применения
EP3558994A4 (en) 2016-12-23 2021-05-12 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF FAST ACCELERATED FIBROSARCOMA POLYPEPTIDES
EP3559006A4 (en) 2016-12-23 2021-03-03 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF F TAL LIVER KINASE POLYPEPTIDES
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
MX2019008934A (es) 2017-01-26 2019-11-05 Arvinas Operations Inc Moduladores de la proteolisis del receptor de estrogeno y métodos asociados de uso,.
EP3577109A4 (en) 2017-01-31 2020-11-18 Arvinas Operations, Inc. CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM
EP3641762B1 (en) 2017-06-20 2026-02-18 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
EP3679028A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Dihydroquinolinones
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
JP2021512153A (ja) 2018-01-26 2021-05-13 イエール ユニバーシティ タンパク質分解のイミド系モジュレーターおよび使用方法
KR20210018199A (ko) 2018-03-26 2021-02-17 씨4 테라퓨틱스, 인코포레이티드 이카로스의 분해를 위한 세레블론 결합제
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
CN119569702A (zh) 2018-04-04 2025-03-07 阿尔维纳斯运营股份有限公司 蛋白水解调节剂及相关使用方法
US12226424B2 (en) 2018-04-09 2025-02-18 Shanghaitech University Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates
EP3774772A1 (en) * 2018-04-13 2021-02-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
FI3784663T3 (fi) 2018-04-23 2023-10-06 Celgene Corp Substituoituja 4-aminoisoindoliini-1,3-dioniyhdisteitä ja niiden käyttö lymfooman hoitamiseksi
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
CU20210002A7 (es) * 2018-07-10 2021-08-06 Novartis Ag Derivados de 3-(5-hidroxi-1-oxoisoindolin-2-il)piperidina-2,6-diona y su uso en el tratamiento de trastornos dependientes de la proteína con dedos de zinc 2 de la familia ikaros (ikzf2)
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
CN112533898A (zh) 2018-07-31 2021-03-19 日商泛美克斯股份有限公司 杂环化合物
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
EP3846800A4 (en) 2018-09-04 2022-08-24 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
AU2019384807A1 (en) * 2018-11-21 2021-05-20 Accutar Biotechnology Inc. Novel compounds having estrogen receptor alpha degradation activity and uses thereof
WO2020128972A1 (en) * 2018-12-20 2020-06-25 Novartis Ag Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
KR20210136973A (ko) * 2019-01-03 2021-11-17 더 리젠츠 오브 더 유니버시티 오브 미시간 에스트로겐 수용체 단백질 분해제
CN113874016A (zh) 2019-01-29 2021-12-31 福宏治疗公司 化合物及其用途
KR102876423B1 (ko) * 2019-02-07 2025-10-24 한국화학연구원 표적 단백질 ｅｅｄ 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 ｅｅｄ, ｅｚｈ2, 또는 ｐｒｃ2 관련 질환의 예방 또는 치료용 약학적 조성물
ES3032659T3 (en) * 2019-02-15 2025-07-23 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
BR112021015672A2 (pt) 2019-02-15 2021-10-05 Novartis Ag Derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona substituída e usos dos mesmos
US12582641B2 (en) 2019-02-25 2026-03-24 Shanghaitech University Sulfur-containing compound based on glutarimide skeleton and application thereof
ES2995214T3 (en) 2019-03-06 2025-02-07 C4 Therapeutics Inc Heterocyclic compounds for medical treatment
CA3133314A1 (en) 2019-03-21 2020-09-24 Codiak Biosciences, Inc. Extracellular vesicle conjugates and uses thereof
US12233356B2 (en) 2019-03-21 2025-02-25 Lonza Sales Ag Process for preparing extracellular vesicles
TW202102497A (zh) 2019-03-29 2021-01-16 瑞典商阿斯特捷利康公司 化合物及它們在治療癌症中之用途
US12414995B2 (en) 2019-04-16 2025-09-16 Northwestern University Bifunctional compounds comprising Apcin-A and their use in the treatment of cancer
US12331061B2 (en) 2019-04-18 2025-06-17 Accutar Biotechnology Inc. Compounds having BET, estrogen receptor, and androgen receptor degradation activity and uses thereof
JP2022533147A (ja) * 2019-05-17 2022-07-21 ヒノバ ファーマシューティカルズ インコーポレイテッド 芳香族アミン類のａｒ及びｂｅｔを標的とするタンパク質分解キメラ化合物及び使用
WO2021011913A1 (en) 2019-07-17 2021-01-21 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021018118A1 (en) * 2019-07-29 2021-02-04 Janssen Pharmaceutica Nv Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 1 proteins
WO2021022163A2 (en) 2019-07-31 2021-02-04 Foghorn Therapeutics Inc. Compounds and uses thereof
CN112321566B (zh) 2019-08-05 2022-06-10 上海科技大学 Egfr蛋白降解剂及其抗肿瘤应用
ES3061133T3 (en) * 2019-08-26 2026-03-31 Arvinas Operations Inc Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
US10836749B1 (en) * 2019-09-23 2020-11-17 Accutar Biotechnology Inc. Substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
CN118930604A (zh) * 2019-09-29 2024-11-12 江西济民可信集团有限公司 作为蛋白降解剂杂环类化合物及包含其的药物组合物和应用
US12310975B2 (en) 2019-10-17 2025-05-27 Arvinas Operations, Inc. Modulators of BCL6 proteolysis and associated methods of use
KR20220103753A (ko) 2019-11-19 2022-07-22 브리스톨-마이어스 스큅 컴퍼니 헬리오스 단백질의 억제제로서 유용한 화합물
CN114761004A (zh) * 2019-12-06 2022-07-15 细胞基因公司 用于制备2-(4-氯苯基)-n-((2-(2，6-二氧代哌啶-3-基)-1-氧代异吲哚啉-5-基)甲基)-2，2-二氟乙酰胺的方法
EP4420728A3 (en) * 2019-12-12 2024-10-30 Accutar Biotechnology Inc. Novel chroman derivatives having estrogen receptor degradation activity and uses thereof
WO2021126974A1 (en) * 2019-12-17 2021-06-24 Orionis Biosciences, Inc. Bifunctional agents for protein recruitment and/or degradation
US20230111853A1 (en) * 2019-12-17 2023-04-13 Orionis Biosciences, Inc. Compounds modulating protein recruitment and/or degradation
ES2980575T3 (es) 2019-12-18 2024-10-02 Novartis Ag Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y usos de los mismos
EP4077309A1 (en) 2019-12-19 2022-10-26 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2021133886A1 (en) * 2019-12-23 2021-07-01 Accutar Biotechnology Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer
WO2021141662A1 (en) * 2020-01-10 2021-07-15 Massachusetts Institute Of Technology Proteolysis targeting chimeric molecules (protacs) with functional handles and uses thereof
US12528825B2 (en) 2020-01-29 2026-01-20 Foghorn Therapeutics Inc. Compounds and uses thereof
KR20220133259A (ko) * 2020-01-29 2022-10-04 포그혼 쎄라퓨틱스 인크. 화합물 및 이의 용도
CN113372327B (zh) * 2020-02-25 2023-07-18 上海科技大学 基于戊二酰亚胺骨架的化合物及其应用
IL295709A (en) 2020-03-05 2022-10-01 C4 Therapeutics Inc Compounds for targeted degradation of brd9
TW202140441A (zh) 2020-03-23 2021-11-01 美商必治妥美雅史谷比公司 經取代之側氧基異吲哚啉化合物
CN111393409A (zh) * 2020-03-27 2020-07-10 苏州昊帆生物股份有限公司 蛋白降解靶向嵌合体化合物、应用及其制备方法
EP4132655A1 (en) * 2020-04-06 2023-02-15 Arvinas Operations, Inc. Compounds and methods for targeted degradation of kras
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
CA3173629A1 (en) 2020-06-19 2021-12-13 Cosimo Dolente Braf degraders
US12415799B2 (en) * 2020-06-28 2025-09-16 Zhejiang Yangli Pharmaceutical Technology Co., Ltd. Indazole-fused cyclic compound
EP4192458A4 (en) 2020-08-05 2024-09-04 C4 Therapeutics, Inc. COMPOUNDS FOR TARGETED DEGRADATION OF RET
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
AU2021342287A1 (en) * 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
CN112094275A (zh) * 2020-09-16 2020-12-18 迪嘉药业集团有限公司 一种（右）佐匹克隆光降解杂质的制备方法
US20240241020A1 (en) 2020-09-23 2024-07-18 Lonza Sales Ag Process for preparing extracellular vesicles
JP2023549341A (ja) 2020-11-06 2023-11-24 プレリュード・セラピューティクス・インコーポレイテッド Ｂｒｍ標的化化合物及び関連する使用方法
US20240058318A1 (en) * 2020-12-10 2024-02-22 Mayo Foundation For Medical Education And Research Degrading pkcb1 to treat cancer
AU2021401580A1 (en) * 2020-12-14 2023-06-22 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
JP2024504932A (ja) 2021-01-13 2024-02-02 モンテ ローザ セラピューティクス， インコーポレイテッド イソインドリノン化合物
WO2022161166A1 (zh) * 2021-01-28 2022-08-04 江苏亚虹医药科技股份有限公司 靶向嵌合化合物、含其的药物组合物及其制备方法和用途
EP4289841A4 (en) * 2021-02-04 2025-02-19 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Benzo seven-membered ring bifunctional compound and application thereof
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
BR112023019967A2 (pt) * 2021-03-29 2023-11-14 Jiangsu Hengrui Pharmaceuticals Co Ltd Composto de tetra-hidronaftaleno e método de preparação para o mesmo e uso do mesmo em medicina
JP2024515545A (ja) 2021-04-05 2024-04-10 ブリストル－マイヤーズ スクイブ カンパニー がん治療のためのピリジニル置換オキソイソインドリン化合物
PT4320112T (pt) 2021-04-06 2025-07-07 Bristol Myers Squibb Co Compostos de oxoisoindolina substituídos por piridinilo
CA3214806A1 (en) 2021-04-16 2022-10-20 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
CA3217892A1 (en) * 2021-05-03 2022-11-10 Joel Mcintosh Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use
BR112023023065A2 (pt) 2021-05-05 2024-01-30 Biogen Ma Inc Compostos para direcionar a degradação da tirosina quinase de bruton
CR20230614A (es) * 2021-06-03 2024-02-01 Novartis Ag Derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona y sus usos médicos
JP2024525580A (ja) 2021-07-07 2024-07-12 バイオジェン・エムエイ・インコーポレイテッド Ｉｒａｋ４タンパク質の分解をターゲティングするための化合物
KR20240035526A (ko) 2021-07-07 2024-03-15 바이오젠 엠에이 인코포레이티드 Irak4 단백질의 분해를 표적하는 화합물
JP2024527934A (ja) * 2021-07-26 2024-07-26 アルビナス・オペレーションズ・インコーポレイテッド 二官能性化合物を製造する方法
KR20240110576A (ko) * 2021-10-22 2024-07-15 글루탁스 테라퓨틱스 (상하이) 씨오., 엘티디. Crbn e3 리가제 리간드 화합물, 리간드 화합물에 기초하여 개발된 단백질 분해제 및 이들의 응용
JP2024543405A (ja) 2021-11-09 2024-11-21 ハンジョウ グルバイオ ファーマシューティカル カンパニー リミテッド Ｗｅｅ１プロテインキナーゼ分解剤及びその使用
CA3237577A1 (en) 2021-12-22 2023-06-29 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
EP4455133A4 (en) * 2021-12-24 2026-04-15 Suzhou Kintor Pharmaceuticals Inc MULTI-PROTEIN DEGRADING AGENT WITH AN IMIDE SKELETON
MX2024008060A (es) 2021-12-30 2024-07-10 Beigene Switzerland Gmbh Degradacion de la tirosina quinasa de bruton (btk) mediante conjugacion de inhibidores de la btk con ligando de ligasa e3 y metodos de uso.
CN114085213B (zh) * 2022-01-20 2022-03-25 苏州国匡医药科技有限公司 一种arv-471的制备方法
EP4493554A1 (en) 2022-03-17 2025-01-22 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
AU2023239642A1 (en) 2022-03-25 2024-11-07 Shenzhen Pharmacin Co., Ltd. Pharmaceutical compositions of protac compounds and uses thereof
TW202404643A (zh) 2022-04-20 2024-02-01 大陸商同宜醫藥（蘇州）有限公司 化合物及用途
CA3249074A1 (en) 2022-06-06 2023-12-14 C4 Therapeutics, Inc. BICYCLIC SUBSTITUTION GLUTARIMIDE CEREBLON BINDERS
CN117229286A (zh) * 2022-06-14 2023-12-15 海创药业股份有限公司 一种芳香类化合物及其制备方法及在制备雌激素受体降解剂中的用途
WO2023242598A1 (en) * 2022-06-16 2023-12-21 Amphista Therapeutics Limited Bifunctional molecules for targeted protein degradation
WO2024006776A1 (en) * 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and medical use thereof
AU2023298115A1 (en) * 2022-06-27 2025-01-16 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and use thereof
WO2024006881A1 (en) * 2022-06-30 2024-01-04 Bristol-Myers Squibb Company Wee1 degrading compounds and uses thereof
WO2024015412A1 (en) * 2022-07-12 2024-01-18 Regents Of The University Of Michigan Tetrahydronaphthalene derivatives as estrogen receptor degraders
TW202416992A (zh) 2022-08-31 2024-05-01 美商亞文納營運公司 雌激素受體降解劑之給藥方案
EP4580631A1 (en) 2022-08-31 2025-07-09 Arvinas Operations, Inc. Dosage regimens of estrogen receptor degraders
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
JP2025531869A (ja) * 2022-09-09 2025-09-25 イノヴォ セラピューティクス、インコーポレイテッド ＣＫ１αおよびＤＵＡＬ ＣＫ１α／ＧＳＰＴ１分解化合物
WO2024073507A1 (en) 2022-09-28 2024-04-04 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
CN120035586A (zh) * 2022-09-29 2025-05-23 江苏恒瑞医药股份有限公司 一种四氢萘类衍生物的可药用盐、晶型及制备方法
CN120051280A (zh) 2022-10-17 2025-05-27 阿斯利康(瑞典)有限公司 用于治疗癌症的serd的组合
US20240180893A1 (en) 2022-11-17 2024-06-06 Astrazeneca Ab Methods of treatment of breast cancer
KR102794861B1 (ko) * 2022-11-25 2025-04-11 재단법인 대구경북첨단의료산업진흥재단 선택적 에스트로겐 수용체 조절제로서의 신규 화합물
EP4626430A1 (en) 2022-12-02 2025-10-08 Arvinas Operations, Inc. Method of treating breast cancer
CN116751186B (zh) * 2022-12-23 2024-10-18 南京知和医药科技有限公司 一种雌激素受体调节剂的制备及其用途
CN118556048A (zh) * 2022-12-27 2024-08-27 标新生物医药科技(上海)有限公司 基于硫/氧取代戊二酰亚胺基异吲哚啉酮骨架的化合物及其应用
CN118271284A (zh) * 2022-12-30 2024-07-02 江苏威凯尔医药科技有限公司 雌激素受体调节剂及其用途
CN121419983A (zh) 2023-01-26 2026-01-27 阿尔维纳斯运营股份有限公司 基于小脑蛋白的kras降解protac及其相关用途
WO2024167904A1 (en) 2023-02-07 2024-08-15 Arvinas Operations, Inc. Dosage regimens of estrogen receptor degraders in combination with an mtor inhibitor
WO2024206147A1 (en) 2023-03-24 2024-10-03 Arvinas Operations, Inc. Dosage regimens of estrogen receptor degraders
KR20260010420A (ko) 2023-05-11 2026-01-20 아스트라제네카 아베 암 치료를 위한 parp1 억제제 및 선택적 에스트로겐 분해제의 병용
CN121368483A (zh) 2023-06-02 2026-01-20 辉瑞公司 雌激素受体降解剂与cdk4抑制剂的组合
WO2024249875A1 (en) 2023-06-02 2024-12-05 Arvinas Operations, Inc. Combinations of estrogen receptor degraders and akt inhibitors
EP4724045A1 (en) 2023-06-12 2026-04-15 Arvinas Operations, Inc. Solid oral dosage forms of estrogen receptor degraders
WO2025006569A1 (en) 2023-06-27 2025-01-02 Arvinas Operations, Inc. Combinations of estrogen receptor degraders and cdk7 inhibitors for the treatment of cancer
WO2025038481A1 (en) 2023-08-11 2025-02-20 Arvinas Operations, Inc. Vepdegestrant dosage regimen in cyp3a-inducer treatment in cancer
WO2025090847A1 (en) * 2023-10-25 2025-05-01 Bpgbio, Inc. Estrogen receptor degraders and their use in the treatment of cancer
WO2025114875A1 (en) 2023-12-01 2025-06-05 Astrazeneca Ab Er degraders and uses thereof
WO2025119380A1 (zh) * 2023-12-08 2025-06-12 江苏威凯尔医药科技股份有限公司 雌激素受体调节剂及其用途
WO2025193454A1 (en) 2024-03-01 2025-09-18 Prelude Therapeutics Incorporated Brm and brg1 targeting antibody-drug conjugates and methods of use thereof
US12558428B2 (en) 2024-03-08 2026-02-24 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and their use in treating disease
WO2025245032A1 (en) 2024-05-20 2025-11-27 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound
WO2026017799A1 (en) 2024-07-18 2026-01-22 Centre Hospitalier Universitaire Vaudois Substituted 3-cyanoquinolines for the prevention and treatment of sexually transmitted diseases
WO2026018182A1 (en) 2024-07-19 2026-01-22 Pfizer Inc. Process for preparing a cis-1,2-diaryltetralin derivative
WO2026044127A1 (en) 2024-08-22 2026-02-26 Arvinas Operations, Inc. Administration of cyp3a inhibitors in the treatment of cancer
US12624035B2 (en) 2024-09-06 2026-05-12 Amphista Therapeutics Limited Compounds for targeted protein degradation

Family Cites Families (152)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5510357A (en) 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
PT2177517E (pt) 1996-07-24 2011-11-10 Celgene Corp 2-(2,6-dioxopiperidin-3-il)-ftalimida amino-substituída para redução dos níveis de tnf-alfa
US5916916A (en) 1996-10-10 1999-06-29 Eli Lilly And Company 1-aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods
ZA982877B (en) 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
WO1998051702A1 (en) 1997-05-14 1998-11-19 Sloan-Kettering Institute For Cancer Research Methods and compositions for destruction of selected proteins
AU9493698A (en) 1997-09-23 1999-04-12 Eli Lilly And Company Benzothiophenes
ATE265853T1 (de) * 1998-06-16 2004-05-15 Pfizer Prod Inc Kombinationstherapeutika, enthaltend einen selektiven östrogenrezeptormodulator und prostaglandin e2
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
EP1176959B1 (en) 1999-05-05 2006-03-08 Merck & Co., Inc. Novel prolines as antimicrobial agents
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
EP1322750A4 (en) 2000-09-08 2004-09-29 California Inst Of Techn PROTEOLYSIS TARGET DRUG TARGET MEDICINE
US7091353B2 (en) 2000-12-27 2006-08-15 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
WO2002066512A1 (en) 2001-02-16 2002-08-29 E.I. Dupont De Nemours And Company Angiogenesis-inhibitory tripeptides, compositions and their methods of use
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
CN100384819C (zh) 2002-07-02 2008-04-30 诺瓦提斯公司 与细胞凋亡蛋白抑制剂结合的smac蛋白的肽抑制剂
WO2005007621A2 (en) 2003-05-30 2005-01-27 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
MXPA06008095A (es) 2004-01-16 2007-03-28 Univ Michigan Mimeticos de smac conformacionalmente restringidos y sus usos.
CA2558615C (en) 2004-03-23 2013-10-29 Genentech, Inc. Azabicyclo-octane inhibitors of iap
RS52545B (sr) 2004-04-07 2013-04-30 Novartis Ag Inhibitori protein apoptoze (iap)
CA2570321C (en) 2004-07-02 2013-10-08 Genentech, Inc. Inhibitors of iap
KR20120127754A (ko) 2004-12-20 2012-11-23 제넨테크, 인크. Ｉａｐ의 피롤리딘 억제제
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
DK1851200T3 (da) 2005-02-25 2014-04-14 Tetralogic Pharm Corp Dimere iap-inhibitorer
CN100383139C (zh) 2005-04-07 2008-04-23 天津和美生物技术有限公司 可抑制细胞释放肿瘤坏死因子的哌啶-2，6-二酮衍生物
WO2006113942A2 (en) 2005-04-20 2006-10-26 Schering Corporation Method of inhibiting cathepsin activity
ES2434946T3 (es) 2005-08-31 2013-12-18 Celgene Corporation Compuestos de isoindol imida y composiciones que los comprenden y métodos para usarlo
EP1994027A2 (en) 2006-03-03 2008-11-26 Novartis AG N-formyl hydroxylamine compounds
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
WO2007109604A2 (en) 2006-03-20 2007-09-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
HRP20141253T1 (en) 2006-05-05 2015-03-13 The Regents Of The Universitiy Of Michigan Intermediates for the preparation of bivalent smac mimetics
JP2009544620A (ja) 2006-07-20 2009-12-17 リガンド・ファーマシューティカルズ・インコーポレイテッド 自己免疫疾患及び炎症のためのプロリン尿素ｃｃｒ１アンタゴニスト
US20100056495A1 (en) 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
NZ575061A (en) 2006-08-30 2011-10-28 Celgene Corp 5-substituted isoindoline compounds
ES2403546T3 (es) 2006-11-03 2013-05-20 Pharmacyclics, Inc. Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización
WO2008109057A1 (en) 2007-03-02 2008-09-12 Dana-Farber Cancer Institute, Inc. Organic compounds and their uses
WO2008128121A1 (en) 2007-04-12 2008-10-23 Joyant Pharmaceuticals, Inc. Smac mimetic dimers and trimers useful as anti-cancer agents
HRP20140885T1 (hr) 2007-04-13 2014-11-21 The Regents Of The University Of Michigan Diazo bicikliäśki smac mimetici i njihove primjene
NZ598890A (en) 2007-04-30 2013-10-25 Genentech Inc Inhibitors of iap
WO2008144925A1 (en) 2007-05-30 2008-12-04 Aegera Therapeutics Inc. Iap bir domain binding compounds
BRPI0811065A2 (pt) * 2007-06-08 2014-12-02 Abbott Lab Indazóis 5-heteroaril substituídos como inibidores de quinase
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
CN101808693A (zh) 2007-07-25 2010-08-18 百时美施贵宝公司 三嗪激酶抑制剂
ES2534899T3 (es) 2007-08-06 2015-04-30 Janssen Pharmaceutica, N.V. Fenilendiaminas sustituidas como inhibidores de la interacción entre MDM2 y p53
EP2058312A1 (en) 2007-11-09 2009-05-13 Universita' degli Studi di Milano SMAC mimetic compounds as apoptosis inducers
EP2358697B1 (en) 2008-10-29 2015-10-21 Celgene Corporation Isoindoline compounds for use in the treatment of cancer.
DK2376480T3 (en) 2008-12-05 2016-09-12 Abbvie Inc Sulfonamide derivatives AS BCL-2-selective apoptosis inducing agents for the treatment of cancer and immune diseases
ES2443948T3 (es) * 2008-12-19 2014-02-21 Bristol-Myers Squibb Company Compuestos de carbazol carboxamida útiles como inhibidores de quinasas
US8063102B2 (en) * 2009-03-13 2011-11-22 N.V. Organon Tetrahydronaphthalen-2-ol derivatives
WO2010107485A1 (en) 2009-03-17 2010-09-23 The Trustees Of Columbia University In The City Of New York E3 ligase inhibitors
CA2929347A1 (en) 2009-05-26 2010-12-02 Milan Bruncko (hetero)aryl substituted sulfonyl-2-(1h-pyrrolo[2,3-b]pyridine-5-oxy)benzamide compounds and their use as apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
US8614201B2 (en) 2009-06-05 2013-12-24 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of TRPA1
BR112012000867A2 (pt) 2009-07-13 2019-09-24 Harvard College "polipeptídeos bifuncional costurado e uso do mesmo"
CA2789879A1 (en) 2009-10-28 2011-05-19 Joyant Pharmaceuticals, Inc. Dimeric smac mimetics
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
SG10201501062SA (en) 2010-02-11 2015-04-29 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
EP2588129A4 (en) 2010-06-30 2014-07-09 Univ Brandeis ON SMALL MOLECULES TARGETED PROTEIN REMOVAL
WO2012040527A2 (en) 2010-09-24 2012-03-29 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
CN102477033A (zh) 2010-11-23 2012-05-30 苏州波锐生物医药科技有限公司 苯并噻酚类化合物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途
CN102477017A (zh) * 2010-11-23 2012-05-30 苏州波锐生物医药科技有限公司 四氢萘衍生物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途
AU2011338615B2 (en) 2010-12-07 2017-07-27 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
US20140243282A1 (en) 2010-12-31 2014-08-28 Satish Reddy Kallam Methods and compositions for designing novel conjugate therapeutics
US8889684B2 (en) 2011-02-02 2014-11-18 Boehringer Ingelheim International Gmbh Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors
EP3096142A3 (en) 2011-04-29 2017-03-08 Celgene Corporation Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
AU2012316055B2 (en) 2011-09-27 2016-05-12 Amgen Inc. Heterocyclic compounds as MDM2 inhibitors for the treatment of cancer
JP2015504425A (ja) 2011-11-09 2015-02-12 アンサンブル・セラピューティクス アポトーシスのインヒビターを阻害するための大環状化合物
WO2013071039A1 (en) 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
CN103159736B (zh) 2011-12-10 2015-05-13 通化济达医药有限公司 取代的吡唑激酶抑制剂
RS55196B1 (sr) 2011-12-31 2017-01-31 Beigene Ltd Fuzionisana triciklična jedinjenja kao inhibitori raf kinaze
JP2015508414A (ja) 2012-01-12 2015-03-19 イエール ユニバーシティ Ｅ３ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
WO2013169858A1 (en) 2012-05-08 2013-11-14 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
US20150119435A1 (en) 2012-05-11 2015-04-30 Yale University Compounds useful for promoting protein degradation and methods using same
JP6171003B2 (ja) 2012-05-24 2017-07-26 ノバルティス アーゲー ピロロピロリジノン化合物
SG11201406889WA (en) 2012-05-30 2015-02-27 Hoffmann La Roche Substituted pyrrolidine-2-carboxamides
WO2014011712A1 (en) 2012-07-10 2014-01-16 Bristol-Myers Squibb Company Iap antagonists
HUE045880T2 (hu) 2012-07-31 2020-01-28 Novartis Ag A humán double minute 2 (MDM2) inhibitorra való érzékenységgel összefüggõ markerek
EP2882740B1 (en) 2012-08-09 2017-03-01 Bristol-Myers Squibb Company Iap antagonists
TR201904785T4 (tr) 2012-08-09 2019-05-21 Celgene Corp (S)-3-(4-((4-MORFOLINOMETİL)BENZİL)OKSİ)-1-OKSOİZOİNDOLİN-2-il)PİPERİDİN-2,6-DİON HİDROKLORİDİN BİR KATI FORMU.
TWI586668B (zh) 2012-09-06 2017-06-11 第一三共股份有限公司 二螺吡咯啶衍生物之結晶
WO2014047024A1 (en) 2012-09-18 2014-03-27 Bristol-Myers Squibb Company Iap antagonists
US9603889B2 (en) 2012-10-02 2017-03-28 Bristol-Myers Squibb Company IAP antagonists
US20140135270A1 (en) 2012-11-09 2014-05-15 Ensemble Therapeutics Corp. Macrocyclic compounds for inhibition of inhibitors of apoptosis
WO2014100071A2 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted pyrrolopyrimidines as hdm2 inhibitors
EP2935263B1 (en) 2012-12-20 2018-12-05 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
EP2752191A1 (en) 2013-01-07 2014-07-09 Sanofi Compositions and methods using hdm2 antagonist and mek inhibitor
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
NL2011274C2 (en) 2013-08-06 2015-02-09 Illumicare Ip B V 51 Groundbreaking platform technology for specific binding to necrotic cells.
CA2902856C (en) 2013-02-28 2021-02-16 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
WO2014151863A1 (en) 2013-03-14 2014-09-25 Amgen Inc. Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
EP3019517A1 (en) 2013-07-12 2016-05-18 Bristol-Myers Squibb Company Iap antagonists
WO2015092420A1 (en) 2013-12-20 2015-06-25 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
AU2015228859A1 (en) * 2014-03-13 2016-07-07 F. Hoffmann-La Roche Ag Therapeutic combinations with estrogen receptor modulators
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN119591582A (zh) 2014-04-14 2025-03-11 阿尔维纳斯运营股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
US20160022642A1 (en) 2014-07-25 2016-01-28 Yale University Compounds Useful for Promoting Protein Degradation and Methods Using Same
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
CN113603736A (zh) 2014-10-03 2021-11-05 康纳根有限公司 无热量甜味剂及合成方法
CN107406424B (zh) * 2014-12-18 2020-08-25 豪夫迈·罗氏有限公司 雌激素受体调节剂及其用途
JP6815318B2 (ja) 2014-12-23 2021-01-20 ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド 二官能性分子によって標的化タンパク質分解を誘導する方法
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
HK1245791A1 (zh) 2015-01-20 2018-08-31 阿尔维纳斯运营股份有限公司 用於雄激素受体的靶向降解的化合物和方法
IL315294A (en) * 2015-03-03 2024-10-01 Pharmacyclics Llc Pharmaceutical formulations of bruton's tyrosine kinase inhibitor
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
JP7269731B2 (ja) 2015-03-18 2023-05-09 アルビナス・オペレーションズ・インコーポレイテッド 標的タンパク質の分解向上のための化合物および方法
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
CN108137507A (zh) 2015-07-10 2018-06-08 阿尔维纳斯股份有限公司 基于mdm2的蛋白水解调节剂和相关的使用方法
CA2988436A1 (en) 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
AU2016301196B2 (en) 2015-08-06 2022-09-08 Dana-Farber Cancer Institute, Inc. Tunable endogenous protein degradation
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
GB201516243D0 (en) 2015-09-14 2015-10-28 Glaxosmithkline Ip Dev Ltd Novel compounds
AU2016349781A1 (en) 2015-11-02 2018-05-10 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same
AU2017235450A1 (en) 2016-03-15 2018-08-16 Merrimack Pharmaceuticals, Inc. Methods for treating ER+, HER2-, HRG+ breast cancer using combination therapies comprising an anti-ErbB3 antibody
CA3017740A1 (en) 2016-03-16 2017-09-21 Pearlie BURNETTE Small molecules against cereblon to enhance effector t cell function
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
JP7037500B2 (ja) * 2016-04-06 2022-03-16 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｍｄｍ２タンパク質分解剤
EP3892272B1 (en) 2016-04-22 2024-07-24 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
WO2017214014A1 (en) 2016-06-06 2017-12-14 Celgene Corporation Treatment of a hematologic malignancy with 2-(4-chlorophenyl)-n-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
ES2975558T3 (es) 2016-09-15 2024-07-09 Arvinas Inc Derivados de indol como degradantes de receptor de estrógeno
LT3660004T (lt) 2016-10-11 2023-06-12 Arvinas Operations, Inc. Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai
EP3535265A4 (en) 2016-11-01 2020-07-08 Arvinas, Inc. PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE
WO2018098280A1 (en) 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use
WO2018102725A1 (en) 2016-12-01 2018-06-07 Arvinas, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
RU2019121527A (ru) 2016-12-23 2021-01-15 Эрвинэс Оперейшнс, Инк. Химерные молекулы, нацеливающиеся на протеолиз egfr, и связанные с ними способы применения
EP3558994A4 (en) 2016-12-23 2021-05-12 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF FAST ACCELERATED FIBROSARCOMA POLYPEPTIDES
EP3559006A4 (en) 2016-12-23 2021-03-03 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF F TAL LIVER KINASE POLYPEPTIDES
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
MX2019008934A (es) 2017-01-26 2019-11-05 Arvinas Operations Inc Moduladores de la proteolisis del receptor de estrogeno y métodos asociados de uso,.
EP3577109A4 (en) 2017-01-31 2020-11-18 Arvinas Operations, Inc. CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM
JP7366031B2 (ja) 2017-09-22 2023-10-20 カイメラ セラピューティクス， インコーポレイテッド タンパク質分解剤およびそれらの使用
CA3121930A1 (en) 2018-12-06 2020-06-11 Radius Pharmaceuticals, Inc. Methods for treating cancer resistant to cdk4/6 inhibitors
ES3061133T3 (en) 2019-08-26 2026-03-31 Arvinas Operations Inc Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
US10836749B1 (en) 2019-09-23 2020-11-17 Accutar Biotechnology Inc. Substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
EP4420728A3 (en) 2019-12-12 2024-10-30 Accutar Biotechnology Inc. Novel chroman derivatives having estrogen receptor degradation activity and uses thereof
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
AU2021401580A1 (en) 2020-12-14 2023-06-22 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
JP2024527934A (ja) 2021-07-26 2024-07-26 アルビナス・オペレーションズ・インコーポレイテッド 二官能性化合物を製造する方法
CN113816927B (zh) 2021-11-23 2022-02-25 苏州国匡医药科技有限公司 一种arv-471中间体的制备方法

Also Published As

Publication number Publication date
KR102173464B1 (ko) 2020-11-04
PT3689868T (pt) 2024-01-02
BR112019011200A2 (pt) 2019-10-08
US20220388984A1 (en) 2022-12-08
MX2022010583A (es) 2022-12-13
MX2019006402A (es) 2019-09-11
IL266842A (en) 2019-07-31
CO2019007091A2 (es) 2019-10-09
JP2021169479A (ja) 2021-10-28
IL266842B (en) 2022-09-01
JP2023021211A (ja) 2023-02-10
SI3689868T1 (sl) 2024-02-29
JP7160497B2 (ja) 2022-10-25
KR102173464B9 (ko) 2022-05-23
JP7611885B2 (ja) 2025-01-10
US10899742B1 (en) 2021-01-26
US20220274955A1 (en) 2022-09-01
JP2022023103A (ja) 2022-02-07
CN114656452B (zh) 2023-01-17
CN110291087B (zh) 2024-07-09
AU2020201793A1 (en) 2020-03-26
US12172981B2 (en) 2024-12-24
CN111454248A (zh) 2020-07-28
US20250320195A1 (en) 2025-10-16
AU2021204549B2 (en) 2023-07-06
RU2020106142A3 (enExample) 2020-08-07
JP2025143400A (ja) 2025-10-01
RU2019120120A3 (enExample) 2021-03-24
HUE064609T2 (hu) 2024-04-28
US11104666B2 (en) 2021-08-31
HRP20231537T1 (hr) 2024-03-15
AU2020201793B2 (en) 2020-08-27
AU2017366693B2 (en) 2021-04-01
IL297717A (en) 2022-12-01
RU2020106142A (ru) 2020-04-13
AU2021204549A1 (en) 2021-08-05
LT3689868T (lt) 2023-12-27
US20210139458A1 (en) 2021-05-13
US20180155322A1 (en) 2018-06-07
US10647698B2 (en) 2020-05-12
KR20190082989A (ko) 2019-07-10
AU2021257895A1 (en) 2021-11-18
CA3042968A1 (en) 2018-06-07
AU2017366693A1 (en) 2019-04-18
CN114656452A (zh) 2022-06-24
AU2024201437A1 (en) 2024-03-21
CN110291087A (zh) 2019-09-27
CN118834201A (zh) 2024-10-25
JP7708960B2 (ja) 2025-07-15
KR102674902B1 (ko) 2024-06-14
RU2019120120A (ru) 2020-12-28
ES2967404T3 (es) 2024-04-30
CA3042968C (en) 2023-10-17
AU2017366693A9 (en) 2019-05-02
EP3548483A4 (en) 2020-06-10
IL316544A (en) 2024-12-01
US20240076281A1 (en) 2024-03-07
RU2750484C2 (ru) 2021-06-28
WO2018102725A1 (en) 2018-06-07
PL3689868T3 (pl) 2024-03-11
BR112019011200B1 (pt) 2021-12-28
KR20200020988A (ko) 2020-02-26
IL272527A (en) 2020-03-31
IL284424A (en) 2021-07-29
KR20240063185A (ko) 2024-05-10
JP2020100659A (ja) 2020-07-02
DK3689868T3 (da) 2024-01-02
FI3689868T3 (fi) 2023-12-18
SMT202300483T1 (it) 2024-01-10
EP3689868B1 (en) 2023-09-27
JP6957620B2 (ja) 2021-11-02
JP6972211B2 (ja) 2021-11-24
IL284424B (en) 2022-12-01
IL284424B2 (en) 2023-04-01
EP3689868A1 (en) 2020-08-05
EP3548483A1 (en) 2019-10-09
IL272527B (en) 2021-07-29
JP2020504089A (ja) 2020-02-06
JP2025060813A (ja) 2025-04-10
US11597720B2 (en) 2023-03-07

Similar Documents

Publication Publication Date Title
US12172981B2 (en) Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
US12275716B2 (en) Modulators of estrogen receptor proteolysis and associated methods of use
JP2020504089A5 (enExample)
HK40023198B (en) Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
RU2797244C2 (ru) Производные тетрагидронафталина и тетрагидроизохинолина в качестве разрушителей эстрогенового рецептора
HK40023198A (en) Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders