KR102674902B1 - 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 - Google Patents

에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 Download PDF

Info

Publication number
KR102674902B1
KR102674902B1 KR1020197019065A KR20197019065A KR102674902B1 KR 102674902 B1 KR102674902 B1 KR 102674902B1 KR 1020197019065 A KR1020197019065 A KR 1020197019065A KR 20197019065 A KR20197019065 A KR 20197019065A KR 102674902 B1 KR102674902 B1 KR 102674902B1
Authority
KR
South Korea
Prior art keywords
alkyl
substituted
optionally substituted
group
formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
KR1020197019065A
Other languages
English (en)
Korean (ko)
Other versions
KR20190082989A (ko
Inventor
앤드류 피. 크루
이민 치안
한칭 동
징 왕
키이스 알. 혼버거
Original Assignee
아비나스 오퍼레이션스, 인코포레이티드
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 아비나스 오퍼레이션스, 인코포레이티드 filed Critical 아비나스 오퍼레이션스, 인코포레이티드
Priority to KR1020207004766A priority Critical patent/KR102173464B1/ko
Priority to KR1020247014021A priority patent/KR20240063185A/ko
Publication of KR20190082989A publication Critical patent/KR20190082989A/ko
Application granted granted Critical
Publication of KR102674902B1 publication Critical patent/KR102674902B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Molecular Biology (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)
  • Peptides Or Proteins (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020197019065A 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 Active KR102674902B1 (ko)

Priority Applications (2)

Application Number Priority Date Filing Date Title
KR1020207004766A KR102173464B1 (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
KR1020247014021A KR20240063185A (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662429041P 2016-12-01 2016-12-01
US62/429,041 2016-12-01
US201762540049P 2017-08-01 2017-08-01
US62/540,049 2017-08-01
PCT/US2017/064283 WO2018102725A1 (en) 2016-12-01 2017-12-01 Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders

Related Child Applications (2)

Application Number Title Priority Date Filing Date
KR1020247014021A Division KR20240063185A (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
KR1020207004766A Division KR102173464B1 (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체

Publications (2)

Publication Number Publication Date
KR20190082989A KR20190082989A (ko) 2019-07-10
KR102674902B1 true KR102674902B1 (ko) 2024-06-14

Family

ID=62240410

Family Applications (3)

Application Number Title Priority Date Filing Date
KR1020247014021A Pending KR20240063185A (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
KR1020197019065A Active KR102674902B1 (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
KR1020207004766A Active KR102173464B1 (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체

Family Applications Before (1)

Application Number Title Priority Date Filing Date
KR1020247014021A Pending KR20240063185A (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020207004766A Active KR102173464B1 (ko) 2016-12-01 2017-12-01 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체

Country Status (24)

Country Link
US (7) US10647698B2 (enExample)
EP (2) EP3689868B1 (enExample)
JP (7) JP6957620B2 (enExample)
KR (3) KR20240063185A (enExample)
CN (4) CN114656452B (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) IL266842B (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 (140)

* 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
KR102564925B1 (ko) 2015-01-20 2023-08-07 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법
EP3302482A4 (en) 2015-06-05 2018-12-19 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
US10683387B2 (en) 2016-10-04 2020-06-16 Massachusetts Institute Of Technology Bottlebrush copolymers and uses thereof
CA3042260C (en) 2016-11-01 2023-10-03 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
RS64976B1 (sr) 2016-12-01 2024-01-31 Arvinas Operations Inc Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora
CN110741004B (zh) 2016-12-23 2023-10-17 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
JP2020505327A (ja) 2016-12-23 2020-02-20 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法
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
AU2018211975B2 (en) 2017-01-26 2022-05-26 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
KR102747905B1 (ko) 2017-01-31 2024-12-31 아비나스 오퍼레이션스, 인코포레이티드 세레블론 리간드 및 이를 포함하는 이작용성 화합물
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
WO2019043214A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag glutarimide
EP3679027A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Dihydrobenzimidazolones
WO2019099868A2 (en) 2017-11-16 2019-05-23 C4 Therapeutics, Inc. Degraders and degrons for targeted protein degradation
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
EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE-BASED PROTEOLYSIS MODULATORS AND RELATED METHODS OF USE
WO2019191112A1 (en) 2018-03-26 2019-10-03 C4 Therapeutics, Inc. Cereblon binders for the degradation of ikaros
BR112020020307A2 (pt) 2018-04-04 2021-01-12 Arvinas Operations, Inc. Moduladores de proteólise e métodos de uso associados
AU2019251151B2 (en) 2018-04-09 2022-07-07 Shanghaitech University Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates
WO2019199816A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
EP3781156A4 (en) 2018-04-16 2022-05-18 C4 Therapeutics, Inc. SPIROCYCLIC COMPOUNDS
CA3096404A1 (en) 2018-04-23 2019-10-31 Celgene Corporation Substituted 4-aminoisoindoline-1,3-dione compounds and their use for treating lymphoma
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
EP3820573B1 (en) 2018-07-10 2023-08-09 Novartis AG 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and their use in the treatment of ikaros family zinc finger 2 (ikzf2)-dependent diseases
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
EP3831811A4 (en) 2018-07-31 2022-04-20 Fimecs, Inc. HETEROCYCLIC COMPOUND
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
CA3120530A1 (en) 2018-11-21 2020-05-28 Accutar Biotechnology Inc. Novel compounds having estrogen receptor alpha degradation activity and uses thereof
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
US20240245670A1 (en) * 2018-12-20 2024-07-25 Novartis Ag Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
CN113614076A (zh) * 2019-01-03 2021-11-05 密执安大学评议会 雌激素受体蛋白降解剂
WO2020160192A1 (en) 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2020162725A1 (ko) * 2019-02-07 2020-08-13 한국화학연구원 표적 단백질 eed 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 eed, ezh2, 또는 prc2 관련 질환의 예방 또는 치료용 약학적 조성물
EP3924055B1 (en) 2019-02-15 2024-04-03 Novartis AG Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
EP3924054B1 (en) * 2019-02-15 2025-04-02 Novartis AG 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
US12233356B2 (en) 2019-03-21 2025-02-25 Lonza Sales Ag Process for preparing extracellular vesicles
CN113747925B (zh) 2019-03-21 2024-10-15 隆萨销售股份公司 胞外囊泡缀合物及其用途
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
WO2020214555A1 (en) 2019-04-16 2020-10-22 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
US20220257774A1 (en) * 2019-05-17 2022-08-18 Hinova Pharmaceuticals Inc. Aromatic amine ar ahd bet targeting protein degradation chimera compound and use
CN114867727B (zh) 2019-07-17 2025-02-21 阿尔维纳斯运营股份有限公司 Tau蛋白靶向化合物及相关使用方法
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
CN114667147B (zh) 2019-08-26 2024-09-06 阿尔维纳斯运营股份有限公司 用四氢萘衍生物作为雌激素受体降解剂的治疗乳腺癌的方法
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
EP4045496A1 (en) 2019-10-17 2022-08-24 Arvinas Operations, Inc. Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety
KR20220103753A (ko) 2019-11-19 2022-07-22 브리스톨-마이어스 스큅 컴퍼니 헬리오스 단백질의 억제제로서 유용한 화합물
IL293481A (en) * 2019-12-06 2022-08-01 Celgene Corp Processes for preparing 2-(4-chlorophenyl)-n-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide
CA3164202A1 (en) * 2019-12-12 2021-06-17 Accutar Biotechnology Inc. Novel chroman derivatives having estrogen receptor degradation activity and uses thereof
EP4076530A4 (en) * 2019-12-17 2024-04-10 Orionis Biosciences, Inc. BIFUNCTIONAL AGENTS FOR RECRUITMENT AND/OR DEGRADATION OF PROTEINS
AU2020404956A1 (en) * 2019-12-17 2022-07-07 Orionis Biosciences, Inc. Compounds modulating protein recruitment and/or degradation
PE20230159A1 (es) 2019-12-18 2023-02-01 Novartis Ag Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y usos
PH12022551486A1 (en) 2019-12-19 2023-11-13 Arvinas Operations Inc Compounds and methods for the targeted degradation of androgen receptor
CA3161892A1 (en) * 2019-12-23 2021-07-01 Jie Fan Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer
US12042513B2 (en) * 2020-01-10 2024-07-23 Massachusetts Institute Of Technology Proteolysis targeting chimeric molecules (PROTACs) with functional handles and uses thereof
TWI877297B (zh) * 2020-01-29 2025-03-21 美商福宏治療公司 化合物及其用途
WO2021170021A1 (zh) * 2020-02-25 2021-09-02 上海科技大学 基于戊二酰亚胺骨架的化合物及其应用
CN115279370B (zh) 2020-03-05 2025-01-10 C4医药公司 用于brd9的靶向降解的化合物
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
JP2023521698A (ja) * 2020-04-06 2023-05-25 アルヴィナス・オペレーションズ・インコーポレイテッド Krasの標的化分解のための化合物及び方法
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
US12415799B2 (en) * 2020-06-28 2025-09-16 Zhejiang Yangli Pharmaceutical Technology Co., Ltd. Indazole-fused cyclic compound
WO2022032026A1 (en) 2020-08-05 2022-02-10 C4 Therapeutics, Inc. Compounds for targeted degradation of ret
US12180193B2 (en) 2020-08-28 2024-12-31 Arvinas Operations, Inc. Accelerating fibrosarcoma protein degrading compounds and associated methods of use
CR20230162A (es) * 2020-09-14 2023-06-02 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógenos
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
EP4259622A4 (en) * 2020-12-10 2024-11-13 Mayo Foundation for Medical Education and Research DEGRADATION OF PKCBBETA1 FOR THE TREATMENT OF CANCER
CA3202592A1 (en) * 2020-12-14 2022-06-23 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
EP4277901A1 (en) 2021-01-13 2023-11-22 Monte Rosa Therapeutics, Inc. Isoindolinone compounds
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
CN116867778A (zh) * 2021-02-04 2023-10-10 正大天晴药业集团股份有限公司 苯并七元环类双功能化合物及其应用
AU2022220869A1 (en) 2021-02-15 2023-08-24 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
US20250099596A1 (en) * 2021-03-29 2025-03-27 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Tetrahydronaphthalene compound, and preparation method therefor and use thereof in medicine
US20250346574A1 (en) 2021-04-05 2025-11-13 Bristol-Myers Squibb Company Pyridinyl substituted oxoisoindoline compounds for the treatment of cancer
AU2022253242A1 (en) 2021-04-06 2023-11-23 Bristol-Myers Squibb Company Pyridinyl substituted oxoisoindoline compounds
AU2022259683A1 (en) 2021-04-16 2023-10-19 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
IL308219A (en) 2021-05-05 2024-01-01 Biogen Ma Inc Compounds to Target Broton Tyrosine Kinase Degradation
AR126052A1 (es) 2021-06-03 2023-09-06 Novartis Ag Derivados de 3-(5-oxi)-1-oxoisoindolin-2-il)piperidina-2,6-diona y sus usos
IL309941A (en) 2021-07-07 2024-03-01 Biogen Ma Inc Compounds to target degradation of IRAK4 proteins
US20250018046A1 (en) 2021-07-07 2025-01-16 Biogen Ma Inc Compounds for targeting degradation of irak4 proteins
CN117715889A (zh) 2021-07-26 2024-03-15 阿尔维纳斯运营股份有限公司 制备双官能化合物的方法
CN116003418A (zh) * 2021-10-22 2023-04-25 标新生物医药科技(上海)有限公司 Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用
CA3237756A1 (en) 2021-11-09 2023-05-19 Hangzhou Glubio Pharmaceutical Co., Ltd. Wee1 protein kinase degradation agent and use thereof
JP2024545193A (ja) 2021-12-22 2024-12-05 ギリアード サイエンシーズ, インコーポレイテッド Ikarosジンクフィンガーファミリー分解剤及びその使用
WO2023116835A1 (zh) * 2021-12-24 2023-06-29 苏州开拓药业股份有限公司 一种具有酰亚胺骨架的多蛋白降解剂
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
US12358887B2 (en) 2022-03-17 2025-07-15 Gilead Sciences, Inc. IKAROS Zinc Finger Family degraders and uses thereof
TW202345842A (zh) 2022-03-25 2023-12-01 大陸商深圳市藥欣生物科技有限公司 Protac化合物之醫藥組合物及其用途
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
KR20250021314A (ko) 2022-06-06 2025-02-12 씨4 테라퓨틱스, 인코포레이티드 비시클릭-치환된 글루타르이미드 세레블론 결합제
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
JP2025521686A (ja) * 2022-06-27 2025-07-10 リレー セラピューティクス, インコーポレイテッド エストロゲン受容体アルファ分解剤及びその使用
PE20251398A1 (es) * 2022-06-30 2025-05-22 Bristol Myers Squibb Co Compuestos de degradacion de wee1 y usos de los mismos
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
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
AU2023338217A1 (en) * 2022-09-09 2025-04-03 Innovo Therapeutics, Inc. CK1α AND DUAL CK1α / GSPT1 DEGRADING COMPOUNDS
WO2024073507A1 (en) 2022-09-28 2024-04-04 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
EP4596538A4 (en) * 2022-09-29 2025-12-31 Jiangsu Hengrui Pharmaceuticals Co Ltd PHARMACEUTICALLY ACCEPTABLE SALT AND CRYSTALLINE FORM OF TETRAHYDRONAPHTALENE DERIVATIVE, AND PROCESS OF PREPARATION
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
CN120603593A (zh) 2022-12-02 2025-09-05 阿尔维纳斯运营股份有限公司 治疗乳腺癌的方法
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
WO2024140638A1 (zh) * 2022-12-27 2024-07-04 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
WO2024141052A1 (zh) * 2022-12-30 2024-07-04 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
EP4655073A2 (en) 2023-01-26 2025-12-03 Arvinas Operations, Inc. Cereblon-based kras degrading protacs ans uses related thereto
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
WO2024231548A1 (en) 2023-05-11 2024-11-14 Astrazeneca Ab Combination of a parp1 inhibitor and a selective estrogen degrader for treating cancer
WO2024246825A1 (en) 2023-06-02 2024-12-05 Pfizer Inc. Combinations of estrogen receptor degraders and cdk4 inhibitors
WO2024249875A1 (en) 2023-06-02 2024-12-05 Arvinas Operations, Inc. Combinations of estrogen receptor degraders and akt inhibitors
WO2024258856A1 (en) 2023-06-12 2024-12-19 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
US20250177539A1 (en) 2023-12-01 2025-06-05 Astrazeneca Ab Er degraders and uses thereof
CN120118067A (zh) * 2023-12-08 2025-06-10 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
WO2025245032A1 (en) 2024-05-20 2025-11-27 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160045607A1 (en) 2014-08-11 2016-02-18 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
US20160097071A1 (en) 2014-10-03 2016-04-07 Conagen Inc. Non-caloric sweeteners and methods for synthesizing
KR102173464B1 (ko) * 2016-12-01 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체

Family Cites Families (149)

* 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
CZ302378B6 (cs) 1996-07-24 2011-04-20 Celgene Corporation Optický izomer (S)-1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindolin a farmaceutická kompozice s jeho obsahem
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.
CA2287387C (en) 1997-05-14 2010-02-16 Sloan-Kettering Institute For Cancer Research Methods and compositions for destruction of selected proteins
WO1999015521A1 (en) 1997-09-23 1999-04-01 Eli Lilly And Company Benzothiophenes
ES2220005T3 (es) * 1998-06-16 2004-12-01 Pfizer Products Inc. Combinaciones terapeuticas que comprenden un modulador selectivo del receptor de estrogeno y prostaglandina e2.
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
CA2372176A1 (en) 1999-05-05 2000-11-09 Merck & Co., Inc. Novel prolines as antimicrobial agents
WO2002020740A2 (en) 2000-09-08 2002-03-14 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
US7091353B2 (en) 2000-12-27 2006-08-15 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
CA2432932A1 (en) 2001-02-16 2002-08-29 Mark A. Scialdone 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
JP4541882B2 (ja) 2002-07-02 2010-09-08 ノバルティス アーゲー Smacタンパク質のアポトーシスタンパク質阻害物質(iap)との結合に対するペプチド阻害剤
WO2005007621A2 (en) 2003-05-30 2005-01-27 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
CN1960728A (zh) 2004-01-16 2007-05-09 密歇根大学董事会 构象受限的smac模拟物及其应用
JP5122275B2 (ja) 2004-03-23 2013-01-16 ジェネンテック, インコーポレイテッド Iapのアザビシクロ−オクタンインヒビター
ME02125B (me) 2004-04-07 2013-04-30 Novartis Ag Inhibitori protein apoptoze (iap)
WO2006014361A1 (en) 2004-07-02 2006-02-09 Genentech, Inc. Inhibitors of iap
ATE477254T1 (de) 2004-12-20 2010-08-15 Genentech Inc Pyrrolidine als inhibitoren von iap
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
EA012810B1 (ru) 2005-02-25 2009-12-30 Тетралоджик Фармасеутикалс Димерные ингибиторы ингибиторов белков апоптоза (iap)
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
CA2822094C (en) 2005-08-31 2015-10-27 Celgene Corporation Isoindole-imide compounds and compositions comprising and methods of using the same
JP2009529008A (ja) 2006-03-03 2009-08-13 ノバルティス アクチエンゲゼルシャフト N−ホルミルヒドロキシルアミン化合物
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
US20070218138A1 (en) 2006-03-20 2007-09-20 Bittorf Kevin J Pharmaceutical Compositions
JP5230610B2 (ja) 2006-05-05 2013-07-10 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 二価smac模倣物およびその使用
AU2007275415A1 (en) 2006-07-20 2008-01-24 Ligand Pharmaceuticals Incorporated Proline urea CCR1 antagonists for the treatment of autoimmune diseases or inflammation
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
JP5523831B2 (ja) 2006-08-30 2014-06-18 セルジーン コーポレイション 5−置換イソインドリン化合物
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008109057A1 (en) 2007-03-02 2008-09-12 Dana-Farber Cancer Institute, Inc. Organic compounds and their uses
BRPI0810178A2 (pt) 2007-04-12 2014-09-23 Joyant Pharmaceuticals Inc Dímeros e trímeros miméticos de smac úteis como agentes anticâncer
EP2139490B1 (en) 2007-04-13 2014-07-02 The Regents of the University of Michigan Diazo bicyclic smac mimetics and the uses thereof
BRPI0809867A2 (pt) 2007-04-30 2014-09-30 Genentech Inc Composto, método de indução da apoptose em uma célula, método de sensibilização de uma célula para um sinal apoptótico, método para inibir a ligação de uma proteína iap a uma proteína caspase e métodos
US20100203012A1 (en) 2007-05-30 2010-08-12 Aegera Therapeutics, Inc. Iap bir domain binding compounds
AU2008262038A1 (en) * 2007-06-08 2008-12-18 AbbVie Deutschland GmbH & Co. KG 5-heteroaryl substituted indazoles as kinase inhibitors
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
KR20100038108A (ko) 2007-07-25 2010-04-12 브리스톨-마이어스 스큅 컴퍼니 트리아진 키나제 억제제
WO2009019274A1 (en) 2007-08-06 2009-02-12 Janssen Pharmaceutica Nv Substituted phenylenediamines as inhibitors of the interaction between mdm2 and p53
EP2058312A1 (en) 2007-11-09 2009-05-13 Universita' degli Studi di Milano SMAC mimetic compounds as apoptosis inducers
EP3354646A1 (en) 2008-10-29 2018-08-01 Celgene Corporation Isoindoline compounds for use in the treatment of cancer
CA2744711C (en) 2008-12-05 2017-06-27 Abbott Laboratories Bcl-2-selective apoptosis-inducing agents for the treatment of cancer and immune diseases
JP5487214B2 (ja) * 2008-12-19 2014-05-07 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なカルバゾールカルボキシアミド化合物
US8063102B2 (en) * 2009-03-13 2011-11-22 N.V. Organon Tetrahydronaphthalen-2-ol derivatives
US20120135089A1 (en) 2009-03-17 2012-05-31 Stockwell Brent R E3 ligase inhibitors
PE20120345A1 (es) 2009-05-26 2012-05-17 Abbvie Bahamas Ltd Derivados de 2-(1h-pirrolo[2,3-b]piridin-5-iloxi)-n-fenilsulfonilbenzamida como inhibidores de proteinas anti-apoptoticas
WO2010141805A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
EP2453908B1 (en) 2009-07-13 2018-03-14 President and Fellows of Harvard College Bifunctional stapled polypeptides and uses thereof
EP2784076A1 (en) 2009-10-28 2014-10-01 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
AU2011272860A1 (en) 2010-06-30 2013-02-07 Brandeis University Small-molecule-targeted protein degradation
AU2011305315A1 (en) 2010-09-24 2013-03-28 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
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
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
EP2649099A4 (en) 2010-12-07 2016-10-19 Univ Yale SMALL MOLECULAR HYDROPHOBIC LABELING OF FUSION PROTEINS AND INDUCED REMOVAL FROM THIS
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
US9365640B2 (en) 2011-04-29 2016-06-14 Celgene Corporation Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
WO2013049250A1 (en) 2011-09-27 2013-04-04 Amgen Inc. Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer
EP2776409B1 (en) 2011-11-09 2016-02-03 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
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
DK2797888T3 (en) 2011-12-31 2016-09-19 Beigene Ltd Fused tricyclic compounds as RAF kinase inhibitors
EP3608317A1 (en) * 2012-01-12 2020-02-12 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
US20150141470A1 (en) 2012-05-08 2015-05-21 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
US9365576B2 (en) 2012-05-24 2016-06-14 Novartis Ag Pyrrolopyrrolidinone compounds
CA2869101A1 (en) 2012-05-30 2013-12-05 F. Hoffmann-La Roche Ag Substituted pyrrolidine-2-carboxamides
WO2014011712A1 (en) 2012-07-10 2014-01-16 Bristol-Myers Squibb Company Iap antagonists
US9371568B2 (en) 2012-07-31 2016-06-21 Novartis Ag Markers associated with human double minute 2 inhibitors
HRP20190398T1 (hr) 2012-08-09 2019-05-17 Celgene Corporation Čvrsti oblik (s)-3-(4-((4-morfolinometil)benzil)oksi)-1-oksoizoindolin-2-il)piperidin-2,6-dion hidroklorida
US9453048B2 (en) 2012-08-09 2016-09-27 Bristol-Myers Squibb Company IAP antagonists
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
EP2897949B1 (en) 2012-09-18 2018-01-10 Bristol-Myers Squibb Company Iap antagonists
WO2014055461A1 (en) 2012-10-02 2014-04-10 Bristol-Myers Squibb Company Iap antagonists
TW201428002A (zh) 2012-11-09 2014-07-16 必治妥美雅史谷比公司 用於抑制細胞凋亡抑制劑之巨環化合物
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
WO2014100071A2 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted pyrrolopyrimidines 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.
MX368703B (es) 2013-02-28 2019-10-11 Amgen Inc Un inhibidor de mdm2 derivado de acido benzoico para el tratamiento del cancer.
MX374513B (es) 2013-03-14 2025-03-06 Amgen Inc Compuestos de morfolinona de ácido heteroarilo como inhibidores mdm2 para el tratamiento de cáncer.
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
EP3019517A1 (en) 2013-07-12 2016-05-18 Bristol-Myers Squibb Company Iap antagonists
ES2883289T3 (es) 2013-12-20 2021-12-07 Astex Therapeutics Ltd Compuestos heterocíclicos bicíclicos y sus usos en terapia
CA2940576A1 (en) * 2014-03-13 2015-09-17 F. Hoffmann-La Roche Ag Therapeutic combinations with estrogen receptor modulators
KR20250127179A (ko) 2014-04-14 2025-08-26 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
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
WO2016097071A1 (en) * 2014-12-18 2016-06-23 F. Hoffmann-La Roche Ag Estrogen receptor modulators and uses thereof
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
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
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
KR102564925B1 (ko) 2015-01-20 2023-08-07 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법
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
EP3270917A4 (en) 2015-03-18 2018-08-08 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
EP3302482A4 (en) 2015-06-05 2018-12-19 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
US20170008904A1 (en) 2015-07-10 2017-01-12 Arvinas, Inc. Mdm2-based modulators of proteolysis and associated methods of use
CA2988436A1 (en) 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
WO2017024319A1 (en) 2015-08-06 2017-02-09 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
RU2018120330A (ru) 2015-11-02 2019-12-04 Йейл Юниверсити Химерные соединения, осуществляющие нацеливание для протеолиза, и способы их получения и применения
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
JP7264642B2 (ja) 2016-03-16 2023-04-25 エイチ リー モフィット キャンサー センター アンド リサーチ インスティテュート インコーポレイテッド エフェクターt細胞機能を増進するための、セレブロンを標的とする小分子
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
CN113788818A (zh) * 2016-04-06 2021-12-14 密执安大学评议会 Mdm2蛋白质降解剂
JP6968823B2 (ja) 2016-04-22 2021-11-17 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 Egfrの分解のための二官能性分子、及び使用方法
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
US10245258B2 (en) 2016-06-06 2019-04-02 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
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
HUE061847T2 (hu) 2016-10-11 2023-08-28 Arvinas Operations Inc Androgén receptor célzott degradálására alkalmas vegyületek és eljárások
CA3042260C (en) 2016-11-01 2023-10-03 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
CA3042301A1 (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
CN110741004B (zh) 2016-12-23 2023-10-17 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
JP2020505327A (ja) 2016-12-23 2020-02-20 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法
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
AU2018211975B2 (en) 2017-01-26 2022-05-26 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
KR102747905B1 (ko) 2017-01-31 2024-12-31 아비나스 오퍼레이션스, 인코포레이티드 세레블론 리간드 및 이를 포함하는 이작용성 화합물
IL322809A (en) 2017-09-22 2025-10-01 Kymera Therapeutics Inc Protein Decomposers and Their Uses
UA130036C2 (uk) 2018-12-06 2025-10-22 Радіус Фармасеутікалс, Інк. Спосіб лікування стійкого до інгібітору cdk4/6 раку
CN114667147B (zh) 2019-08-26 2024-09-06 阿尔维纳斯运营股份有限公司 用四氢萘衍生物作为雌激素受体降解剂的治疗乳腺癌的方法
US10836749B1 (en) 2019-09-23 2020-11-17 Accutar Biotechnology Inc. Substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
CA3164202A1 (en) 2019-12-12 2021-06-17 Accutar Biotechnology Inc. Novel chroman derivatives having estrogen receptor degradation activity and uses thereof
CR20230162A (es) 2020-09-14 2023-06-02 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógenos
CA3202592A1 (en) 2020-12-14 2022-06-23 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
CN117715889A (zh) 2021-07-26 2024-03-15 阿尔维纳斯运营股份有限公司 制备双官能化合物的方法
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160045607A1 (en) 2014-08-11 2016-02-18 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
US20160097071A1 (en) 2014-10-03 2016-04-07 Conagen Inc. Non-caloric sweeteners and methods for synthesizing
KR102173464B1 (ko) * 2016-12-01 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체

Also Published As

Publication number Publication date
MX2019006402A (es) 2019-09-11
MX2022010583A (es) 2022-12-13
IL284424B2 (en) 2023-04-01
EP3689868A1 (en) 2020-08-05
BR112019011200B1 (pt) 2021-12-28
RU2020106142A (ru) 2020-04-13
IL272527A (en) 2020-03-31
CN110291087B (zh) 2024-07-09
CN114656452A (zh) 2022-06-24
US20240076281A1 (en) 2024-03-07
AU2017366693A1 (en) 2019-04-18
JP6972211B2 (ja) 2021-11-24
CO2019007091A2 (es) 2019-10-09
KR20240063185A (ko) 2024-05-10
PL3689868T3 (pl) 2024-03-11
FI3689868T3 (fi) 2023-12-18
JP2025060813A (ja) 2025-04-10
IL284424B (en) 2022-12-01
JP7160497B2 (ja) 2022-10-25
AU2021204549A1 (en) 2021-08-05
RU2750484C2 (ru) 2021-06-28
IL297717A (en) 2022-12-01
SMT202300483T1 (it) 2024-01-10
US11104666B2 (en) 2021-08-31
US10899742B1 (en) 2021-01-26
IL266842A (en) 2019-07-31
DK3689868T3 (da) 2024-01-02
IL284424A (en) 2021-07-29
JP2025143400A (ja) 2025-10-01
JP2021169479A (ja) 2021-10-28
US20210139458A1 (en) 2021-05-13
JP2020100659A (ja) 2020-07-02
AU2017366693A9 (en) 2019-05-02
CA3042968C (en) 2023-10-17
KR20190082989A (ko) 2019-07-10
JP7708960B2 (ja) 2025-07-15
US20250320195A1 (en) 2025-10-16
EP3689868B1 (en) 2023-09-27
RS64976B1 (sr) 2024-01-31
WO2018102725A1 (en) 2018-06-07
AU2024201437A1 (en) 2024-03-21
HRP20231537T1 (hr) 2024-03-15
ES2967404T3 (es) 2024-04-30
CN110291087A (zh) 2019-09-27
JP2022023103A (ja) 2022-02-07
IL266842B (en) 2022-09-01
JP2023021211A (ja) 2023-02-10
CA3042968A1 (en) 2018-06-07
KR102173464B9 (ko) 2022-05-23
SI3689868T1 (sl) 2024-02-29
AU2020201793B2 (en) 2020-08-27
BR112019011200A2 (pt) 2019-10-08
US11597720B2 (en) 2023-03-07
RU2019120120A3 (enExample) 2021-03-24
KR102173464B1 (ko) 2020-11-04
RU2020106142A3 (enExample) 2020-08-07
EP3548483A4 (en) 2020-06-10
US12172981B2 (en) 2024-12-24
AU2017366693B2 (en) 2021-04-01
CN114656452B (zh) 2023-01-17
US20220388984A1 (en) 2022-12-08
AU2021204549B2 (en) 2023-07-06
RU2019120120A (ru) 2020-12-28
AU2021257895A1 (en) 2021-11-18
LT3689868T (lt) 2023-12-27
JP2020504089A (ja) 2020-02-06
IL316544A (en) 2024-12-01
CN118834201A (zh) 2024-10-25
HUE064609T2 (hu) 2024-04-28
EP3548483A1 (en) 2019-10-09
US10647698B2 (en) 2020-05-12
KR20200020988A (ko) 2020-02-26
CN111454248A (zh) 2020-07-28
US20180155322A1 (en) 2018-06-07
AU2020201793A1 (en) 2020-03-26
IL272527B (en) 2021-07-29
JP7611885B2 (ja) 2025-01-10
US20220274955A1 (en) 2022-09-01
PT3689868T (pt) 2024-01-02
JP6957620B2 (ja) 2021-11-02

Similar Documents

Publication Publication Date Title
KR102674902B1 (ko) 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
KR102582886B1 (ko) 에스트로겐 수용체 단백질 분해 조절제 및 관련 사용 방법
JP2022023103A5 (enExample)
JP2020504089A5 (enExample)
RU2797244C2 (ru) Производные тетрагидронафталина и тетрагидроизохинолина в качестве разрушителей эстрогенового рецептора
HK40023198A (en) Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
HK40023198B (en) Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A107 Divisional application of patent
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

R15-X000 Change to inventor requested

St.27 status event code: A-3-3-R10-R15-oth-X000

R16-X000 Change to inventor recorded

St.27 status event code: A-3-3-R10-R16-oth-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E601 Decision to refuse application
PE0601 Decision on rejection of patent

St.27 status event code: N-2-6-B10-B15-exm-PE0601

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T13-X000 Administrative time limit extension granted

St.27 status event code: U-3-3-T10-T13-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T13-X000 Administrative time limit extension granted

St.27 status event code: U-3-3-T10-T13-oth-X000

AMND Amendment
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PX0901 Re-examination

St.27 status event code: A-2-3-E10-E12-rex-PX0901

PX0701 Decision of registration after re-examination

St.27 status event code: A-3-4-F10-F13-rex-PX0701

X701 Decision to grant (after re-examination)
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601