HUE064609T2 - Tetrahidronaftalin és tetrahidroizokinolin származékok mint ösztrogénreceptor-lebontó anyagok - Google Patents

Tetrahidronaftalin és tetrahidroizokinolin származékok mint ösztrogénreceptor-lebontó anyagok

Info

Publication number
HUE064609T2
HUE064609T2 HUE20150584A HUE20150584A HUE064609T2 HU E064609 T2 HUE064609 T2 HU E064609T2 HU E20150584 A HUE20150584 A HU E20150584A HU E20150584 A HUE20150584 A HU E20150584A HU E064609 T2 HUE064609 T2 HU E064609T2
Authority
HU
Hungary
Prior art keywords
tetrahydronaphthalene
estrogen receptor
tetrahydroisoquinoline derivatives
receptor degraders
degraders
Prior art date
Application number
HUE20150584A
Other languages
English (en)
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 HUE064609T2 publication Critical patent/HUE064609T2/hu

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • C07K5/06139Dipeptides 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (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)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
HUE20150584A 2016-12-01 2017-12-01 Tetrahidronaftalin és tetrahidroizokinolin származékok mint ösztrogénreceptor-lebontó anyagok HUE064609T2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662429041P 2016-12-01 2016-12-01
US201762540049P 2017-08-01 2017-08-01

Publications (1)

Publication Number Publication Date
HUE064609T2 true HUE064609T2 (hu) 2024-04-28

Family

ID=62240410

Family Applications (1)

Application Number Title Priority Date Filing Date
HUE20150584A HUE064609T2 (hu) 2016-12-01 2017-12-01 Tetrahidronaftalin és tetrahidroizokinolin származékok mint ösztrogénreceptor-lebontó anyagok

Country Status (23)

Country Link
US (6) US10647698B2 (hu)
EP (2) EP3689868B1 (hu)
JP (5) JP6957620B2 (hu)
KR (3) KR102674902B1 (hu)
CN (3) CN110291087B (hu)
AU (5) AU2017366693B2 (hu)
BR (1) BR112019011200B1 (hu)
CA (1) CA3042968C (hu)
CO (1) CO2019007091A2 (hu)
DK (1) DK3689868T3 (hu)
ES (1) ES2967404T3 (hu)
FI (1) FI3689868T3 (hu)
HR (1) HRP20231537T1 (hu)
HU (1) HUE064609T2 (hu)
IL (4) IL266842B (hu)
LT (1) LT3689868T (hu)
MX (2) MX2019006402A (hu)
PL (1) PL3689868T3 (hu)
PT (1) PT3689868T (hu)
RS (1) RS64976B1 (hu)
RU (1) RU2750484C2 (hu)
SI (1) SI3689868T1 (hu)
WO (1) WO2018102725A1 (hu)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
JP6817962B2 (ja) 2015-01-20 2021-01-20 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. ターゲティングされたアンドロゲン受容体分解のための化合物および方法
EP3302482A4 (en) 2015-06-05 2018-12-19 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
WO2017197036A1 (en) 2016-05-10 2017-11-16 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
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
US20180072711A1 (en) 2016-09-15 2018-03-15 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
CN110234646A (zh) 2016-11-01 2019-09-13 阿尔维纳斯股份有限公司 靶向PROTAC的Tau蛋白及相关使用方法
US10647698B2 (en) 2016-12-01 2020-05-12 Arvinas Operations, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
EP3558994A4 (en) 2016-12-23 2021-05-12 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, 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
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma 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
AU2018211975B2 (en) 2017-01-26 2022-05-26 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
WO2018237026A1 (en) 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS
CN118108706A (zh) 2017-09-04 2024-05-31 C4医药公司 戊二酰亚胺
EP3679027A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Dihydrobenzimidazolones
EP3679028A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Dihydroquinolinones
WO2019099868A2 (en) 2017-11-16 2019-05-23 C4 Therapeutics, Inc. Degraders and degrons for targeted protein degradation
EP3710443A1 (en) 2017-11-17 2020-09-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
US11220515B2 (en) 2018-01-26 2022-01-11 Yale University Imide-based modulators of proteolysis and associated methods of use
EP3773576A4 (en) 2018-03-26 2021-12-29 C4 Therapeutics, Inc. Cereblon binders for the degradation of ikaros
KR20240095318A (ko) 2018-04-04 2024-06-25 아비나스 오퍼레이션스, 인코포레이티드 단백질분해 조절제 및 연관된 사용 방법
CN110357889B (zh) * 2018-04-09 2022-03-15 上海科技大学 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用
CN118480030A (zh) * 2018-04-13 2024-08-13 阿尔维纳斯运营股份有限公司 小脑蛋白配体和包括其的双官能化合物
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
PL3784663T3 (pl) 2018-04-23 2023-12-27 Celgene Corporation Podstawione związki 4-aminoizoindolino-1,3-dionowe i ich zastosowanie do leczenia chłoniaka
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
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
CR20210001A (es) * 2018-07-10 2021-04-19 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 proteina con dedos de zinc 2 de la familia ikaros (1kzf2)
JP7515175B2 (ja) 2018-07-31 2024-07-12 ファイメクス株式会社 複素環化合物
JP7297053B2 (ja) 2018-08-20 2023-06-23 アルビナス・オペレーションズ・インコーポレイテッド 神経変性疾患を治療するためのe3ユビキチンリガーゼ結合活性を有するキメラ(protac)化合物を標的とし、アルファ-シヌクレインタンパク質を標的とするタンパク質分解
WO2020051235A1 (en) 2018-09-04 2020-03-12 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
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
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
AU2019418416A1 (en) * 2019-01-03 2021-07-22 The Regents Of The University Of Michigan Estrogen receptor protein degraders
WO2020165834A1 (en) * 2019-02-15 2020-08-20 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
EP3924054A1 (en) * 2019-02-15 2021-12-22 Novartis AG 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
US20220387906A1 (en) 2019-03-21 2022-12-08 Codiak Biosciences, Inc. Process for preparing extracellular vesicles
EP3941528A1 (en) 2019-03-21 2022-01-26 Codiak BioSciences, Inc. Extracellular vesicle conjugates and uses thereof
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
US20220241424A1 (en) 2019-04-16 2022-08-04 Northwestern University Treatment of cancer
WO2020214952A1 (en) * 2019-04-18 2020-10-22 Accutar Biotechnology Inc. Novel compounds having bet, estrogen receptor, and androgen receptor degradation activity and uses thereof
JP7548992B2 (ja) 2019-07-17 2024-09-10 アルビナス・オペレーションズ・インコーポレイテッド タウタンパク質標的化化合物および関連する使用方法
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
US20210060008A1 (en) * 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
IL291590B2 (en) * 2019-09-23 2023-11-01 Accutar Biotechnology Inc Novel modified quinoline-8-carbonitrile compounds with androgen receptor unblocking activity and their uses
CN112574278B (zh) * 2019-09-29 2024-08-23 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其制备方法和医药应用
KR20220103753A (ko) 2019-11-19 2022-07-22 브리스톨-마이어스 스큅 컴퍼니 헬리오스 단백질의 억제제로서 유용한 화합물
MX2022006133A (es) * 2019-12-06 2022-06-17 Celgene Corp Procesos para preparar 2-(4-clorofenil)-n-((2-(2,6-dioxopiperidin- 3-il)-1-oxoisoindolin-5-il)metil)-2,2-difluoroacetamida.
EP4420728A2 (en) * 2019-12-12 2024-08-28 Accutar Biotechnology Inc. Novel chroman derivatives having estrogen receptor degradation activity and uses thereof
JP2023507590A (ja) * 2019-12-17 2023-02-24 オリオニス バイオサイエンシズ,インコーポレイテッド タンパク質の動員および/または分解を調節する化合物
CR20220278A (es) 2019-12-18 2022-07-01 Novartis Ag Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y usos de los mismos
TW202136240A (zh) 2019-12-19 2021-10-01 美商亞文納營運公司 用於靶向降解雄激素受體之化合物及方法
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
US11851445B2 (en) * 2020-01-29 2023-12-26 Foghorn Therapeutics Inc. Compounds and uses thereof
US20230096517A1 (en) * 2020-02-25 2023-03-30 Shanghaitech University Glutarimide skeleton-based compounds and application thereof
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
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
MX2023002979A (es) 2020-09-14 2023-04-10 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradacion dirigida del receptor de estrogenos.
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
WO2022066928A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Process for preparing extracellular vesicles
IL302669A (en) 2020-11-06 2023-07-01 Prelude Therapeutics Inc BRM-targeted compounds and related methods of use
MX2023007058A (es) 2020-12-14 2023-06-23 Arvinas Operations Inc Metodos de tratamiento del cancer de mama con derivados de tetrahidronaftaleno como degradadores del receptor de estrogenos.
MX2023008296A (es) 2021-01-13 2023-09-29 Monte Rosa Therapeutics Inc Compuestos de isoindolinona.
CN116438177A (zh) * 2021-01-28 2023-07-14 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
EP4289841A1 (en) * 2021-02-04 2023-12-13 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Benzo seven-membered ring bifunctional compound and application thereof
EP4317146A1 (en) 2021-03-29 2024-02-07 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Tetrahydronaphthalene compound, and preparation method therefor and use thereof in medicine
WO2022216573A1 (en) 2021-04-05 2022-10-13 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
CN117279910A (zh) 2021-04-16 2023-12-22 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
MX2023012981A (es) * 2021-05-03 2024-01-11 Nurix Therapeutics Inc Compuestos para inhibir o degradar proteinas objetivo, composiciones que los comprenden, metodos para su preparacion y metodos para usarlos.
AU2022268977A1 (en) 2021-05-05 2023-11-30 Biogen Ma Inc. Compounds for targeting degradation of bruton's tyrosine kinase
AU2022284366A1 (en) * 2021-06-03 2023-10-26 Novartis Ag 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and medical uses thereof
TW202321236A (zh) 2021-07-07 2023-06-01 美商百健Ma公司 用於靶向irak4蛋白降解之化合物
WO2023283372A1 (en) 2021-07-07 2023-01-12 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
CA3227425A1 (en) 2021-07-26 2023-02-02 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound
EP4421071A1 (en) * 2021-10-22 2024-08-28 Gluetacs Therapeutics (Shanghai) Co., Ltd. Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications
EP4431511A1 (en) 2021-11-09 2024-09-18 Hangzhou Glubio Pharmaceutical Co. Ltd. Wee1 protein kinase degradation agent and use thereof
CN118401512A (zh) * 2021-12-24 2024-07-26 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
EP4245756A1 (en) 2022-03-17 2023-09-20 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
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
WO2024006781A1 (en) * 2022-06-27 2024-01-04 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
WO2024049926A1 (en) 2022-08-31 2024-03-07 Arvinas Operations, Inc. Dosage regimens of 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
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
US20240158370A1 (en) * 2022-09-09 2024-05-16 Innovo Therapeutics, Inc. CK1 alpha AND DUAL CK1 alpha / GSPT1 DEGRADING COMPOUNDS
WO2024073507A1 (en) 2022-09-28 2024-04-04 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
WO2024067781A1 (zh) * 2022-09-29 2024-04-04 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
WO2024083716A1 (en) 2022-10-17 2024-04-25 Astrazeneca Ab Combinations of a serd for the treatment of cancer
US20240180893A1 (en) 2022-11-17 2024-06-06 Astrazeneca Ab Methods of treatment of breast cancer
KR20240078553A (ko) * 2022-11-25 2024-06-04 재단법인 대구경북첨단의료산업진흥재단 선택적 에스트로겐 수용체 조절제로서의 신규 화합물
WO2024119081A1 (en) 2022-12-02 2024-06-06 Arvinas Operations, Inc. Method of treating breast cancer
CN116751186A (zh) * 2022-12-23 2023-09-15 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
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
WO2024167904A1 (en) 2023-02-07 2024-08-15 Arvinas Operations, Inc. Dosage regimens of estrogen receptor degraders in combination with an mtor inhibitor

Family Cites Families (134)

* 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
ES2339425T3 (es) 1996-07-24 2010-05-20 Celgene Corporation 2-(2,6-dioxopiperidin-3-il)-ftalimidas y -1-oxoisoindolinas sustituidas y procedimiento para reducir los niveles 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.
EP1023315B1 (en) 1997-05-14 2010-03-10 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
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
DE60026514T2 (de) 1999-05-05 2006-11-09 Merck & Co., Inc. Neue prolinverbindungen als mikrobizide mittel
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
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
US7915293B2 (en) 2003-05-30 2011-03-29 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
AU2005228950B2 (en) 2004-03-23 2012-02-02 Genentech, Inc. Azabicyclo-octane inhibitors of IAP
NZ549925A (en) 2004-04-07 2010-08-27 Novartis Ag Inhibitors of IAP
WO2006014361A1 (en) 2004-07-02 2006-02-09 Genentech, Inc. Inhibitors of iap
DE602005022936D1 (de) 2004-12-20 2010-09-23 Genentech Inc Pyrrolidine als inhibitoren von iap
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
AU2006216450C1 (en) 2005-02-25 2013-01-10 Medivir Ab Dimeric IAP inhibitors
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
KR20080095895A (ko) 2006-03-03 2008-10-29 노파르티스 아게 N―포르밀 히드록실아민 화합물
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
EP2019671B1 (en) 2006-05-05 2014-09-24 The Regents Of The University Of Michigan Intermediates for the preparation of bivalent smac mimetics
EP2059502A2 (en) 2006-07-20 2009-05-20 Ligand Pharmaceuticals Incorporated Proline urea ccr1 antagonists for the treatment of autoimmune diseases or inflammation
WO2008014236A1 (en) 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
CL2007002513A1 (es) 2006-08-30 2008-04-04 Celgene Corp Soc Organizada Ba Compuestos derivados de isoindolina sustituidos, compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento y prevencion de enfermedades tales como cancer, dolor, degeneracion macular, entre otras.
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
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
AU2008240153B2 (en) 2007-04-12 2013-01-31 Joyant Pharmaceuticals, Inc. SMAC mimetic dimers and trimers useful as anti-cancer agents
WO2008128171A2 (en) 2007-04-13 2008-10-23 The Regents Of The University Of Michigan Diazo bicyclic smac mimetics and the uses thereof
WO2008134679A1 (en) 2007-04-30 2008-11-06 Genentech, Inc. Inhibitors of iap
WO2008144925A1 (en) 2007-05-30 2008-12-04 Aegera Therapeutics Inc. Iap bir domain binding compounds
MX2009013213A (es) * 2007-06-08 2010-03-30 Abbott Lab Indazoles 5-sustituidos 5-heteroarilo como inhibidores de cinasa.
WO2009015254A1 (en) 2007-07-25 2009-01-29 Bristol-Myers Squibb Company Triazine kinase inhibitors
EP2058312A1 (en) 2007-11-09 2009-05-13 Universita' degli Studi di Milano SMAC mimetic compounds as apoptosis inducers
JP5603876B2 (ja) 2008-10-29 2014-10-08 セルジーン コーポレイション 癌の治療に使用するためのイソインドリン化合物
CA2747670A1 (en) * 2008-12-19 2010-07-15 Bristol-Myers Squibb Company Carbazole carboxamide compounds useful as kinase inhibitors
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
US8614201B2 (en) 2009-06-05 2013-12-24 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
JP5529282B2 (ja) 2009-10-28 2014-06-25 ジョイアント ファーマスーティカルズ、インク. 二量体Smac模倣薬
US8440693B2 (en) * 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
ES2730763T3 (es) 2010-02-11 2019-11-12 Celgene Corp Derivados de arilmetoxi isoindolina y composiciones que los comprenden y métodos de uso de los mismos
US9765019B2 (en) 2010-06-30 2017-09-19 Brandeis University Small-molecule-targeted protein degradation
EP2619184B1 (en) 2010-09-24 2018-05-23 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
CN103502275A (zh) 2010-12-07 2014-01-08 耶鲁大学 融合蛋白的小分子疏水性标记和引起的其降解
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
JP6016892B2 (ja) 2011-04-29 2016-10-26 セルジーン コーポレイション セレブロンを予測因子として使用する癌及び炎症性疾患の治療方法
US9376425B2 (en) 2011-09-27 2016-06-28 Amgen, Inc. Heterocyclic compounds as MDM2 inhibitors for the treatment of cancer
WO2013071039A1 (en) 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
EP2776409B1 (en) 2011-11-09 2016-02-03 Ensemble Therapeutics Corporation 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
PL2797888T3 (pl) 2011-12-31 2016-12-30 Połączone związki tricykliczne jako inhibitory kinazy raf
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
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
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
CN104321325B (zh) 2012-05-24 2016-11-16 诺华股份有限公司 吡咯并吡咯烷酮化合物
JP6067108B2 (ja) 2012-05-30 2017-01-25 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 置換ピロリジン−2−カルボキサミド
US9345740B2 (en) 2012-07-10 2016-05-24 Bristol-Myers Squibb Company IAP antagonists
CN104520714A (zh) 2012-07-31 2015-04-15 诺华股份有限公司 与对人双微体2(mdm2)抑制剂的敏感性相关的标志物
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
CA2930030A1 (en) 2012-11-09 2014-05-15 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
US9637493B2 (en) 2012-12-20 2017-05-02 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.
MX2015012427A (es) 2013-03-14 2016-01-12 Amgen Inc Compuestos de morfolinona de acido heteroarilo como inhibidores mdm2 para el tratamiento de 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
JP2017507964A (ja) * 2014-03-13 2017-03-23 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト エストロゲン受容体モジュレーターを用いた治療的組合せ
KR20240038809A (ko) 2014-04-14 2024-03-25 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
US10071164B2 (en) * 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
MY182725A (en) 2014-10-03 2021-02-03 Conagen Inc Non-caloric sweeteners and methods for synthesizing
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
CN107257800B (zh) 2014-12-23 2020-06-30 达纳-法伯癌症研究所股份有限公司 通过双功能分子诱导靶蛋白降解的方法
JP6817962B2 (ja) 2015-01-20 2021-01-20 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. ターゲティングされたアンドロゲン受容体分解のための化合物および方法
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
CN108601764A (zh) 2015-03-18 2018-09-28 阿尔维纳斯股份有限公司 用于靶蛋白的增强降解的化合物和方法
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
KR20180035828A (ko) 2015-07-10 2018-04-06 아비나스 인코포레이티드 단백질 분해의 mdm2계 조절인자 및 관련된 이용 방법
WO2017011590A1 (en) 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
CA2995036A1 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Tunable endogenous protein degradation
WO2017030814A1 (en) 2015-08-19 2017-02-23 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
CA3011949A1 (en) 2016-03-15 2017-09-21 Merrimack Pharmaceuticals, Inc. Methods for treating er+, her2-, hrg+ breast cancer using combination therapies comprising an anti-erbb3 antibody
MX2018011216A (es) 2016-03-16 2019-08-29 H Lee Moffitt Cancer Ct & Res Moléculas pequeñas contra cereblon para mejorar la función efectora de los linfocitos t.
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
EP3892272B1 (en) 2016-04-22 2024-07-24 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
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
US20180072711A1 (en) 2016-09-15 2018-03-15 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
PL3660004T3 (pl) * 2016-10-11 2023-10-02 Arvinas Operations, Inc. Związki i sposoby do ukierunkowanej degradacji receptora androgenowego
CN110234646A (zh) 2016-11-01 2019-09-13 阿尔维纳斯股份有限公司 靶向PROTAC的Tau蛋白及相关使用方法
AU2017363257B2 (en) 2016-11-22 2021-08-19 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use
US10647698B2 (en) 2016-12-01 2020-05-12 Arvinas Operations, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
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
EP3558994A4 (en) 2016-12-23 2021-05-12 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal 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
AU2018211975B2 (en) 2017-01-26 2022-05-26 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
KR20190116315A (ko) 2017-01-31 2019-10-14 아비나스 오퍼레이션스, 인코포레이티드 세레블론 리간드 및 이를 포함하는 이작용성 화합물
US20210060008A1 (en) 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
EP4420728A2 (en) 2019-12-12 2024-08-28 Accutar Biotechnology Inc. Novel chroman derivatives having estrogen receptor degradation activity and uses thereof
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
CN111454248A (zh) 2020-07-28
BR112019011200B1 (pt) 2021-12-28
IL272527A (en) 2020-03-31
SI3689868T1 (sl) 2024-02-29
WO2018102725A1 (en) 2018-06-07
ES2967404T3 (es) 2024-04-30
AU2020201793B2 (en) 2020-08-27
IL272527B (en) 2021-07-29
KR20240063185A (ko) 2024-05-10
KR102173464B1 (ko) 2020-11-04
CN110291087B (zh) 2024-07-09
JP2023021211A (ja) 2023-02-10
MX2019006402A (es) 2019-09-11
IL284424B2 (en) 2023-04-01
FI3689868T3 (fi) 2023-12-18
EP3689868B1 (en) 2023-09-27
HRP20231537T1 (hr) 2024-03-15
JP6957620B2 (ja) 2021-11-02
RS64976B1 (sr) 2024-01-31
LT3689868T (lt) 2023-12-27
CA3042968C (en) 2023-10-17
JP7160497B2 (ja) 2022-10-25
MX2022010583A (es) 2022-12-13
JP2020100659A (ja) 2020-07-02
IL284424B (en) 2022-12-01
JP2021169479A (ja) 2021-10-28
CN110291087A (zh) 2019-09-27
US20220388984A1 (en) 2022-12-08
EP3548483A4 (en) 2020-06-10
US20180155322A1 (en) 2018-06-07
US20240076281A1 (en) 2024-03-07
AU2021257895A1 (en) 2021-11-18
AU2020201793A1 (en) 2020-03-26
IL266842A (en) 2019-07-31
PT3689868T (pt) 2024-01-02
US10647698B2 (en) 2020-05-12
KR20190082989A (ko) 2019-07-10
JP6972211B2 (ja) 2021-11-24
EP3548483A1 (en) 2019-10-09
PL3689868T3 (pl) 2024-03-11
JP2022023103A (ja) 2022-02-07
BR112019011200A2 (pt) 2019-10-08
CA3042968A1 (en) 2018-06-07
RU2020106142A (ru) 2020-04-13
IL297717A (en) 2022-12-01
CN114656452B (zh) 2023-01-17
EP3689868A1 (en) 2020-08-05
US20220274955A1 (en) 2022-09-01
AU2024201437A1 (en) 2024-03-21
JP2020504089A (ja) 2020-02-06
US11104666B2 (en) 2021-08-31
AU2017366693A9 (en) 2019-05-02
AU2021204549A1 (en) 2021-08-05
DK3689868T3 (da) 2024-01-02
IL266842B (en) 2022-09-01
RU2750484C2 (ru) 2021-06-28
KR102173464B9 (ko) 2022-05-23
CO2019007091A2 (es) 2019-10-09
AU2021204549B2 (en) 2023-07-06
AU2017366693B2 (en) 2021-04-01
US10899742B1 (en) 2021-01-26
RU2019120120A (ru) 2020-12-28
KR102674902B1 (ko) 2024-06-14
CN114656452A (zh) 2022-06-24
RU2019120120A3 (hu) 2021-03-24
AU2017366693A1 (en) 2019-04-18
KR20200020988A (ko) 2020-02-26
US20210139458A1 (en) 2021-05-13
US11597720B2 (en) 2023-03-07
RU2020106142A3 (hu) 2020-08-07
IL284424A (en) 2021-07-29

Similar Documents

Publication Publication Date Title
IL284424A (en) History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
ZA201805573B (en) Selective estrogen receptor degraders and uses thereof
HK1247199A1 (zh) 雌激素受體調節劑及其用途
IL266353A (en) Steroids and their protein conjugates
IL261654B (en) Estrogen receptor modulators
HK1248683A1 (zh) 雜環雌激素受體調節劑及其用途
HK1258851A1 (zh) 四氫萘雌激素受體調節劑及其用途
HK1214532A1 (zh) 雌激素受體調節劑及其用途
IL247252A0 (en) History of isoquinoline and its use
HK1258886A1 (zh) T細胞受體及其用途
HK1252202A1 (zh) 部署裝置及相關的組件和方法
ZA201900113B (en) Ethynyl derivatives
GB2546327B (en) Security cowl and fixing
HK1253294A1 (zh) 阿片受體調節劑及其用途
IL261055A (en) Derivatives of tetrahydroisoquinoline
GB2550927B (en) Repositionable self-adhesive closed-cell solid-foam insulation material
GB201500597D0 (en) DAP wallpaper (Design and Print Wallpaper)