CO2021013927A2 - Protacs que degradan el receptor de estrógeno - Google Patents

Protacs que degradan el receptor de estrógeno

Info

Publication number
CO2021013927A2
CO2021013927A2 CONC2021/0013927A CO2021013927A CO2021013927A2 CO 2021013927 A2 CO2021013927 A2 CO 2021013927A2 CO 2021013927 A CO2021013927 A CO 2021013927A CO 2021013927 A2 CO2021013927 A2 CO 2021013927A2
Authority
CO
Colombia
Prior art keywords
protacs
degrade
compounds
estrogen receptor
treatment
Prior art date
Application number
CONC2021/0013927A
Other languages
English (en)
Inventor
Bin Yang
Thomas George Christopher Hayhow
Charlene Fallan
James Stewart Scott
Coura Diene
Bernard Christophe Barlaam
Johannes Wilhelmus Maria Nissink
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of CO2021013927A2 publication Critical patent/CO2021013927A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La memoria descriptiva se refiere en general a compuestos de Fórmula (I): (I) y sales farmacéuticamente aceptables de los mismos, donde R1, R2, R3, R4, R6, R7, R8, enlazador, A, G, D y E tienen cualquiera de los significados definidos en la presente. Esta memoria descriptiva también se refiere al uso de tales compuestos y sales farmacéuticamente aceptables de estos en métodos de tratamiento del cuerpo humano o animal, por ejemplo, en la prevención o el tratamiento del cáncer. Esta memoria descriptiva también se refiere a procesos y compuestos intermedios implicados en la preparación de dichos compuestos y a composiciones farmacéuticas que los contienen.
CONC2021/0013927A 2019-03-29 2021-10-15 Protacs que degradan el receptor de estrógeno CO2021013927A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962825924P 2019-03-29 2019-03-29
PCT/EP2020/058702 WO2020201080A1 (en) 2019-03-29 2020-03-27 Estrogen receptor degrading protacs

Publications (1)

Publication Number Publication Date
CO2021013927A2 true CO2021013927A2 (es) 2021-10-29

Family

ID=70050126

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2021/0013927A CO2021013927A2 (es) 2019-03-29 2021-10-15 Protacs que degradan el receptor de estrógeno

Country Status (24)

Country Link
US (1) US20220169643A1 (es)
EP (1) EP3947376A1 (es)
JP (1) JP2022526370A (es)
KR (1) KR20210146984A (es)
CN (1) CN113646306A (es)
AR (1) AR118515A1 (es)
AU (1) AU2020252116B2 (es)
BR (1) BR112021019007A2 (es)
CA (1) CA3133763A1 (es)
CL (1) CL2021002489A1 (es)
CO (1) CO2021013927A2 (es)
CR (1) CR20210532A (es)
DO (1) DOP2021000198A (es)
EA (1) EA202192553A1 (es)
EC (1) ECSP21077887A (es)
IL (1) IL286461A (es)
JO (1) JOP20210259A1 (es)
MA (1) MA55495A (es)
MX (1) MX2021011811A (es)
PE (1) PE20220131A1 (es)
SG (1) SG11202110527RA (es)
TW (1) TW202102497A (es)
UY (1) UY38625A (es)
WO (1) WO2020201080A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022217010A1 (en) * 2021-04-09 2022-10-13 Endotarget Inc. Compounds and methods for the targeted degradation of estrogen receptors
TW202321219A (zh) 2021-08-11 2023-06-01 大陸商四川海思科製藥有限公司 雜環衍生物及其組合物和藥學上的應用
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
WO2023212599A2 (en) * 2022-04-26 2023-11-02 Endotarget Inc. Compounds and methods for targeted degradation of estrogen receptors
CN114853751B (zh) * 2022-05-13 2024-01-16 郑州大学第一附属医院 一组吩噻嗪类衍生物及其应用
WO2024015406A1 (en) * 2022-07-12 2024-01-18 Regents Of The University Of Michigan Indole derivatives as estrogen receptor degraders

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008152394A1 (en) * 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
NO2714752T3 (es) * 2014-05-08 2018-04-21
WO2018019793A1 (en) 2016-07-25 2018-02-01 Astrazeneca Ab N-(2-(4-((1r,3r)-3-methyl-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indol-1-yl)phenoxy)ethyl)propan-1-amine derivatives and related compounds as selective down-regulators of the estrogen receptor for treating cancer
PL3660004T3 (pl) 2016-10-11 2023-10-02 Arvinas Operations, Inc. Związki i sposoby do ukierunkowanej degradacji receptora androgenowego
IL266842B (en) 2016-12-01 2022-09-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
BR112019015312A2 (pt) * 2017-01-26 2020-03-10 Arvinas Operations, Inc. Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados

Also Published As

Publication number Publication date
EP3947376A1 (en) 2022-02-09
AR118515A1 (es) 2021-10-20
CN113646306A (zh) 2021-11-12
DOP2021000198A (es) 2021-10-31
EA202192553A1 (ru) 2022-02-21
CA3133763A1 (en) 2020-10-08
US20220169643A1 (en) 2022-06-02
JOP20210259A1 (ar) 2023-01-30
BR112021019007A2 (pt) 2021-11-30
ECSP21077887A (es) 2021-11-30
KR20210146984A (ko) 2021-12-06
IL286461A (en) 2021-10-31
AU2020252116A1 (en) 2021-11-11
MX2021011811A (es) 2021-10-22
TW202102497A (zh) 2021-01-16
JP2022526370A (ja) 2022-05-24
CR20210532A (es) 2022-02-10
WO2020201080A1 (en) 2020-10-08
UY38625A (es) 2020-10-30
CL2021002489A1 (es) 2022-06-03
PE20220131A1 (es) 2022-01-27
SG11202110527RA (en) 2021-10-28
MA55495A (fr) 2022-02-09
AU2020252116B2 (en) 2023-04-27

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