CL2025002736A1 - Compuestos bifuncionales capaces de degradar receptores de andrógenos - Google Patents

Compuestos bifuncionales capaces de degradar receptores de andrógenos

Info

Publication number
CL2025002736A1
CL2025002736A1 CL2025002736A CL2025002736A CL2025002736A1 CL 2025002736 A1 CL2025002736 A1 CL 2025002736A1 CL 2025002736 A CL2025002736 A CL 2025002736A CL 2025002736 A CL2025002736 A CL 2025002736A CL 2025002736 A1 CL2025002736 A1 CL 2025002736A1
Authority
CL
Chile
Prior art keywords
atom
alkyl
alkoxy
atoms
framework
Prior art date
Application number
CL2025002736A
Other languages
English (en)
Inventor
Scott James
Astles Peter
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 CL2025002736A1 publication Critical patent/CL2025002736A1/es

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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

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)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Un compuesto de la Fórmula (I): o una sal farmacéuticamente aceptable de este, en donde: X1 es CH o N; p es 0, 1 o 2; donde: cada R1 es un sustituyente en cualquier átomo C y se selecciona independientemente de F, Cl, alquilo C1-3 y alcoxi C1-3, en donde dicho alquilo C1-3 y alcoxi C1-3 pueden sustituirse opcionalmente de manera independiente con uno o más F; RN se selecciona de H y Me; n es 0, 1 o 2; m es 0 o 1; Q1 es CH o N; cuando n y m son ambos distintos de 0, Q2 es CH o N; cuando n y m son ambos 0, Q2 es CH; cuando n es 0 o 1, Q3 es CH; cuando n es 2 y Q2 es N, Q3 es CH; cuando n es 2 y Q2 es CH, Q3 es CH u O; R2a y R2b son sustituyentes en el mismo átomo de C o en átomos de C diferentes distintos de Q1 o Q2, cada uno independientemente seleccionado de H, F y alquilo C1-3, o R2a y R2b juntos forman un grupo -(CH2)r- donde r es 1, 2 o 3; Q4 es un enlace único o -NR4C(=O); R4 es H o Me; 0, 1 o 2 de Y1, Y2, Y3, Y4 y Y5 es-son N, y son de cualquier otra manera C; cada R3 es un sustituyente de cualquier átomo C en Y1, Y2, Y3, Y4 y Y5, y se selecciona independientemente de F, Cl, CN, alquilo C1-3 y alcoxi C1-3, en donde dicho alquilo C1-3 y alcoxi C1-3 pueden sustituirse opcionalmente de manera independiente con uno o más F; q es 0, 1 o 2; en donde el Enlazador está unido a cualquier átomo C disponible en Y4 y Y5; el Enlazador es un marco saturado o parcialmente o totalmente insaturado que comprende átomos de C y H y al menos un heteroátomo, en donde dicho marco tiene puntos finales de unión a y b y una longitud de 5 a 26 átomos entre a y b; en donde dicho marco puede incluir una o más cadenas lineales y-o ramificadas y-o anillos y está opcionalmente sustituido en cualquier átomo(s) de C disponible(s) por uno o más F; y W es una unidad de unión al cereblon de la ligasa de ubiquitina E3.
CL2025002736A 2023-03-10 2025-09-09 Compuestos bifuncionales capaces de degradar receptores de andrógenos CL2025002736A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202363489528P 2023-03-10 2023-03-10

Publications (1)

Publication Number Publication Date
CL2025002736A1 true CL2025002736A1 (es) 2026-01-02

Family

ID=90364229

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2025002736A CL2025002736A1 (es) 2023-03-10 2025-09-09 Compuestos bifuncionales capaces de degradar receptores de andrógenos

Country Status (16)

Country Link
EP (1) EP4676922A1 (es)
JP (1) JP2026510359A (es)
KR (1) KR20250154418A (es)
CN (1) CN120835881A (es)
AR (1) AR132085A1 (es)
AU (1) AU2024235906A1 (es)
CL (1) CL2025002736A1 (es)
CO (1) CO2025013819A2 (es)
CR (1) CR20250426A (es)
DO (1) DOP2025000220A (es)
IL (1) IL323195A (es)
MX (1) MX2025010560A (es)
PE (1) PE20252537A1 (es)
TW (1) TW202502749A (es)
UY (1) UY40670A (es)
WO (1) WO2024189488A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025125575A1 (en) 2023-12-14 2025-06-19 Astrazeneca Ab Irak4 protacs

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110506039A (zh) 2016-10-11 2019-11-26 阿尔维纳斯股份有限公司 用于雄激素受体靶向降解的化合物和方法
WO2021061644A1 (en) * 2019-09-23 2021-04-01 Accutar Biotechnology Inc. Novel substituted quinoline-8-carbonitrile derivatives with androgen receptor degradation activity and uses thereof
JP7307796B2 (ja) * 2019-09-23 2023-07-12 アキュター バイオテクノロジー インコーポレイテッド アンドロゲン受容体分解活性を有する新規の置換キノリン－８－カルボニトリル誘導体およびその使用
WO2021231927A1 (en) * 2020-05-14 2021-11-18 The Regents Of The University Of Michigan Androgen receptor protein degraders with a tricyclic cereblon ligand

Also Published As

Publication number Publication date
KR20250154418A (ko) 2025-10-28
EP4676922A1 (en) 2026-01-14
WO2024189488A1 (en) 2024-09-19
MX2025010560A (es) 2025-10-01
CR20250426A (es) 2025-11-21
CO2025013819A2 (es) 2025-10-20
TW202502749A (zh) 2025-01-16
JP2026510359A (ja) 2026-04-02
PE20252537A1 (es) 2025-10-27
AR132085A1 (es) 2025-05-21
AU2024235906A1 (en) 2025-10-30
UY40670A (es) 2024-09-13
IL323195A (en) 2025-11-01
DOP2025000220A (es) 2025-10-31
CN120835881A (zh) 2025-10-24

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