CR20250426A - Compuestos bifuncionales capaces de degradar receptores de andrógenos - Google Patents
Compuestos bifuncionales capaces de degradar receptores de andrógenosInfo
- Publication number
- CR20250426A CR20250426A CR20250426A CR20250426A CR20250426A CR 20250426 A CR20250426 A CR 20250426A CR 20250426 A CR20250426 A CR 20250426A CR 20250426 A CR20250426 A CR 20250426A CR 20250426 A CR20250426 A CR 20250426A
- Authority
- CR
- Costa Rica
- Prior art keywords
- atom
- alkyl
- alkoxy
- atoms
- framework
- Prior art date
Links
Classifications
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- 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.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202363489528P | 2023-03-10 | 2023-03-10 | |
| PCT/IB2024/052251 WO2024189488A1 (en) | 2023-03-10 | 2024-03-08 | Bifunctional compounds capable of degrading androgen receptors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20250426A true CR20250426A (es) | 2025-11-21 |
Family
ID=90364229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20250426A CR20250426A (es) | 2023-03-10 | 2024-03-08 | 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025125575A1 (en) | 2023-12-14 | 2025-06-19 | Astrazeneca Ab | Irak4 protacs |
Family Cites Families (4)
| 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 |
-
2024
- 2024-03-08 WO PCT/IB2024/052251 patent/WO2024189488A1/en not_active Ceased
- 2024-03-08 AR ARP240100579A patent/AR132085A1/es unknown
- 2024-03-08 PE PE2025001965A patent/PE20252537A1/es unknown
- 2024-03-08 CR CR20250426A patent/CR20250426A/es unknown
- 2024-03-08 EP EP24711274.1A patent/EP4676922A1/en active Pending
- 2024-03-08 TW TW113108535A patent/TW202502749A/zh unknown
- 2024-03-08 CN CN202480017738.0A patent/CN120835881A/zh active Pending
- 2024-03-08 AU AU2024235906A patent/AU2024235906A1/en active Pending
- 2024-03-08 JP JP2025552091A patent/JP2026510359A/ja active Pending
- 2024-03-08 KR KR1020257030598A patent/KR20250154418A/ko active Pending
- 2024-03-11 UY UY0001040670A patent/UY40670A/es unknown
-
2025
- 2025-09-07 IL IL323195A patent/IL323195A/en unknown
- 2025-09-08 DO DO2025000220A patent/DOP2025000220A/es unknown
- 2025-09-08 MX MX2025010560A patent/MX2025010560A/es unknown
- 2025-09-09 CL CL2025002736A patent/CL2025002736A1/es unknown
- 2025-10-06 CO CONC2025/0013819A patent/CO2025013819A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20250154418A (ko) | 2025-10-28 |
| EP4676922A1 (en) | 2026-01-14 |
| WO2024189488A1 (en) | 2024-09-19 |
| CL2025002736A1 (es) | 2026-01-02 |
| MX2025010560A (es) | 2025-10-01 |
| 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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