PE20252585A1 - G PROTEIN-COUPLED RECEPTOR KINASE 2 (GRK2) DEGRADATION COMPOUNDS AND THEIR USES - Google Patents
G PROTEIN-COUPLED RECEPTOR KINASE 2 (GRK2) DEGRADATION COMPOUNDS AND THEIR USESInfo
- Publication number
- PE20252585A1 PE20252585A1 PE2025001718A PE2025001718A PE20252585A1 PE 20252585 A1 PE20252585 A1 PE 20252585A1 PE 2025001718 A PE2025001718 A PE 2025001718A PE 2025001718 A PE2025001718 A PE 2025001718A PE 20252585 A1 PE20252585 A1 PE 20252585A1
- Authority
- PE
- Peru
- Prior art keywords
- grk2
- protein
- degradation
- coupled receptor
- receptor kinase
- 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
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non 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
-
- 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
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- C07D417/00—Heterocyclic 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
- C07D417/14—Heterocyclic 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se refiere a compuestos de degradacion de la cinasa 2 del receptor acoplado a proteinas G (GRK2) o una sal farmaceuticamente aceptable, un isomero, un isotopo, un profarmaco, un solvato, o un polimorfo de este, composiciones farmaceuticas que comprenden los mismos, kits que comprenden los mismos, y usos de los mismos para prevenir o tratar enfermedades o afecciones al menos parcialmente medicadas por GRK2 o que pueden beneficiarse de la degradacion de GRK2. Se trata de un compuesto de Formula (1): GBM-DT (1) o una sal farmaceuticamente aceptable, un isomero, un isotopo, un profarmaco, un solvato o un polimorfo de este; en donde: GBM es un resto de union a GRK2; y DT es una etiqueta de degradacion que tiene capacidad de union a la ligasa E3.This refers to G protein-coupled receptor kinase 2 (GRK2) degradation compounds or a pharmaceutically acceptable salt, isomer, isotope, prodrug, solvate, or polymorph thereof, pharmaceutical compositions comprising the same, kits comprising the same, and uses thereof for preventing or treating diseases or conditions at least partially medicated by GRK2 or that may benefit from GRK2 degradation. It is a compound of Formula (1): GBM-DT (1) or a pharmaceutically acceptable salt, isomer, isotope, prodrug, solvate, or polymorph thereof; wherein: GBM is a GRK2-binding residue; and DT is a degradation tag having E3 ligase-binding capability.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2023075491 | 2023-02-10 | ||
| PCT/CN2024/077138 WO2024165075A1 (en) | 2023-02-10 | 2024-02-09 | G protein-coupled receptor kinase 2 (grk2) degradation compounds and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20252585A1 true PE20252585A1 (en) | 2025-11-11 |
Family
ID=92262085
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2025001718A PE20252585A1 (en) | 2023-02-10 | 2024-02-09 | G PROTEIN-COUPLED RECEPTOR KINASE 2 (GRK2) DEGRADATION COMPOUNDS AND THEIR USES |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP4662211A1 (en) |
| KR (1) | KR20250139885A (en) |
| CN (1) | CN120917020A (en) |
| AU (1) | AU2024218793A1 (en) |
| IL (1) | IL322532A (en) |
| MX (1) | MX2025009366A (en) |
| PE (1) | PE20252585A1 (en) |
| WO (1) | WO2024165075A1 (en) |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2957226C (en) * | 2008-10-29 | 2018-08-14 | Celgene Corporation | Isoindoline compounds for use in the treatment of cancer |
| CA3174266A1 (en) * | 2020-05-27 | 2021-12-02 | Grazia Piizzi | Grk2 inhibitors and uses thereof |
| WO2022159688A1 (en) * | 2021-01-22 | 2022-07-28 | Cygnal Therapeutics, Inc. | Degraders of grk2 and uses thereof |
| WO2022200857A1 (en) * | 2021-03-22 | 2022-09-29 | Monte Rosa Therapeutics Ag | Pharmaceutical compositions for use in the prevention and treatment of a disease or disorder caused by or associated with one or more premature termination codons |
| EP4347860A1 (en) * | 2021-06-04 | 2024-04-10 | Monte Rosa Therapeutics, Inc. | E3 ligase fusion proteins for proximity detection |
| CN115504963A (en) * | 2021-06-22 | 2022-12-23 | 苏州开拓药业股份有限公司 | A c-Myc protein degradation agent |
| WO2023129564A1 (en) * | 2021-12-27 | 2023-07-06 | Cygnal Therapeutics, Inc. | Degraders of grk2 and uses thereof |
-
2024
- 2024-02-09 PE PE2025001718A patent/PE20252585A1/en unknown
- 2024-02-09 IL IL322532A patent/IL322532A/en unknown
- 2024-02-09 EP EP24752929.0A patent/EP4662211A1/en active Pending
- 2024-02-09 CN CN202480021341.9A patent/CN120917020A/en active Pending
- 2024-02-09 WO PCT/CN2024/077138 patent/WO2024165075A1/en not_active Ceased
- 2024-02-09 AU AU2024218793A patent/AU2024218793A1/en active Pending
- 2024-02-09 KR KR1020257030248A patent/KR20250139885A/en active Pending
-
2025
- 2025-08-08 MX MX2025009366A patent/MX2025009366A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN120917020A (en) | 2025-11-07 |
| IL322532A (en) | 2025-10-01 |
| EP4662211A1 (en) | 2025-12-17 |
| AU2024218793A1 (en) | 2025-08-21 |
| KR20250139885A (en) | 2025-09-23 |
| MX2025009366A (en) | 2025-11-03 |
| WO2024165075A1 (en) | 2024-08-15 |
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