AR132032A1 - PYRIDAZINYL AMINO DERIVATIVES AS ALK5 RECEPTOR INHIBITORS - Google Patents
PYRIDAZINYL AMINO DERIVATIVES AS ALK5 RECEPTOR INHIBITORSInfo
- Publication number
- AR132032A1 AR132032A1 ARP240100519A ARP240100519A AR132032A1 AR 132032 A1 AR132032 A1 AR 132032A1 AR P240100519 A ARP240100519 A AR P240100519A AR P240100519 A ARP240100519 A AR P240100519A AR 132032 A1 AR132032 A1 AR 132032A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocycloalkyl
- oxo
- sulfanyl
- alk5
- alkylene
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
En términos generales, la presente invención se refiere a compuestos que inhiben el receptor tipo I del factor de crecimiento transformante b (TGF b) (ALK5) (en adelante inhibidores de ALK5), a métodos para preparar dichos compuestos, a composiciones farmacéuticas que los contienen y al uso terapéutico que se hace de ellos. Los compuestos de la invención pueden ser útiles, por ejemplo, en el tratamiento de muchas enfermedades, trastornos o afecciones que se asocian con la vía de señalización ALK5. Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptables, donde A es el grupo de fórmula A1; R¹ se selecciona del grupo que consta de -[2-(sulfanil)etil]-5-oxooxolano-3-carboxilato, -(2-oxo-2H-piran-6-il)metilsulfanilo, -(2-(1-(1-oxo-1H-isocromen-3-il)etoxi)etilsulfanil), -[(2-hidroxietil)sulfanil], -(((1-oxo-1H-isocromen-3-il)metil)sulfanil) y -[(1-oxo-3,4-dihidro-1H-2-benzopiran-3-il)metil]sulfanilo; R² es -NR³C(O)R⁴; R³ es H; R⁴ se selecciona del grupo que consta de -alquileno(C₁-C₆)-heterocicloalquilo(C₃-C₆), donde dicho -heterocicloalquilo(C₃-C₆) está opcionalmente sustituido por uno o más -alquilo(C₁-C₆); -alquileno(C₁-C₆)-heterocicloalquilo(C₃-C₆)-alquileno(C₁-C₆)-heterocicloalquilo(C₃-C₆), donde dicho -heterocicloalquilo(C₃-C₆) está opcionalmente sustituido por uno o más -alquilo(C₁-C₆) y oxo. Reivindicación 4: Una composición farmacéutica que comprende el compuesto de la fórmula (1) según cualquiera de las reivindicaciones 1 a 3, en mezcla con uno o más vehículos o excipientes farmacéuticamente aceptables.In general terms, the present invention relates to compounds that inhibit the transforming growth factor b (TGF b) type I receptor (ALK5) (hereinafter ALK5 inhibitors), to methods for preparing said compounds, to pharmaceutical compositions containing them and to the therapeutic use that is made of them. The compounds of the invention may be useful, for example, in the treatment of many diseases, disorders or conditions that are associated with the ALK5 signaling pathway. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein A is the group of formula A1; R¹ is selected from the group consisting of -[2-(sulfanyl)ethyl]-5-oxooxolane-3-carboxylate, -(2-oxo-2H-pyran-6-yl)methylsulfanyl, -(2-(1-(1-oxo-1H-isochromen-3-yl)ethoxy)ethylsulfanyl), -[(2-hydroxyethyl)sulfanyl], -(((1-oxo-1H-isochromen-3-yl)methyl)sulfanyl) and -[(1-oxo-3,4-dihydro-1H-2-benzopyran-3-yl)methyl]sulfanyl; R² is -NR³C(O)R⁴; R³ is H; R⁴ is selected from the group consisting of -(C₁-C₆)alkylene-(C₃-C₆)heterocycloalkyl, wherein said -(C₃-C₆)heterocycloalkyl is optionally substituted by one or more -(C₁-C₆)alkyl; -(C₁-C₆)alkylene-(C₃-C₆)heterocycloalkyl-(C₁-C₆)alkylene-(C₃-C₆)heterocycloalkyl, wherein said -(C₃-C₆)heterocycloalkyl is optionally substituted by one or more -(C₁-C₆)alkyl and oxo. Claim 4: A pharmaceutical composition comprising the compound of formula (1) according to any one of claims 1 to 3, in admixture with one or more pharmaceutically acceptable carriers or excipients.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP23159709 | 2023-03-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR132032A1 true AR132032A1 (en) | 2025-05-21 |
Family
ID=85461867
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP240100519A AR132032A1 (en) | 2023-03-02 | 2024-03-01 | PYRIDAZINYL AMINO DERIVATIVES AS ALK5 RECEPTOR INHIBITORS |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP4673213A1 (en) |
| AR (1) | AR132032A1 (en) |
| WO (1) | WO2024180207A1 (en) |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3947384B1 (en) | 2019-04-04 | 2023-11-01 | Chiesi Farmaceutici S.p.A. | Isochromene derivatives as phosphoinositide 3-kinases inhibitors |
| DK4182308T3 (en) | 2020-07-15 | 2024-10-21 | Chiesi Farm Spa | Pyridazinylamino derivatives as ALK5 inhibitors |
| IL307165A (en) * | 2021-03-26 | 2023-11-01 | Sumitomo Pharma Oncology Inc | Alk-5 inhibitors and uses thereof |
| US20250011299A1 (en) | 2021-09-21 | 2025-01-09 | Chiesi Farmaceutici S.P.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
| KR20240134173A (en) * | 2022-01-11 | 2024-09-06 | 키에시 파르마슈티시 엣스. 피. 에이. | Pyridazinyl amino derivatives as ALK5 inhibitors |
-
2024
- 2024-03-01 WO PCT/EP2024/055318 patent/WO2024180207A1/en not_active Ceased
- 2024-03-01 EP EP24707551.8A patent/EP4673213A1/en active Pending
- 2024-03-01 AR ARP240100519A patent/AR132032A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP4673213A1 (en) | 2026-01-07 |
| WO2024180207A1 (en) | 2024-09-06 |
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