AMINOPYRIDYLOXYPYRAZOLE COMPOUNDS

• Main Authors: Craig D. WOLFANGEL, David A. COATES, Sajan JOSEPH, Huaxing PEI, Saravanan PARTHASARATHY, Gaiying ZHAO, William T. MCMILLEN, Jason Scott SAWYER, Douglas W. BEIGHT
• Format: Patent
• Language: English; Spanish
• Published: 16.08.2019
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to novel aminopyridyloxypyrazole compounds that inhibit the activity of transforming growth factor beta receptor 1 (TGFpRI), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, preferably colon cancer, melanoma, hepatocellular carcinoma, renal cancer, glioblastoma, pancreatic cancer, myelodysplastic syndrome, lung cancer, and gastric cancer, and/or fibrosis, preferably liver fibrosis and chronic kidney disease. La presente invención se refiere a compuestos novedosos de aminopiridiloxipirazol que inhiben la actividad del receptor 1 del factor del crecimiento transformante beta (TGFßR1), composiciones farmacéuticas que comprenden los compuestos y métodos para utilizar los compuestos para tratar cáncer, preferentemente cáncer de colon, melanoma, carcinoma hepatocelular, cáncer renal, glioblastoma, cáncer de páncreas, síndrome mielodisplásico, cáncer de pulmón y cáncer gástrico y/o fibrosis, preferentemente fibrosis hepática y enfermedad renal crónica.