COMPUESTOS DE TRIAZOLONA Y USOS DE LOS MISMOS

• Main Authors: STOCK, NICHOLAS SIMON, CHEN, AUSTIN CHIH-YU, JACINTHO, JASON DUARTE, BRAVO, YALDA MOSTOFI
• Format: Patent
• Language: Spanish
• Published: 22.09.2016
• 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

Se refiere a compuestos de formulas Ia y Ib, y sales farmaceuticamente aceptables de los mismos, en los cuales A1 es fenilo o piridilo; A2 es fenilo, un anillo heteroaromatico de 6 miembros conteniendo 1, 2 o 3 atomos de N, o un anillo heteroaromatico de 5 miembros conteniendo 1, 2, 3 o 4 heteroatomos independiente seleccionados de O, S y N, entre otros; X es –(CH2)m– o –(CH2)m–NH–(CH2)n–, en donde m y n son independientemente 0, 1, 2, 3 o 4, y m + n es 2, 3 o 4; R1 y R2 son independientemente H, halogeno, CN, CF3, alquilo C1–6 o cicloalquilo C3–6, entre otros; R5 es alquilo C1–6, arilo, heteroarilo, cicloalquilo C3–6 o alquenilo C2–6, entre otros; y R6 es arilo o heteroarilo, cada uno de ellos opcionalmente sustituido con 1 o 2 sustituyentes independientemente seleccionados entre halogeno, NO2, CF3, OCF3, alquilo C1–6 o CN, entre otros. Tambien se refiere a composiciones farmaceuticas que comprenden dichos compuestos de formula Ia o Ib, o sales de los mismos. Los compuestos de la invencion son antagonistas duales de PPAR-alfa y PPAR-delta, por lo cual son utiles en el tratamiento de canceres de prostata, mama, colon, pancreatico, leucemia linfocitica cronica humana, melanoma y otros. Asimismo, tambien son utiles en el tratamiento de infecciones virales, tales como infecciones por HCV e infecciones por VIH. The invention disclosed herein is directed to compounds of Formula (1a) and (1b) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocyticδ leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (1a) or (1b), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a therapeutically effective amount of a compound which is a dual antagonist of PPARα and PPARδ. The compounds and pharmaceutical compositions of the invention are also useful in the treatment of viral infections, such as HCV infections and HIV infections. The invention disclosed herein is also directed to a methods of preventing the onset of and/or recurrence of acute and chronic myeloid leukemia, as well as other cancers, comprising administration of a herapeutically effective amount of a dual antagonist of PPARα and PPARδ.