ALEXANDER HIRD,MICHELLE LAMB,CHRISTOPHER DE SAVI,KURT GORDON PIKE,JANET HAWKINS,MELISSA MARIE VASBINDER,BERNARD CHRISTOPHER BARLAAM
申请号：
DO2018000207
公开号：
DOP2018000207A
申请日:
2018.09.25
申请国别(地区):
DO
年份:
2018
代理人:
摘要：
A series of novel pyridines or pyrimidine derivatives with chemical formula (I) are provided, these derivatives inhibit CDK9 and can be used for treating hyperproliferative disease. Specifically, these compounds are useful in the treatment of following proliferative disease, the proliferative disease is such as cancer, including malignant hematologic disease, such as acute myelocytic leukemia, Huppert's disease, chronic lymphocytic leukemia, diffusivity large B cell lymphoid tumor, Burkitt lymphoma, follicular lymphoma and solid tumor such as breast cancer, lung cancer, neuroblastoma and colon cancer. A is C (R5) or N； R5 is H, C1-3 alkyl, CN or halogen； R2 is optionally substituted 3-7 membered heterocycloalkyls or 3-7 member naphthenic base； R4 is (A) or (B), wherein X and Y and their atoms of attachment thereon are formed together optionally substituted, saturation or fractional saturation 5 to 7 membered heterocycloalkyl rings, other than bridge nitrogen, which may include one or two hetero atom for being selected from N, O and S； J is N or CR11； And R11 is H or C1-3 alkyl.Se provee una serie de derivados novedosos de piridina o pirimidina que inhiben CDK9 y pueden se útiles para el tratamiento de enfermedades hiperproliferativas. En particular, los compuestos son útiles en el tratamiento de enfermedades proliferativas como por ejemplo cáncer, incluyendo trastornos hematológicos malignos, como por ejemplo leucemia mieloide aguda, mieloma múltiple, leucemia linfocítica crónica, linfoma difuso de células B grandes, linfoma de Burkitt, linfoma folicular y tumores sólidos como por ejemplo cáncer de mama, cáncer de pulmón, neuroblastoma y cáncer de colon.
