GIBBONS, PAUL,HANAN, EMILY,LIU, WENDY,LYSSIKATOS, JOSEPH P.,MAGNUSON, STEVEN R.,MENDONCA, ROHAN,PASTOR, RICHARD,RAWSON, THOMAS E.,SIU, MICHAEL,ZAK, MARK E.,ZHOU, AIHE,ZHU, BING-YAN
申请号：
PE2015000692
公开号：
PE20151249A1
申请日:
2010.07.02
申请国别(地区):
PE
年份:
2015
代理人:
摘要：
A compound made from a derivative of formula (I) pyrazolpyridin,where R1 is H, C1-C6 alkyl, OR6, NR6R7 or halogen； R2 is a 5- or 6-membered heteroaryl optionally substituted with R4； R3 is phenyl, C3-C6 cycloalkyl, 3-10 membered heterocyclyl, among others； R4 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, among others； R6 and R7 are H, C1-C6 alkyl, C2-C6 alkynyl, CN, among others. Preferred compounds are: N- (3- (5-chloro-2-methoxyphenyl) -1-methyl-1H-pyrazol-4-yl) pyrazolo [1,5-a] pyrimidine-3-carboxamide, N- (5- (5-chloro-2-methoxyphenyl) -1-methyl-1H-pyrazol-4-yl) pyrazolo [1,5-a] pyrimidine-3-carboxamide, N- (3- (2,5-dimethylphenyl) -1 -methyl-1H-pyrazol-4-yl) pyrazolo [1,5-a] pyrimidine-3-carboxamide,There are others A pharmaceutical composer was also mentioned These compounds inhibit one or more JAK quinaas,It is very useful in the treatment of cancer, polypeptide bacteria, gallbladder fibrosis, Crohn's disease, rheumatoid arthritis, primary thrombositis and so on.Referida a un compuesto derivado de pirazolopirimidina de formula (I), donde R1 es H, alquilo C1-C6, OR6, NR6R7 o halogeno； R2 es un heteroarilo de 5 o 6 miembros opcionalmente sustituido con R4； R3 es fenilo, cicloalquilo C3-C6, heterociclilo de 3 a 10 miembros, entre otros； R4 es alquilo C1-C6, alquenilo C2-C6, alquinilo C2-C6, entre otros； R6 y R7 son H, alquilo C1-C6, alquinilo C2-C6, CN, entre otros. son compuestos preferidos: N-(3-(5-cloro-2-metoxifenil)-1-metil-1H-pirazol-4-il)pirazolo[1,5-a]pirimidina-3-carboxamida, N-(5-(5-cloro-2-metoxifenil)-1-metil-1H-pirazol-4-il)pirazolo[1,5-a]pirimidina-3-carboxamida, N-(3-(2,5-dimetilofenil)-1-metil-1H-pirazol-4-il)pirazolo[1,5-a]pirimidina-3-carboxamida, entre otros. Tambien esta referida a una composicion farmaceutica. Dichos compuestos inhiben una o mas janus quinasas, (JAK quinasas), y son utiles en el tratamiento de cancer, policitemia vera, mielofibrosis, enfermedad de Chron, artritis reumatoide, trombocitosis primaria, entre otros
