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：
PE0006922015
公开号：
PE12492015A1
申请日:
2010.07.02
申请国别(地区):
PE
年份:
2015
代理人:
摘要：
Referring to a pirazolopirimidina derivative Compound of formula (i), wherein R1 is H, alkyl of C1 - C6, or6, nr6r7 or Halogen R2 is a heteroaryl of 5 or 6 members optionally substituted cycloalkyl R4 R3 is phenyl C3, C6, heterociclilo 3 to 10 members, among others R4 is C1 to C6 alkyl -, Lquenilo C2 - C6, alquinilo C2 - C6, among others R6 and R7 are h, alkyl of C1 - C6, alquinilo C2 - C6, NS,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 - 1 - pyrazole - 4-yl) pyrazolo [1,5-a] pyrimidine - 3 - carboxamide, N - (3 - (2.5 - dimetilofenil) - 1 - methyl - 1h-pyrazol-4-yl) pyrazolo [1,5-a] - 3 - carboxa pyrimidine Measure, among others. It also relates to a Pharmaceutical composition.These compounds inhibit one or more Janus Kinase (jak Kinases), and are useful in the treatment of cancer, polycythemia vera, myelofibrosis, Crohns disease, rheumatoid arthritis, Primary thrombocytosis, among othersReferida 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
