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：
PE0000032012
公开号：
PE05752012A1
申请日:
2010.07.02
申请国别(地区):
PE
年份:
2012
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 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 Y SON UTILES EN EL TRATAMIENTO DE CANCER, POLICITEMIA VERA, MIELOFIBROSIS, ENFERMEDAD DE CHRON, ARTRITIS REUMATOIDE,
