DERIVADOS DE 6-TERT-BUTIL-8-FLUOR-2-(2-HIDROXIMETIL-3-{1-METIL-5-PIRIDIN-2-IL-AMINO-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL}-FENIL)-FTALAZIN-1-ONA COMO INHIBIDORES DE LA TIROSINA-QUINASA DE BRUTON
BERTHEL, STEVEN JOSEPH,FISHLOCK, DANIEL,FIROOZNIA, FARIBORZ,HONG, JUN-BAE,LOU, YAN,LUCAS, MATTHEW,OWENS, TIMOTHY D.,SARMA, KESHAB,SWEENEY, ZACHARY KEVIN,TAYGERLY, JOSHUA PAUL GERGELY
申请号：
PE0015512011
公开号：
PE00812012A1
申请日:
2010.02.25
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Relates to Heterocyclic compounds of formula (a) wherein R IS h, - - - - R1 R2 R1, R3, among others, where R1 is cycloalkyl, aryl, heteroaryl, among others R2 is - C (= o) - NHC (= o) or - S (= o) 2, among others R3 is H or alkyl R4 R4, where is lower, Lower alkoxy, amino, among others and OS X X Each CH N o n y1 is H, alkyl or lower than haloalquilo y2 and Y2 are each HalogenOptionally substituted with lower alkyl oxime or lower alkoxy, halogen, Hydroxy, among others n is 0 to 2 Z * is a compound of formula (IA) (IIA), among others, where is y3 h, halogen or lower alkyl M is 0 to 1 and is Halogen, Hydroxy Lower alkyl, Y4 is y4a, among others Y4b, among others, where H is y4a Lower alkyl or Halogen y4b is optionally substituted.Preferred compounds are: 2 - (3 - (5 - [5 - (1 - amino - 1 - methyl - ethyl) - pyridin - 2 - ilamino] - 1 - methyl - 2 - oxo - 1.6 - dihydro - pyridin-3-yl) - phenyl - 2 - 6 - Hydroxymethyl TERT) butyl - 8 - fluor - 2H - 1 - 6 - ftalazin ona Tert Butyl 2 - (3 - (5 - [4 - (ethylamino) - 1 - 1 - methyl - ethyl) - pyridin - 2 - ilamino] - 1 - methyl - 2 - oxo - 1.6 - dihydro - pyridin - 3 - 2 - Hydro - il} Ximetil - phenyl) - 8 - fluor - 2H - ftalazin - 1 - One among others.It also relates to a preparation method and a Pharmaceutical composition. These compounds are inhibitors of the tyrosine kinase Bruton (BTK) being useful in the treatment of rheumatoid arthritis, psoriasis, asthmaSE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (A) DONDE R ES H, -R1, -R1-R2-R3, ENTRE OTROS, EN DONDE R1 ES ARILO, HETEROARILO, CICLOALQUILO, ENTRE OTROS R2 ES -C(=O), -NHC(=O)O, -S(=O)2, ENTRE OTROS R3 ES H O R4, EN DONDE R4 ES ALQUILO INFERIOR, ALCOXI INFERIOR, AMINO, ENTRE OTROS X Y X SON CADA UNO CH O N Y1 ES H, ALQUILO INFERIOR O HALOALQUILO INFERIOR Y2 E Y2 SON CADA UNO HALOGENO, OXIMA O ALQUILO INFERIOR OPCIONALMENTE SUSTITUIDO CON HIDROXI, ALCOXI INFERIOR, HALOGENO, ENTRE OTROS n ES DE 0 A 2 Z* ES UN COMPUESTO DE FORMULA (Ia), (IIa), ENTRE OTROS, EN DONDE
