BROTHERTON-PLEISS, CHRISTINE,JAIME-FIGUEROA, SAUL,LOPEZ-TAPIA, FRANCISCO JAVIER,LOU, YAN,OWENS, TIMOTHY D.
申请号：
PE0002202014
公开号：
PE08652014A1
申请日:
2012.08.14
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Relates to Heterocyclic compounds of formula (i) where X is n, CH, CH2, among others R IS h, R1, among others, where R1 is cycloalkyl, aryl, heteroaryl, among others and, Y1 and Y2 are each CH o n Y3 is H or F Y4 is y4a, y4b, among others, where H is y4a is alkyl or Halogen y4b in Lower optionally replaced with Halogen, Hydroxy, CN, among others.Preferred compounds are: 6 - 8 - Tert Butyl fluoride - 2 - 3 - 4 - (hydroxymethyl) - [1 - (1 - methyl - 5 - methyl - 1 , 2 , 3, 4 , 5, 6 - - hexahidro [3,4] bipiridinil - 6 - ilamino) - 6 - oxo - 1.6 - dihydro - pyridazin-3 - il - 3] pyridin-2-yl) - 2H - ftalazin ONA - 1 - 6 - Tert Butyl fluoride - 8 - 2 - 3 - (hydroxymethyl) - 4 - (1 - methyl - 5 - [5 - (((S) - 1 - Methyl - pyrrolidin-2-one il) - P Iridin ilamino] - 6 - 2 - oxo - 1.6 - dihydro - il - 3} pyridazin-3 pyridin-2-yl) - 2H - ftalazin - 1 - One among others.It also relates to a Pharmaceutical composition. These compounds are inhibitors of the tyrosine kinase Bruton (BTK) being useful in the treatment of rheumatoid arthritis, asthmaSE REFIERE A COMPUESTOS HETEROCICLOS DE FORMULA (I) DONDE X ES CH, CH2, N, ENTRE OTROS R ES H, R1, ENTRE OTROS, EN DONDE R1 ES ARILO, HETEROARILO, CICLOALQUILO, ENTRE OTROS A, Y, Y1 E Y2 SON CADA UNO CH O N Y3 ES H O F Y4 ES Y4a, Y4b, ENTRE OTROS, EN DONDE Y4a ES H O HALOGENO Y4b ES ALQUILO INFERIOR OPCIONALMENTE SUSTITUIDO CON HALOGENO, HIDROXI, CN, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-TERT-BUTIL-8-FLUOR-2-{3-HIDROXIMETIL-4-[1-METIL-5-(1-METIL-1,2,3,4,5,6-HEXAHIDRO-[3,4]BIPIRIDINIL-6-ILAMINO)-6-OXO-1,6-DIHIDRO-PIRIDAZIN-3-IL]-PIRIDIN-2-IL}-2H-FTALAZIN-1-ONA 6-TERT-BUTIL-8-FLUOR-2-(3-HIDROXIMETIL-4-{1-METIL-5-[5-((S)-1-METIL-PIRROLIDIN-2-IL)-PIRIDIN-2-ILAMINO]-6-OXO-1,6-DIHIDRO-PIRIDAZIN-3-IL}-PIRIDIN-2-IL)-2H-FTALAZIN-1-ONA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA TIROSINA QUINASA DE BRUTON (BTK) SIENDO UTILES EN EL TRATAMIENTO DE ARTRITIS REUMATOIDE, ASMA
