COOKE, NIGEL GRAHAM,FERNANDES GOMES DOS SANTOS, PAULO,GRAVELEAU, NADEGE,HEBACH, CHRISTINA,HOGENAUER, KLEMENS,HOLLINGWORTH, GREGORY JOHN,SMITH, ALEXANDER BAXTER,SOLDERMANN, NICOLAS,STOWASSER, FRANK,STR
申请号:
PE0000172013
公开号:
PE06502013A1
申请日:
2011.07.06
申请国别(地区):
PE
年份:
2013
代理人:
摘要:
Referring to a pirido - tetrahydro - pyrimidine Derivative of formula (i), where y is u or NR1 r1 is phenyl, piridilo, pirimidinilo, pirazinilo, among others R2 is phenyl, naphthyl, piridilo, pirimidinilo,Among others R3 is H, c1-c4 alkyl or haloalquilo c1-c4 M is 0 OR 1.Preferred compounds are: {(S) - 3 - [6 - (4 - methoxy - 5 - methyl - pyridin-3-yl) - pirido - 5,6,7,8-tetrahydro - [4,3-d] - pyrimidine - 4 - iloxi pyrrolidin-1-yl]} - (Tetrahydro - piran - 4 - il - methanone,)2 - methoxy - 3 - (4 - [(S) - 1 - (4 - tetrahydro - piran - carbonyl) - pyrrolidin-3-yl] - 3 - iloxi - 7,8-dihydro-5h - pirido [4,3-d] pyrimidine - il - 6 nicotinonitrilo} - {3, 5 - [6 - (6 methoxy - 3 - methyl - pyridin-3-yl) - 5,6,7,8 - terahidro - pirido [4,3-d] - pyrimidine - iloxi pyrrolidin-3-yl] - 4 - 1 - carbonyl} - 1H - pyridin - 2 - ona, among others. It also relates to a Pharmaceutical Composition and a preparation method.These compounds are inhibitors of the 3 - Oh - phosphoinositide Kinase (PI3K) and are useful in the treatment of inflammatory, Allergic, autoimmune diseases, cancer, respiratory,Among otherREFERIDA A UN DERIVADO DE TETRAHIDRO-PIRIDO-PIRIMIDINA DE FORMULA (I), DONDE Y ES NR3 U O R1 ES FENILO, PIRIDILO, PIRIMIDINILO, PIRAZINILO, ENTRE OTROS R2 ES FENILO, NAFTILO, PIRIDILO, PIRIMIDINILO, ENTRE OTROS R3 ES H, ALQUILO C1-C4 O HALOALQUILO C1-C4 m ES 0 O 1. SON COMPUESTOS PREFERIDOS: {(S)-3-[6-(6-METOXI-5-METIL-PIRIDIN-3-IL)-5,6,7,8-TETRAHIDRO-PIRIDO-[4,3-d]-PIRIMIDIN-4-ILOXI]-PIRROLIDIN-1-IL}-(TETRAHIDRO-PIRAN-4-IL)-METANONA, 2-METOXI-5-{4-[(S)-1-(TETRAHIDRO-PIRAN-4-CARBONIL)-PIRROLIDIN-3-ILOXI]-7,8-DIHIDRO-5H-PIRIDO[4,3-d]PIRIMIDIN-6-IL}-NICOTINONITRILO, 5-{3-[6-(6-METOXI-5-METIL-PIRIDIN-3-IL)-5,6,7,8-TERAHIDRO-PIRIDO-[4,3-d]PIRIMIDIN-4-ILOXI]-PIRROLIDIN-1-CARBONIL}-1H-PIRIDIN-2-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA 3-OH-CINASA DE FOSFOINOSITIDA (PI3K) Y SON UTI