ALTMAN, MICHAEL D.,ANDRESEN, BRIAN M.,ARRINGTON, KENNETH L.,KALEEN KONRAD, CHILDERS,DI FRANCESCO, MARIA EMILIA,DONOFRIO, ANTHONY,ELLIS, JOHN MICHAEL,FISCHER, CHRISTIAN,GUERIN, DAVID JOSEPH,HAIDLE, AND
申请号：
PE0008382012
公开号：
PE14802012A1
申请日:
2010.12.15
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Aminopirimidinas refers to compounds of formula (i) where p is 0 to 4 Q is 0 to 2 CY is cycloalkyl (c4-c7), oxetanilo, pirrolidinilo, piperidinilo, among others r1 is H, alkyl (c1-c4), haloalquilo (c1-c4), cycloalkyl (C3 and C6), among others R4 is h, alkyl (c1-c4) or cicloalqu ILO (C3 - C4) ry () is aminometilo, Oh, OCH3, F, among others RZ (a) is fluoroalquilo (C1 - C3), halogen,CN, alkyl (c1-c4), among others.Preferred compounds are: acid (1R, 4S) - 4 - [5 - (3 - 2-cyclopropyl-1 - 5 - ((4 - (trifluoromethyl) pyrimidine il] amino} - 2 - phenyl) - 1,3 - thiazol-2-yl] - 4 - hydroxy - 2.2 - dimetilciclohexanocarboxilico acid (1S, 4R) - 4 - hydroxy - 2,2-dimethyl - [4 - (5 - 3 - methyl - 5 - (4 - methyl - 2 - ilamino - pyrimidin-2-yl) - phenyl] thiazol-2-yl} - ciclohexanocarboxilico 5 - hydroxy - 3 - [5 - (2 - methyl - 5 - ((4 - (trifluoromethyl) pyrimidine IL - 2 - phenyl] amino} - 1)3 - Azepan thiazol-2-yl] - 2 - One among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of Spleen Tyrosine Kinase (SYK) being useful in the treatment of Asthma, ulcerative colitis, dermatitis, psoriasisSE REFIERE A COMPUESTOS DERIVADOS DE AMINOPIRIMIDINAS DE FORMULA (I) DONDE p ES DE 0 A 4 q ES DE 0 A 2 Cy ES CICLOALQUILO(C4-C7), OXETANILO, PIRROLIDINILO, PIPERIDINILO, ENTRE OTROS R1 ES H, ALQUILO(C1-C4), HALOALQUILO(C1-C4), CICLOALQUILO(C3-C6), ENTRE OTROS R4 ES H, ALQUILO(C1-C4) O CICLOALQUILO(C3-C4) Ry(a) ES AMINOMETILO, OH, OCH3, F, ENTRE OTROS Rz(a) ES FLUOROALQUILO(C1-C3), HALOGENO, CN, ALQUILO(C1-C4), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO (1R,4S)-4-[5-(3-CICLOPROPIL-5-{[4-(TRIFLUOROMETIL)PIRIMIDIN-2-IL]AMINO}FENIL)-1,3-TIAZOL-2-IL]-4-HIDROXI-2,2-DIMETILCICLOHEXANOCARBOXILICO ACIDO (1S,4R)-4-HIDROXI-2,2-DIMETIL-4-{5-[3-METIL-5-(4-METIL-PIRIMIDIN-2-ILAMINO)-FENIL]-TIAZOL-2-IL}-CICLOHEXANOCARBOXILICO 5-HIDROXI-5-[5-(3-METIL-5-{[4-(TRIFLUOROMETIL)PIRIMIDIN-2-IL]AMINO}FENIL)-1,3-TIAZOL-2-IL]AZEPAN-2-ONA ENTRE OTROS. TAMBIEN SE REFIERE A
