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DERIVADOS DE 2,4-DIAMINO-PIRIMIDINA N2, N4-DISUSTITUIDOS COMO INHIBIDORES DE JAK3
专利权人:
RIGEL PHARMACEUTICALS; INC.
发明人:
LI, HUI,HECKRODT, THILO, J.,CHEN, YAN,MCMURTRIE, DARREN JOHN,TAYLOR, VANESSA,SINGH, RAJINDER,DING, PINGYU,THOTA, SAMBAIAH,YEN, ROSE
申请号:
PE0003612015
公开号:
PE06212015A1
申请日:
2010.01.22
申请国别(地区):
PE
年份:
2015
代理人:
摘要:
The Invention relates to Derivatives of pyrimidine compounds of formula (i) where X and y are each or s, S (OR), among others, the ring a is aryl or heteroaryl (C6 C10) from 5 to 10 members R2 is H, re, RB, among others, where re (C1 - C6 alkyl, cycloalkyl, aryl (C3 - C8) (C6 C10), among others Ra is H, alkyl (C1 - C6), heteroaryl 5 to 15 members p is 0 to 4 Z1 and Z2 are each CHCR2 or N R3 and R4 are each h, alkyl (C1 - C6) optionally replaced, among others R5 is Halo, CN (C1 - C6), alkyl, Nitro, among others.Preferred compounds are: N4 - (1,3 - dimetilbenzimidazolin - 2 - on - 5 - yl) - N2 - ((4 - metilsulfonilamino) phenyl) - 5 - fluoropyrimidine - 2.4 - diamine 5 - [2 - (2.4 - difluoro - 5 - methoxy phenylamino) - 5 - methyl - 4 - pyrimidine ilamino] - 3H - benzoxazole - 2 - One 5 - (2 - (4 - (1 - (ciclopropilamino) ethyl) phenylamino) - 5 - metilpirimidin - 4 - ilamino) Ben Zo [d] oxazole - 2 (3H) - One among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of jak Kinases being useful in the treatment of T Cell mediated autoimmune disease, Transplantation of Allograft RejectionLA INVENCION SE REFIERE A COMPUESTOS DERIVADOS DE PIRIMIDINA DE FORMULA (I) DONDE X E Y SON CADA UNO O, S, S(O), ENTRE OTROS EL ANILLO A ES ARILO(C6-C10) O HETEROARILO DE 5 A 10 MIEMBROS R2 ES H, Re, Rb, ENTRE OTROS, EN DONDE Re ES ALQUILO(C1-C6), CICLOALQUILO(C3-C8), ARILO(C6-C10), ENTRE OTROS Ra ES H, ALQUILO(C1-C6), HETEROARILO DE 5 A 15 MIEMBROS p ES DE 0 A 4 Z1 Y Z2 SON CADA UNO CH, CR2 O N R3 Y R4 SON CADA UNO H, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO, ENTRE OTROS R5 ES HALO, CN, ALQUILO(C1-C6), NITRO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N4-(1,3-DIMETILBENZIMIDAZOLIN-2-ON-5-IL)-N2-((4-METILSULFONILAMINO)FENIL)-5-FLUOROPIRIMIDINA-2,4-DIAMINA 5-[2-(2,4-DIFLUORO-5-METOXI-FENILAMINO)-5-METIL-PIRIMIDIN-4-ILAMINO]-3H-BENZOXAZOL-2-ONA 5-(2-(4-(1-(CICLOPROPILAMINO)ETIL)FENILAMINO)-5-METILPIRIMIDIN-4-ILAMINO)BENZO[d]OXAZOL-2(3H)-ONA ENTRE OTROS. TAM
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