RODGERS, JAMES D.,SHEPARD, STACEY,ZHU, WENYU,SHAO, LIXIN,GLENN, JOSEPH
申请号：
PE0012202013
公开号：
PE01462014A1
申请日:
2011.11.18
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Refers to compounds derived from pirrolopiridina and pirrolopirimidina replaced with ciclobutilo of formula (i) where X and W are each CH or N and CN, is H, alkyl (C1 - C3), among others l is o, S, C (= o) C (= o), or between other CR4 Z is o n, R1, R2, R3 and R4 are each Hydroxy alkyl, Halo, h, C 1 - C3), among others R5 is Hydroxy, alkoxy (c1-c4), F, alkyl (c1-c4), among others is H,(C1 - C6 alkyl, cycloalkyl, aryl (C3 - C10) (C6 C10), among others M is 0 to 2 n is 0 to 4.Preferred compounds are: 3 - [(4 - [3 - (cyanomethyl) - 3 - [4 - (7H pyrrolo [2,3-d] pyrimidin-4-yl) - 1H pyrazol-1-yl) cyclobutyl] piperazin-1-yl) methyl] - 3 - [5 - fluorobenzonitrilo (4 - (3 - (cyanomethyl) - 3 - [4 - (7h pyrrolo [2,3-d] pyrimidin-4-yl) - 1H pyrazol-1-yl) cyclobutyl] piperazin-1-yl) methyl] - 6 - (dimethylamino) - 2 - fluorobenzo Nitrile 4 - (3 - (cyanomethyl) - 3 - [4 - (7H pyrrolo [2,3 - d] pyrimidin-4-yl) - 1H pyrazol-1-yl] cyclobutyl} - N - fluoro - 2 - [4 - (trifluoromethyl) phenyl] - 1 - piperazin carboxamide among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of Janus Kinase (JAK) being useful in the treatment of Multiple sclerosis, rheumatoid arthritis, cancer, myelofibrosisSE REFIERE A COMPUESTOS DERIVADOS DE PIRROLOPIRIDINA Y PIRROLOPIRIMIDINA SUSTITUIDOS CON CICLOBUTILO DE FORMULA (I) DONDE X Y W SON CADA UNO CH O N Y ES H, CN, ALQUILO(C1-C3), ENTRE OTROS L ES O, S, C(=O), C(=O)O, ENTRE OTROS Z ES CR4 O N R1, R2, R3 Y R4 SON CADA UNO H, HIDROXI, HALO, ALQUILO(C1-C3), ENTRE OTROS R5 ES HIDROXI, ALCOXI(C1-C4), F, ALQUILO(C1-C4), ENTRE OTROS A ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C10), ARILO(C6-C10), ENTRE OTROS m ES DE 0 A 2 n ES DE 0 A 4. SON COMPUESTOS PREFERIDOS: 3-[(4-{3-(CIANOMETIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]CICLOBUTIL}PIPERAZIN-1-IL)METIL]-5-FLUOROBENZONITRILO 3-[(4-{3-(CIANOMETIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]CICLOBUTIL}PIPERAZIN-1-IL)METIL]-6-(DIMETILAMINO)-2-FLUO
