BROWN, MATTHEW FRANK,CASIMIRO-GARCIA, AGUSTIN,CHE, YE,COE, JOTHAM WADSWORTH,FLANAGAN, MARK EDWARD,GILBERT, ADAM MATTHEW,UNWALLA, RAYOMAND JAL,LANGILLE, JONATHAN DAVID,MONTGOMERY, JUSTIN IAN,TELLIEZ, J
申请号：
PE0007232016
公开号：
PE12462016A1
申请日:
2014.11.20
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
Refers to compounds of acrylamide pirrolo [2,3-d] pirimidinilo, pirrolo [2,3-b] pirazinilo and pirrolo [2,3-d] pyridinyl of formula (i) where R2 is H, alkyl deuterium, C1 - C6, among others R3 is H, halogen, deuterium, among others it is - crarb) - Q (crcrd), Where ra, RB, RC and Rd are each h, alkyd ILO C1 - C6, among others R0, R1, R4, R5, R6, R7, R8, R9 and R10 are each h, alkyl of C1 - C6Aryl C6 C10, among others R11 is H or deuterium and o u n one of the dotted links to Z and Z is a single link Z and Z are each C, N or cr16 where R16 is c1-c4 alkyl, aryl C6 C10, among others X is o, among others n, P and q are from 0 to 2.Preferred compounds are: 2 - (1 - acriloilpiperidin - 4 - ilamino) - N - isopropyl - 5h pyrrolo [2,3-b] pyrazine - 7 - carboxamide n - isopropyl - 2 - (3 - (N - metilacrilamido) azetidin - 1 - il) - 5h pyrrolo [2,3-b] pyrazine - 7 - carboxamide among Others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of Janus Kinase (JAK) being useful in the treatment of rheumatoid arthritis, Alzheimers diseaseSE REFIERE A COMPUESTOS ACRILAMIDAS DE PIRROLO[2,3-d]PIRIMIDINILO, PIRROLO[2,3-b]PIRAZINILO Y PIRROLO[2,3-d]PIRIDINILO DE FORMULA (I) DONDE R2 ES H, DEUTERIO, ALQUILO C1-C6, ENTRE OTROS R3 ES H, DEUTERIO, HALOGENO, ENTRE OTROS A ES -(CRaRb)q-(CRcRd)-, EN DONDE Ra, Rb, Rc Y Rd SON CADA UNO H, ALQUILO C1-C6, ENTRE OTROS R0, R1, R4, R5, R6, R7, R8, R9 Y R10 SON CADA UNO H, ALQUILO C1-C6, ARILO C6-C10, ENTRE OTROS R11 ES H O DEUTERIO Y ES O U N UNO DE LOS ENLACES PUNTEADOS A Z Y Z’ ES UN ENLACE INDIVIDUAL Z Y Z’ SON CADA UNO C, N O CR16, EN DONDE R16 ES ALQUILO C1-C4, ARILO C6-C10, ENTRE OTROS X ES O, ENTRE OTROS n, p Y q SON DE 0 A 2. SON COMPUESTOS PREFERIDOS: 2-(1-ACRILOILPIPERIDIN-4-ILAMINO)-N-ISOPROPIL-5H-PIRROLO[2,3-b]PIRAZINA-7-CARBOXAMIDA N-ISOPROPIL-2-(3-(N-METILACRILAMIDO)AZETIDIN-1-IL)-5H-PIRROLO[2,3-b]PIRAZINA-7-CARBOXAMIDA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON IN
