JAMES D. RODGERS,STACEY SHEPARD,THOMAS P. MADUSKUIE,HAISHENG WANG,NIKOO FALAHATPISHEH,MARIA RAFALSKI,ARGYRIOS G. ARVANITIS,LOUIS STORACE,RAVI KUMAR JALLURI,JORDAN S. FRIDMAN,KRISHNA VADDI,James D. Rodgers,Stacey Shepard,Thomas P. Maduskuie,Haisheng Wang,Nikoo Falahatpisheh,Maria Rafalsk
申请号：
HRP20110903
公开号：
HRP20110903T1
申请日:
2011.12.01
申请国别(地区):
HR
年份:
2012
代理人:
摘要：
The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines (I) and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Spoj formule I: ili njegova farmaceutski prihvatljiva sol, naznačen time da: T, U, i V su nezavisno odabrani od O, S, N, CR5, i NR6；pri čemu 5-člani prsten koji formira atom ugljika, atom dušika, U, T, i V je aromatski； X je N ili CR4；n je 0； ilin je I i Y je C1-8alkilen, C2-8alkenilen, (CR11R12)pC(O)(CR11R12)q, (CR11R12)pC(O)NRc(CR11R12)q, (CR11R12)pC(O)O(CR11R12)q, ili (CR11R12)pOC(O)(CR11R12)q, pri čemu navedeni C1-8alkilen ili C2-8alkenilen, je proizvoljno supstituiran sa 1, 2, ili 3 halo, OH, CN, amino, C1-4alkilamino, ili C2-8dialkilamino； Z je aril, cikloalkil, heteroaril, ili heterocikloalkil, svaki proizvoljno supstituiran sa 1, 2, 3, 4, 5, ili 6 nezavisnih supstituenata odabranih od halo, C1-4 alkila, C2-4 alkenila, C2-4 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, C1-4 cijanoalkila, Cy1, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRcRd, NRcC(O)ORa, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb, i S(O)2NRcRd；Cy1 je nezavisno odabran od arila, heteroarila, cikloalkila, i heterocikloalkila, svaki proizvoljno supstituiran sa 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-4 alkila, C2-4 alkenila, C2-4 alkinila, C1-4 haloalkila, CN, NO2, ORa, SRa, C(O)Rb , C(O)NRcRd", C(O)ORa", OC(O)Rb", OC(O)NRc"Rd", NRc" Rd", NRc"C(O)Rb", NRc"C(O)ORa" S(O)Rb", S(O)NRcRd", S(O)2Rb", i S(O)2NRc"Rd"；R4 je H； R5 je H, halo, C1-4alkil, C2-4alkenil, C2-4alkinil, C1-4haloalkil, CN, NO2, OR7, SR7, C(O)R8, C(O)NR9R10, C(O)OR7,OC(O)R8, OC(O)NR9R10, NR9R10, NR9C(O)R8, NR9C(O)OR7, S(O)R8, S(O)NR9R10 S(O)2R8, NR9S(O)2R8 ili S(O)2NRR10；R6 je H, C1-4al
