Triazolopiridinas Derivatives, Pharmaceutical compositions containing them, a process for preparing them, intermediaries that process and Use thereof for the treatment of autoimmune and inflammatory diseases
GRAHAM JAMES M.,HEUROU YVAN LE,LYON MICHAEL,ROBINSON JOHN E.,WALLACE ELI M.,WANG BIN,XU RUI,BLAKE JAMES F.,DLISLE ROBERT KIRK,DMEESE LISA A.
申请号：
ARP120100626
公开号：
AR085489A1
申请日:
2012.02.24
申请国别(地区):
AR
年份:
2013
代理人:
摘要：
Claim 1: a compound of the General formula (1), and stereoisomers, pharmaceutically acceptable Salts and solvates thereof, wherein: R1 is H, halogen, alkyl of C1 - CN, - 6, - 6 difluoroalquilo fluoroalquilo C1, C1 trifluoroalquilo C1 - 6, - 6, - 6 hidroxialquilo C1, C1 - cianoalquilo 6 (LAC Oxy c1-3 alkyl C1) - 6 (optionally substituted by Hydroxy), di (c1-3 alkyl alkoxy) - 6 - alkoxy C1, C1 6Fluoroalcoxi difluoroalcoxi C1 C1 - 6, - 6, - 6 hidroxialcoxi trifluoroalcoxi C1, C2 - 6, 6 - (alkoxy cianoalcoxi C1, C1 - C2 - alkoxy 3) 6, di (3 alkoxy C1 - C2 (alkoxy) - 6, 6 - methoxy cicloalquil C3), oxetanilmetoxi (optionally substituted methyl) (6 sulfanilo, C1 - alkyl) - C (= o) - nrarb, CH2C (= o) or cicloalqui nrcrd The C3 - 6 - CH2OH optionally substituted by alkyl or CH2O - C1 - ra, RB, 4)；RC and Rd are selected independently of H and c1-4 alkyl； R2 is H, alkyl or Halogen, CN, C1, C1 fluoroalquilo - 6, - 6, - 6 trifluoroalquilo difluoroalquilo C1, C1 - 6, 6 - (hidroxialquilo C1, C1 c1-3 alkyl alkoxy) - 6, 6 - alkoxy C1 (optionally substituted by alkyl C1 - 6) or C (= o) - (C1 - amino alkyl 6) or C (= o) -, or phenyl (c = o) -), or fluoroalcoxi C1 - 6, 6 - trifluoroalcoxi difluoroalcoxi C1, C1 - 6(6 hidroxialcoxi C2, C1 - C2 3 alkoxy (alkoxy) - 6, 6 - methoxy cicloalquil C3, C3 cicloalcoxi) - 6 (optionally replaced by OH), oxetanilmetoxi (optionally substituted by Methyl tetrahidropiraniloxi (C1), alkyl Hydroxy (- 6) sulfanilo, C2 - 6 sulfanilo, alkyl (alkyl) C1 - C2) 3sulfanil alkoxy - 6, - COOH, het AR1, - C (= o) nrerf, nrec (= o) - RFOxetanilo or ciclopropilo optionally replaced by CH2OH CH2O (alkyl - or - C1 - 6)； R1 and R2 together with Atoms that are United to form a Heterocyclic Ring of 5-6 members have 1 - 2 Ring heteroatoms are selected irrespective of o and N where the Ring Optionally substituted by alkyl c1-4, hetar1 is a heteroaryl Ring of 5-6 members have uNo or two nitrogen Atoms of the ring and is optionally substituted by one or more selected from al
