Gurney, Mark,Hagen, Timothy,Mo, Xuesheng,Vellekoop, A.,Romero, Donna,Campbell, Robert,Walker, Joel,Zhu, Lei
申请号：
NZ70588113
公开号：
NZ705881A
申请日:
2013.10.24
申请国别(地区):
NZ
年份:
2018
代理人:
摘要：
The present invention relates to compounds and their use as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease. Specifically disclosed are compounds of structural Formula XI and their use in pharmaceutical compositions, and the preparation of medicaments for treating a subject, the Formula XI compounds defined as: (XI) or a salt thereof, wherein: Y is CH2 X is chosen from CH and N R3 is chosen from methyl, ethyl, trifluoromethyl, and cyclopropyl R4 is chosen from hydrogen and ethyl or R3 and R4, together with the atoms to which they are attached, join to form a 5 to 6 membered cycloalkyl or heterocycloalkyl of the form: V1 is chosen from CH2, N, O, SO2, and S V2 is chosen from a bond, N, O and CH2 R5 is either benzoxaborole, or is chosen from phenyl and pyridinyl, either of which is para-substituted with a substituent of the form R8-R9-(R10)a(R10)b, and is optionally substituted with a substituent R13 R8 is chosen from a bond and lower alkyl R9 is chosen from halogen, lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower alkoxy, lower haloalkoxy, cyano, -C(O)N-, S(O)2-, B(OH)2, 5-6 membered monocyclic heterocycloalkyl, and 5-6 membered monocyclic heteroaryl (R10)a and (R10)b are each independently chosen from null, hydrogen, halogen, trifluoromethyl, trifluoromethoxy, hydroxyl, lower hydroxyalkyl, cyano, oxo, lower alkyl, C(O)OH, and C(O)O lower alkyl R13 is chosen from halogen, hydroxy, lower alkyl, trifluoromethyl, lower alkoxy, trifluoromethoxy, NH2, and cyano R6 is chosen from 3-chlorophenyl, 5-chloro-2-thienyl, cyclopentyl optionally substituted with one or two R14, and cyclopentoxy optionally substituted with one or two R14 and each R14 is independently chosen from halogen, hydroxy, lower alkyl, trifluoromethyl, lower alkoxy, trifluoromethoxy, NH2, and cyano.
