Hydrazino 1H-imidazoquinolin-4-amines and conjugates made therefrom

摘要

1H-Imidazo[4,5-c]quinolin-4-amines substituted at the 1-position with a substituent bearing a hydrazinobenzamide or hydrazinonicotinamide, a salt thereof, or a protected hydrazinobenzamide or hydrazinonicotinamide and conjugates made from such compounds are disclosed. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed.

主权项

1. A conjugate comprising a reaction product of an aldehyde-bearing antigen and a compound or salt of formula:wherein:
X is alkylene having up to 8 carbon atoms optionally interrupted or terminated by —O—; R2 is hydrogen, alkyl, alkoxyalkylenyl, alkylaminoalkylenyl, or hydroxyalkylenyl; A is CH or N: R is halogen, hydroxyl, alkyl, haloalkyl, or alkoxy; and n is an integer from 0 to 4;or a pharmaceutically acceptable salt thereof.