BERNADINO, JOSEPH N.,O'TOOLE, DORIS C.,BAY, WILLIAM E.
申请号：
CA2402719
公开号：
CA2402719C
申请日:
2001.03.21
申请国别(地区):
CA
年份:
2012
代理人:
摘要：
The present invention relates to a method of preparing an alkylatedsalicylamide froma protected and activated salicylamide via a dicarboxylated salicylamideintermediate. The present invention also relates to dicarboxylic salicylamidedeliveryagent compounds for the delivery of active agents. Methods of administrationareprovided as well. A non limitative example of a particularly preferreddicarboxylatedsalicylamide may be represented by the formula:(see above formula)where R1, R2, R3, and R4 are independently hydrogen； halogen； C1-C4 alkoxy,optionally substituted with -OH or F； -OH； C1-C4 alkyl, optionally substitutedwith -OHor F； -COOH； -OC(O)CH3； -SO3H； nitrile； or -NR9R1O； R9 and R10 areindependently hydrogen, C1-C4 alkyl, or oxygen； R5 is a protecting group； R6is anactivating group； or R5 and R6 are combined to form a substituted orunsubstitutedcyclic group； R7 is a linear C1-C20 alkylene, a linear C2-C20 alkenylene, alinear C2-C20 alkynylene, a branched C3-C20 alkylene, a branched C3-C20 alkenylene, or abranched C3-C20 alkynylene, and comprises a CH unit that is substituted bysaid -COOR8 and COOR11 groups； R7 is optionally substituted with C1-C4 alkyl, C1-C4alkenyl, oxygen, nitrogen, sulfur, halogen, -OH, C1-C4 alkoxy, aryl,heteraryl, or vinyl；R7 is optionally interrupted with aryl, heteroaryl, vinyl, oxygen, nitrogen,or sulfur； R8and R11 are independently C1-C4 alkyl or C1-C4 haloalkyl； and R9 and R10 areindependently hydrogen, C1-C4 alkyl, or oxygen.
