Heteroaromatic derivatives having an inhibitory activity against HIV integrase
AssigneeShionogi & Co., Ltd.
InventorsToshio Fujishita, Tomokazu Yoshinaga, Akihiko Sato
Life of this patent
Estimating the term…
Abstract
A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteoaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.
Claims16
1-[5-(4-fluorobenzyl)furan-2-yl]-3-hydroxy-3-(1H-1,2,4-triazol-3-yl)-propenone.
A process for producing a compound of the formula (V):
- wherein A1 is 5-(4-fluorobenzyl)furan-2-yl, and A is C—W wherein W is hydrogen, which comprises reacting a compound of the formula (III):
- wherein A1 is as defined above, with a compound of the formula (IV):
- wherein A is as defined above, Q is a protective group and L is a leaving group, in the presence of a base, and deprotecting Q.
A compound of the formula:
- wherein Z2 is CH2 and R1 is 4-fluorobenzy.
A compound of the formula (IV):
- wherein A is C—W wherein W is hydrogen, Q is trityl and L is ethoxy.
Dependencies are inferred from the claim text.