IP Library › Granted Patent US 8,580,967
Granted Patent B2
US 8,580,967 · App. 13/054,847 · Granted Nov 12, 2013

Methyl 3-(benzyloxy)-1-(2,2-dihydroxyethyl)-4-oxo-1,4-dihydropyridine-2-carboxylate and processes for the preparation thereof

Inventors: Brian Alvin Johns (Research Triangle Park, NC); Jason Gordon Weatherhead (Research Triangle Park, NC); Toshikazu Hakogi (Osaka, JP); Yasunori Aoyama (Osaka, JP)
Assignees: Shionogi & Co., Ltd.; VIIV Healthcare Company
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Quick Facts
Patent No.
US 8,580,967
App. No.
13/054,847
Granted
Nov 12, 2013
Kind
B2
Abstract

The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. For example, the present invention includes methyl 3-(benzyloxy)-1-(2,2-dihydroxyethyl)-4-oxo-1,4-dihydropyridine-2 -carboxylate of the formula P-8: and processes for the preparation thereof.

Claims (12)

1. A compound of formula P-8

2. A process for the preparation of a compound of formula P-8

comprising the steps of:

a) treating a compound of formula P-5

with 3-amino-propane-1,2-diol to form a compound of formula P-6

b) methylating a compound of formula P-6 to form a compound of formula P-7

c) treating a compound of formula P-7 with NaIO 4 to form a compound of formula P-8.

3. A process for the preparation of a compound of formula P-8

comprising the steps of:

a) methylating a compound of formula P-6

to form a compound of formula P-7

b) treating a compound of formula P-7 with NaIa 4 to form a compound of formula P-8.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2013
From: GLAXOSMITHKLINE LLC
To: VIIV HEALTHCARE COMPANY
Reel/Frame 030688/0909 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 8, 2011
From: JOHNS, BRIAN ALVIN; WEATHERHEAD, JASON GORDON
To: GLAXOSMITHKLINE LLC
Reel/Frame 026095/0905 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 8, 2011
From: HAKOGI, TOSHIKAZU; AOYAMA, YASUNORI
To: SHIONOGI & CO., LTD.
Reel/Frame 026095/0920 →
Continuity (2)
Provisional Application 61083621 · Jul 25, 2008
Related Publication 20110183940A1 · Jul 28, 2011