IP Library › Granted Patent US 8,962,857
Granted Patent B2
US 8,962,857 · App. 14/269,659 · Granted Feb 24, 2015

Compounds for preparing immunological adjuvant

Inventors: Francis G. Fang (Andover, MA); James E. Foy (Andover, MA); Lynn Hawkins (Concord, MA); Charles Lemelin (North Chelmsford, MA); Andre LesCarbeau (Sommerville, MA); Xiang Niu (Malden, MA); Kuo-Ming Wu (Acton, MA)
Assignee: Eisai R&D Management Co., Ltd.
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Quick Facts
Patent No.
US 8,962,857
App. No.
14/269,659
Granted
Feb 24, 2015
Kind
B2
Abstract

The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.

Claims (10)

1. Crystalline ER-806158, (R)-1-(((R)-4,5-dihydro-2-phenyloxazol-4-yl)methoxy)decan-3-ol having a powder x-ray diffraction pattern substantially as shown in FIG. 3 .

2. Crystalline ER-806158, (R)-1-(((R)-4,5-dihydro-2-phenyloxazol-4-yl)methoxy)decan-3-ol of claim 1 having a triclinic crystal system and a P1 space group.

3. Crystalline ER-806158, (R)-1-(((R)-4,5-dihydro-2-phenyloxazol-4-yl)methoxy)decan-3-ol of claim 2 , characterized by crystal lattice parameters of:

a = 4.6047(11) Å

α = 106.008(4)°

b = 8.1161(19) Å

β = 95.604(4)°

c = 13.579(3) Å

γ = 98.696(4)°

Volume = 477.0(2) Å 3 and Z = 1.

Continuity (6)
Division 13947593 · Jul 22, 2013
Division 13468634 · May 10, 2012
Division 12698686 · Feb 2, 2010
Division 11477936 · Jun 30, 2006
Provisional Application 60695324 · Jun 30, 2005
Related Publication 20140323739A1 · Oct 30, 2014