David L Askin

US Patent:

7598264, Oct 6, 2009

Filed:

Mar 9, 2005

Appl. No.:

10/587682

Inventors:

Wei Han - West Chester PA, US
Melissa Egbertson - Ambler PA, US
John S. Wai - Harleysville PA, US
Linghang Zhuang - Chalfont PA, US
Rowena D. Ruzek - North Wales PA, US
Debra S. Perlow - East Greenville PA, US
Mark Cameron - Brick NJ, US
Bruce S. Foster - Scoth Plains NJ, US
Ulf H. Dolling - Westfield NJ, US
R. Scott Hoerrner - Westfield NJ, US
Philip J. Pye - Guttenberg NJ, US
Remy Angelaud - Union NJ, US
Danny E. Mancheno - Rego Park NY, US
David Askin - Warren NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A01N 43/42
A61K 31/44
C07D 471/02
C07D 491/02
C07D 498/02
C07D 513/02

US Classification:

514300, 546113

Abstract:

Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.