Merck Sharp + Dohme Corp.

Merck Canada Inc.

Daniel Mckay

John A McCauley

Peter D Williams

Oscar Miguel Moradei

Thomas J Greshock

Christopher James Bungard

David Jonathan Bennett

Christian Beaulieu

Vouy Linh Truong

Carmela Molinaro

Sheldon N Crane

Satyanarayana Tummanapalli

Christian Nadeau

Philippe G Nantermet

M Katharine Holloway

William D Shipe

Ronald K Chang

Catherine M Wiscount

Jesse J Manikowski

Karine M Villeneuve

Stephanie Lessard

Katharine M Holloway

Daniel Simard

Vijayasaradhi Sivalenka

Helen Juteau

Li Hao

Kate Holloway

Sanjay Kumar Singh

Sivalenka Vijayasaradhi

John A Mccauley

Tummanapalli Satyanarayana

The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z, Z, V, V, V, R, R, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. 

HIV protease inhibitors

The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

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Milton, MA, United States of America

Daniel Mckay