Merck Canada Inc.

Merck Sharp + Dohme Corp.

Merck Frosst Canada & Co.

Merck Frosst Canada, Inc.

Sheldon N Crane

Oscar Miguel Moradei

Vouy Linh Truong

John A McCauley

Peter D Williams

Thomas J Greshock

Christopher James Bungard

David Jonathan Bennett

Christian Beaulieu

Carmela Molinaro

Satyanarayana Tummanapalli

Cameron Black

Daniel Mckay

Joel S Robichaud

Daniel J McKay

Renata Oballa

Katharine M Holloway

Christian Nadeau

Philippe G Nantermet

Michael John Boyd

Eduardo Setti

Christopher I Bayly

M Katharine Holloway

William D Shipe

Ronald K Chang

Catherine M Wiscount

Jesse J Manikowski

André Giroux

Karine M Villeneuve

Stephanie Lessard

Vijayasaradhi Sivalenka

Dana Davis

Daniel McKay

Marie-Eve Lebrun

Daniel Simard

Sivalenka Vijayasaradhi

Jean-Francois Chiasson

Helen Juteau

Li Hao

Kate Holloway

Sanjay Kumar Singh

John A Mccauley

Daniel J Mckay

Tummanapalli Satyanarayana

Jean-François Chiasson

Oscar M Moradei

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 2,5,6-substituted morpholine 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 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.

Compounds of Formula I are disclosed: wherein L, A, R, R, R, R, R, R, R, Rand Rare defined herein. 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. 

Sulfonamides as HIV protease inhibitors

Compounds of Formula I are disclosed: wherein A, R, R, R, R, R, R, Rand Rare defined herein. The compounds encompassed by Formula I include compounds which are 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. 

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Cathepsin cysteine protease inhibitors

This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.

Cyanoalkylamino derivatives as protease inhibitors

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Sheldon N Crane