Merck + Co., Inc.

Mary Beth Young

Harold G Selnick

Philippe G Nantermet

Peter D Williams

Joseph P Vacca

Craig Alan Coburn

James C Barrow

Shaun R Stauffer

Philip E Sanderson

Randall W Hungate

Terry A Lyle

Donnette D Staas

Hemaka Anthony Rajapakse

Richard C Isaacs

Kenneth J Stauffer

The present invention is directed to benzylether and benzylamino derivative compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)&#x2014;N(R)CH(R)&#x2014; wherein the nitrogen atom is attached to R, and Rand Rare independently selected from the group consisting of hydrogen, Ccycloalkyl, and Calkyl, or 2) wherein the nitrogen atom is attached to R, and m is 0, 1, or 2 

Thrombin inhibitors

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein R2 is R3 is selected from the group consisting of 1) hydrogen, 2) halogen, 3) C1&#x2013;4 alkyl, 4) C3&#x2013;7 cycloalkyl, 5) CF3, 6) OCF3, 7) C1&#x2013;4 alkoxy, and 8) cyano; and R12 is a 5-membered heteroaryl ring having 2, 3, or 4 heteroatoms, provided that at least 1 heteroatom is N, and at most 1 of the heteroatoms is S, said ring being unsubstituted or substituted, at any one ring atom, with CH3.

Compounds such as ##STR1## or pharmaceutically acceptable salts thereof, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

HIV protease inhibitors useful for the treatment of AIDS

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Lansdale, PA, United States of America

Mary Beth Young