Merck + Co., Inc.

Joel R Huff

Joseph P Vacca

Walfred S Saari

John J Baldwin

Bruce D Dorsey

Steven D Young

James P Guare

Wayne J Thompson

Stella W King

Susan J DeSolms

Jane deSolms

Jonathan M Wiggins

William J Greenlee

Ian M Bell

Clarence S Rooney

Theresa M Williams

William C Lumma, Jr

John S Wai

Philip E Sanderson

Randall W Hungate

M Katharine Holloway

Allen I Oliff

Terrence M Ciccarone

Jacob M Hoffman, Jr

Susan F Britcher

Suresh K Balani

Mark E Goldman

Rhonda B Levin

Jennie B Nerenberg

Yojiro Sakurai

Anthony D Theoharides, Deceased

Hee Y Lee

Arun K Ghosh

Hee-Yoon Lee

Compounds of formula ##STR1## 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

Alpha IC adrenergic receptor antagonists

Compounds of formula ##STR1## where A is usually carbonyl or --CH.sub.2 --, D is usually --CH.sub.2 --; R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, 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.

Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Inhibitors of HIV reverse transcriptase

Compounds of formula ##STR1## are HIV protease inhibitors, and are synthesized via a novel route. 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 inhibitor compounds

Oligopeptide analogs are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivitals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

HIV protease inhibitors

Compounds of formula I and its pharmaceutically acceptable salts are formulated with a pharmaceutical carrier for the treatment or prevention of neoplastic diesase states sensitive to such treatment in animals including humans ##STR1## wherein: A is an alkyl group having 1-6 carbons;

Quinolizine sulfonamides used against certain neoplastic disease states

Certain substituted hexahydroarylquinolizines and pharmaceutically acceptable salts thereof are peripherally selective .alpha..sub.2 -adrenoceptor antagonists. The compounds are adapted to be employed for the treatment of certain pathological disorders such as hypertension, diabetes, disorders involving platelet aggregation and the like without side effects attributable to effect on the central nervous system.

Substituted hexahydroarylquinolizines

Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.

.alpha..sub.2 -adrenoceptor antagonistic arylquinolizines

Anti-depressant spiro hexahydro arylquinolizine derivatives,

Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.6 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors.

Substituted hexahydro arylquinolizines as .alpha..sub.2 blockers

Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.

Substituted benzo[b]furo- and benzo[b]thieno quinolizines

2-[2-Pyridinyloxy(thio or amino)methyl]-1H-imidazoles and derivatives and acid addition salts thereof generally are selective .alpha..sub.2 -adrenergic receptor antagonists and .alpha..sub.1 -adrenergic receptor agonists and thereby useful as antidepressants and nasal decongestants.

2-[2-Pyridinyloxy(thio or amino)methyl]-1H-imidazoles and derivatives

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Gwynedd Valley, PA, United States of America

Joel R Huff