Merck + Co., Inc.

Thomas A Rano

Frank P DiNinno

Mark L Greenlee

Zhijian Lu

James R Tata

Subharekha Raghavan

Wendy Lee

Tracy Huening

Yuan Cheng

David Askin

Kevin Tyler Chapman

Richard John Varsolona

Nancy J Kevin

Joseph Leslie Duffy

Mark G Charest

R Scott Hoerrner

Fengqi Zhang

Joseph D Armstrong, Iii

Brian Anthony Kirk

Robert M Purick

Fred Fleitz

Daniel E Petrillo

&ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and 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. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof

Certain &agr;-hydroxy-&ggr;-&lsqb;&lsqb;(carbocyclic- or heterocyclic-substituted)amino&rsqb;carbonyl&rsqb;alkanamide derivatives are described as inhibitors of HIV protease and inhibitors of HIV replication. These compounds 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, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Alpha-hydroxy-gamma-&lsqb;&lsqb;(carbocyclic-or heterocyclic-substituted)amino&rsqb;carbonyl&rsqb;alkanamide derivatives and uses thereof

The present invention relates to antibacterial agents of the carbapenem class, in which the 2-position sidechain is characterized by a phenanthridine moiety typically having a substituent attached to the nitrogen of the phenanthridine and substituted at other positions by various neutral substituents. When there is substitution on the nitrogen of the phenathridine moiety that nitrogen is a charged quaternary nitrogen.

2-phenanthridinyl carbaphenem antibacterial agent

The present invention relates to antibacterial agents of the carbapenem class, in which the 2-position sidechain is characterized by a phenanthridine moiety, substituted by various neutral substituents.

2-phenanthridinyl carbapenem antibacterial agents

Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.

2-benzocoumarinyl-carbapenems

Carbapenems of the formula ##STR1## wherein: P' is a removable protecting group for hydroxy; and

2-phenanthridonyl-carbapenems

Carbapenems of the formula ##STR1## wherein: P' is a removable protecting group for hydroxy; and M is a removable protecting group for carboxy; are useful intermediates for carbapenem antibiotics.

2-phenanthridonyl carbapenem intermediates

2-benzocoumarinyl carbapenems

Carbapenems of the formula ##STR1## with E as ##STR2## are useful antibacterial agents.

Carbapenems of the formula ##STR1## are useful antibacterial agents.

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Somerville, NJ, United States of America

Thomas A Rano