Warner-lambert Company

Other

Otsuka Pharmaceutical Company, Limited

Agouron Pharmaceuticals, Inc.

John Michael Domagala

Joseph P Sanchez

Susan E Hagen

Thomas F Mich

Edmund Lee Ellsworth

Bradley Dean Tait

Elizabeth Ann Lunney

Edward Faith Elslager

Rocco Dean Gogliotti

John S Kiely

Mel C Schroeder

Frederick Earl Boyer

Christopher Andrew Gajda

Bharat Kalidas Trivedi

Rajeshwar Singh

Gary Louis Bolton

Michael Andrew Stier

Terri Stoeber Purchase

Townley P Culbertson

Jeffrey B Nichols

Liren Huang

Larry James Markoski

Mark J Suto

William R Turner

Alexander James Bridges

Ronald G Micetich

Josyula Venkata Prasad

Harriet W Hamilton

Vara Prasad Venkata Nagendra Josyula

Kimberly Suzanne Para

Tomi Sawyer

Thomas Eric Renau

Michael James Lovdahl

Maureen Elizabeth Carey

Albert Kudzoi Amegadzie

Arkadii Vaisburg

Marjorie S Solomon

Alexander Pavlovsky

Josyula Venkata Nagendra Vara Prasad

Bruce D Roth

Drago R Sliskovic

Helen Tsenwhei Lee

Daniel Fred Ortwine

James R Zeller

Randy Ranjee Ramharack

James N Wemple

Ashok K Trehan

Michael Roe

David Michael Thornton

Josyula Venkata Vara Prasad

Susan E Prugh

Shouming Wang

Stephen Keith Wrigley

The present invention relates to novel dihydropyrones of Formula Iwherein X is NH or NR, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.

HIV protease inhibitors

The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.

The invention is a series of 7-substituted quinazolin-2,4-diones useful as antibacterial agents, processes for the preparation of the compounds, and a pharmaceutical composition containing one or more of the compounds.

7-Substituted quinazolin-2,4-diones useful as antibacterial agents

The present invention related to novel dihydropyrones possessing 3-position nitrogen atom, which inhabit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections, and diseases, including AIDS.

Benzo&lsqb;de&rsqb;isoquinoline-1,3-diones which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents are described as well as methods for their preparation and formulation. Novel intermediates useful in the preparation of the final products are also described.

Isoquinolones

7-substituted quinazolin-2,4-diones useful as antibacterial agents

Benzo&lsqb;de&rsqb;isoquinoline-1,3-dione of Formula

Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.

Isothiazolones and pharmaceutical formulations

Antibacterial agents

This invention pertains to improved antiviral activity of 6,6-disubstituted-5,6-dihydropyran-2-ones caused by judicious placement of certain polar substituents at the 3 and/or 6 positions. The same substituents which enhance the cellular activity also diminish cytotoxicity further enhancing the desirable properties of these agents as antivirals.

Dihydropyrones with improved antiviral activity

The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.

Pyrone derivatives as protease inhibitors and antiviral agents

Isothiazolones

Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,

Arylthio compounds

Growing community of inventors

Canton, MI, United States of America

John Michael Domagala