Warner-lambert Company

Michael Andrew Stier

Rajeshwar Singh

John Michael Domagala

Edmund Lee Ellsworth

Liren Huang

James S Kaltenbronn

Joseph P Sanchez

Ronald G Micetich

Joseph Thomas Repine

James P Hudspeth

Brian Morgan Watson

Dai Q Nguyen

Howard Daniel Hollis Showalter

Tuan Phong Tran

Judy Yip

Thomas Eric Renau

Paul Bird

W Howard Roark

Arkadii Vaisburg

Maureen Elizabeth Carey

Albert Kudzoi Amegadzie

Francis John Tinney

William Howard Roark

Elizabeth Ann Lunney

Ernest D Nicolaides

Peter W Woo

Dai Quoc Nguyen

Shouming Wang

Stephen Keith Wrigley

Michael Roe

David Michael Thornton

Joseph Peter Sanchez

Howard Daniel Showalter

Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: Rand Rinclude alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclic, and heteroaryl; R, R, and Rinclude H, alkyl, alkoxy, halo, NO, CN, NH, alkyl and dialkylamino; Rincludes hydrogen, alkyl, cycloalkyl, heterocyclic, fused heterocyclic, aryl and fused aryl; J and K are C or N; and pharmaceutically acceptable salts thereof. 

3-aminoquinazolin-2,4-dione antibacterial agents

Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: Rand Rinclude alkyl, alkenyl, cycloalkyl, aryl, hetero-cyclic, and heteroaryl; R, R, and Rinclude H, alkyl, alkoxy, halo, NO, CN, NH, alkyl and dialkylamino; Rincludes hydrogen, alkyl, cycloalkyl, hetero-cyclic, fused heterocyclic, aryl and fused aryl; J and K are C or N; and pharmaceutically acceptable salts thereof. 

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

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

Antibacterial agents

The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension, hyperaldosternoism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic test using the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.

Renin inhibitors III

The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension and for treating hyperaldosteronism. Novel intermediates, processes for preparing both the intermediates and the novel peptides, pharmaceutical compositions, and methods of treatment are included.

Renin inhibitors

The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension and hyperaldosteronism. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic test using the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.

The S,S-isomers of Boc-benztine and Boc-cyclotine can be produced via the fractional crystallization of R-(+)-alpha-methylbenzylamine salt(s). The products are useful in the production of renin inhibitors.

Separation of diastereomers

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Ypsilanti, MI, United States of America

Michael Andrew Stier