Synphar Laboratories, Inc.

Fedora Pharmaceuticals Inc.

Warner-lambert Company

Naeja Pharmaceutical Inc.

Taiho Pharmaceutical Company Limited

Dai Q Nguyen

Jehangir Khan

Samarendra N Maiti

Rong Ling

Mohsen Daneshtalab

Ronald G Micetich

Rajeshwar Singh

Edmund Lee Ellsworth

Howard Daniel Hollis Showalter

Chan M Ha

Joseph P Sanchez

Brian Morgan Watson

Michael Andrew Stier

Tuan Phong Tran

Judy Yip

Paul Bird

Inderjit Sidhu

Hiep T Luu

Norio Unemi

Ronald J Micetich

Mark Abel

Tetsuo Furukawa

Sameeh Salama

Kim Marie Hutchings

Laurence M Tempest

Yadagiri Bathini

Bicyclic compounds and their use as antibacterial agents and &#x3b2;-lactamase inhibitors

A compound of formula (I): wherein:M is hydrogen or a pharmaceutically acceptable salt-forming cation;Y is ORor NRR,and R, R, Rand M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.

New bicyclic compounds, their preparation, and their use as antibacterial agents, either alone or in combination with an antibiotic for the treatment of infections caused by &#x3b2;-lactamase-producing pathogenic bacteria, are described.

Bicyclic compounds and their use as antibacterial agents and beta-lactamase inhibitors

Bicyclic compounds and their use as antibacterial agents and betalactamase inhibitors

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 present invention provides compounds of Formula (I):wherein R-Rand K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antibacterial agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.

Antibacterial agents

A compound of formula I, or an optical isomer or pharmaceutically acceptable salt thereof, ##STR1## is disclosed as well as a pharmaceutical composition and a method of treating or preventing a fungal infection using the compound.

Triazoles as therapeutic agents for fungal infections

A process for the synthesis of compounds of the formulas Ia and Ib below, wherein R.sub.1, R.sub.2, and R.sub.3, which are the same or different, are each selected from hydrogen and C.sub.1 -C.sub.4 alkyl, including the compound Anabaseine (Ia, wherein R.sub.1 =R.sub.2 R.sub.3 =H) (3,4,5,6-tetrahydro-2', 3'-bipyridine), the process comprising reacting sodium salt of .delta.-valerolactone with substituted ethyl nicotinate derivative to produce the Claisen product sodium 3-nicotinoyl-2-tetrahydropyranone enolate derivative, heating the sodium 3-nicotinoyl-2-tetrahydropyranone enolate derivative with concentrated HCl to produce 3-(5-chloro-1-pentanone-1-yl) pyridine derivative, dissolving the 3-(5-chloro-1-pentanone-1-yl) pyridine derivative in ethanol and then heating the 3-(5-chloro-1-pentanone-1-yl) pyridine derivative in ethanol with ethanolic ammonia solution in a sealed container to produce the compound Ia. Also, the process steps in the above process, and the products and intermediate products produced thereby. ##STR1##

Synthesis of anabaseine, salts and derivatives thereof

A 1,4-dihydropyridine derivative of the formula I: ##STR1## is provided in which: A is an azole moiety;

Generation of 1,4-dihydropyridine derivatives

There are provided compounds having the general formulae ##STR1## wherein R is a non-fused azole moiety;

Novel generation of heteroaryl thio, sulfoxy, or sulfonyl alkyl azoles

A heteroaryloxyalkylheterocyclic derivative of the Formula I:

Novel generation of heteroaryloxyalkyl heterocycles with

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Edmonton, Canada

Dai Q Nguyen