American Cyanamid Company

Wyeth

Other

Wyeth Holdings Corporation

Wyeth, Five Giralda Farms

Yang-I Lin

Panayota Bitha

Joseph J Hlavka

Ralph G Child

Stanley A Lang, Jr

Carl B Ziegler

Thomas L Fields

Daniel B Moran

Gregg Brian Feigelson

Paul Frank Fabio

Karen Bush

Zhong Li

Timothy W Strohmeyer

Subas Sakya

Phaik-Eng Sum

Keith C Murdock

Tarek Suhayl Mansour

Raymond G Wilkinson

Takao Abe

Aranapakam Mudumbai Venkatesan

Atul Agarwal

Ving J Lee

Fuk-Wah Sum

Joseph P Joseph

David N Ridge

Osvaldo Dos Santos

Gerardo De Francisco

Itsuki Yamamura

Tsuyoshi Takasaki

Carl B Ziegler, Jr

Andrew S Tomcufcik

Jeremy Ian Levin

Jerauld S Skotnicki

Frank Eldridge Lovering

Joseph W Marsico, Jr

George Diamantidis

Leonard Alexander McDonald

Kaapjoo Park

Leon Goldman

Weiheng Wang

Jeffrey Scott Condon

Soon M Kang

The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group as defined herein; X is O; Ris H, C1-C6 alkyl, C5-C6 cycloalkyl, or CHROCOC1-C6 alkyl; and Ris hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.

Bicyclic 6-alkylidene-penems as &#x3b2;-lactamase inhibitors

This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-&#x3b1;, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.

Beta-sulfonamide hydroxamic acid inhibitors of tace/matrix metalloproteinase

The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is S.

Nucleoside peptide antibiotics of AA-896

The invention is a process improvement for producing the carbapenem antibacterial agent (4R, 5S, 6S)-3-&lsqb;&lsqb;2R,3R)-2-&lsqb;&lsqb;&lsqb;(S)-2-amino-3-methyl-1-oxobutyl&rsqb;amino&rsqb;methyl&rsqb;tetrahydro-3-furanyl&rsqb;thio&rsqb;-6-&lsqb;R)-1-hydroxyethyl&rsqb;-4-methyl-7-oxo-1-azabicyclo&lsqb;3.2.0&rsqb;hept-2-ene-2-carboxylic acid by hydrogenation of 4-nitrobenzyl (4R,5S,6S)-6-&lsqb;(1R)-1-hydroxyethyl&rsqb;-4-methyl-3-&lcub;&lsqb;2R,3R)-2-(&lcub;&lsqb;(2S)-3-methyl-2-(&lcub;&lsqb;4-nitrobenzyl)oxy&rsqb;carbonyl&rcub;amino)butanoyl&rsqb;amino&rcub;methyl)-tetrahydrofuran-3-yl&rsqb;thio&rcub;-7-oxo-1-azabicyclo&lsqb;3.2.0&rsqb;hept-2-ene-2-carboxylate in a biphasic solvent mixture comprising a water portion and an organic solvent portion, not containing an acid acceptor. The water portion is separated from the organic solvent portion and (4R,5S,6S)-3-&lsqb;&lsqb;(2R,3R)-2-&lsqb;&lsqb;&lsqb;(S)-2-amino-3-methyl-1-oxobutyl&rsqb;amino&rsqb;methyl&rsqb;tetrahydro-3-furanyl&rsqb;thio&rsqb;-6-&lsqb;R-hydroxyethyl&rsqb;-4-methyl-7-oxo-1-azabicyclo&lsqb;3.2.0&rsqb;hept-2-ene-2-carboxylic acid is isolated from the separated water portion by lyophilization or reverse osmosis.

PROCESS IMPROVEMENT IN THE PREPARATION OF (4R, 5S, 6S)-3-&lsqb;&lsqb;(2R,3R)-2-&lsqb;&lsqb;&lsqb;(S)-2-AMINO-3-METHYL-1-OXOBUTYL&rsqb;AMINO&rsqb;METHYL&rsqb;TETRAHYDRO-3-FURANYL&rsqb;THIO&rsqb;-6-&lsqb;(R)-1-HYDROXYETHYL&rsqb;-4-METHYL-7-OXO-1-AZABICYCLO&lsqb;3.2.0&rsqb;HEPT-2-ENE-2-CARBOXYLIC ACID

3,6-disubstituted penam sulfone derivatives

Organic platinum complexes active as anti-tumor agents in warm-blooded animals, and methods for synthesis of same, are described.

(Gem-heterocyclodimethanamine-n,n&prime;)platinum complexes

Carbapenem antibiotic compounds of the general formula: ##STR1## wherein the moiety ##STR2## is a 4, 5 or 6 membered mono, di- or tri-substituted oxygen or sulfur containing ring; wherein Z is oxygen, sulfur, sulfoxide and sulfone, pharmaceutical compositions thereof useful for the treatment of bacterial infections, processes for preparing the compounds and new intermediates useful in the process.

2-thiosubstituted carbapenems

Carbapenem antibiotic compounds of the general formula: ##STR1## wherein the moiety ##STR2## is a 4, 5 or 6 membered mono, di- or tri- substituted oxygen or sulfur containing ring; wherein Z is oxygen, sulfur, sulfoxide and sulfone, pharmaceutical compositions thereof useful for the treatment of bacterial infections, method of inhibiting a Beta-lactamase enzyme by administering said compounds, processes for preparing the compounds and new intermediates useful in the process are disclosed.

Method of inhibiting a .beta.-lactamase enzyme by administering novel

Tetrahydrofuanyl compounds of the following formulae: ##STR1## are disclosed.

Method for producing tetrahydrofuranyl compounds

Carbapenem antibiotic compounds of the general formula: ##STR1## wherein the moiety ##STR2## is a 4, 5 or 6 membered mono, di- or tri- substituted oxygen or sulfur containing ring; wherein Z is oxygen, sulfur, sulfoxide and sulfone, pharmaceutical compositions thereof useful for the treatment of bacterial infections, processes for preparing the compounds and new intermediates useful in the process.

7-(substituted)piperazinyl-1-ethyl-6-fluoro-4-oxo-3-quinolinecarboxylic acids, the pharmacologically acceptable salts thereof, compositions containing them, processes and intermediates for producing them, and methods of using them to treat bacterial infections in warm-blooded animals.

Piperazine derivatives

This disclosure sets forth a novel process for producing cisplatin analogs which possess antitumor activity.

Synthesis of cisplatin analogs

Novel antibacterial compounds of the formula: ##STR1## in which R.sub.1 is alkyl (C.sub.1 -C.sub.4), cycloalkyl (C.sub.3 -C.sub.6), alkoxy (C.sub.1 -C.sub.4), alkylamino (C.sub.1 -C.sub.3), vinyl, phenyl, benzyl, --CH.sub.2 CH.sub.2 F or mono or polysubstituted phenyl (wherein the substituent is halogen, CF.sub.3 or OCH.sub.2 F); n is an integer of from 1 to 4; and R.sub.2 is cis or trans hydroxy, amino, mono or disubstituted alkyl (C.sub.1 -C.sub.3) amino and the pharmacologically accepted salts thereof are described.

7-(substituted)cycloalkylamino-1

Novel substituted quinolinecarboxylic acid derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, alkali metal, alkaline earth metal or lower alkyl; R.sub.2 is hydrogen, benzyl or alkyl (C.sub.1 -C.sub.3); X is hydrogen or fluoro; which have antibacterial activity, intermediates useful in the preparation of the compounds, methods of producing and using the compounds to treat bacterial infections in animals.

8-fluoro and 7, 8,

Growing community of inventors

Nanuet, NY, United States of America

Yang-I Lin