Warner-lambert Company

Signal Pharmaceuticals, Inc.

Trega Biosciences, Inc.

Houghten Pharmaceuticals, Inc.

Mark J Suto

Richard Allen Houghten

Ronald R Tuttle

Beverly E Girten

Moorthy S Palanki

William R Turner

Costas C Loullis

Jagadish C Sircar

John Michael Domagala

Charles F Schwender

Susan E Hagen

Leah M Gayo

Lynn J Ransone-Fong

Leslie M Werbel

James R Zeller

James N Wemple

Victor Fedij

Mark E Goldman

Amaresh Basu

Patricia A Weber

Robert Warren Sullivan

Ellen M Berman

Paul Omholt

Patrick Fagan

Ali Andalibi

The present invention provides novel cytokine restraining agents, which limit or control the biological activity of cytokines. The invention also provides pharmaceutical compositions comprising a cytokine restraining peptide and methods of administering the pharmaceutical composition to a subject. The invention further provides methods for using the novel peptides to restrain cytokine activity in a subject.

Cytokine restraining agents

Compounds having utility as anti-inflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are quinazoline-containing compounds. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

Pyridopyrimidine analogs and related compounds and methods for treating

Quinazoline analogs and related compounds and methods for treating

Compounds having utility as anti-inflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are pyrimidine-containing compounds and, in one embodiment, are esters of the same. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

Pyrimidine carboxylates and related compounds and methods for treating

Compounds having utility as antinflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are pyrimidine- or pyrazine-containing compounds and, in one embodiment, are carboxyamides of the same. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

Pyrimidine carboxamides and related compounds and methods for treating

The present invention relates to novel peptides that are potent cytokine restraining agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a cytokine restraining agent. Administration of such a cytokine restraining agent to a subject restrains, but does not necessarily suppress, cytokine activity completely. Thus, the present invention provides a method of restraining pathologically elevated cytokine activity in a subject. The invention also provides methods of treating disuse deconditioning and diseases mediated by nitric oxide and cytokines, such as diabetes and glomerulonephritis, a method of organ protection, a method of organ protection, and a method of reducing the negative side effects of cancer chemotherapy, such as nephrotoxicity.

Cytokine restraining agents and methods of use in pathologies and

The present invention relates to novel peptides that are potent cytokine regulatory agents. In addition, the present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a cytokine regulatory agent. Administration of such a cytokine regulatory agent to a subject can enhance or restrain cytokine activity. Thus, the present invention provides a method of regulating cytokine activity in a subject having a condition characterized by aberrant or altered cytokine activity. The invention also provides methods of treating such conditions, including, for example, disuse deconditioning, diseases mediated by nitric oxide and cytokines, adverse drug reactions, obesity, septic shock, and adverse side effects due to cancer chemotherapy or occurring as in response to organ transplantation.

Cytokine regulatory agents and methods of use in pathologies and

Chiral 3-cyanopyrrolidines of the following formula are disclosed, wherein R' is as defined herein. The compounds are useful as intermediates for naphthyridine and quinoline antibiotics. ##STR1##

Chiral 3-cyano-1-substituted-pyrrolidines

Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1-pyrrolidinyl]quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating bacterial infections therewith. Also described is a method of manufacture of the quinolones and naphthyridones as well as the starting materials, the optically pure pyrrolidine moieties for attachment at the 7-position.

Optical isomers of

The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-substituted-3-pyrrolidinols to their corresponding chiral sulfonate esters; converting the sulfonate esters to chiral 1-substituted-3-cyanopyrrolidines having an inverse configuration, and then dialkylating the chiral cyanopyrrolidines with alkyl lithium in the presence of a Lewis acid without racemization at the asymmetric carbon atom is described.

Process for chiral

Optically pure R-enantiomer of alpha,alpha-dilower

Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.

Quinolinecarboxylic acid antibacterial agents

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San Diego, CA, United States of America

Mark J Suto