Warner-lambert Company

Marland P Hutt, Jr

Theodore H Haskell

John S Kiely

Thomas F Mich

Ernest D Nicolaides

Townley P Culbertson

Peter W Woo

Gin G Huang

Novel quinoline-, naphthyridine-, and benzoxazine-carboxylic acid derivatives with bridged sidechains useful as antibacterial agents are described. Methods for their preparation, formulation, and use in treatment of bacterial infections is also described.

Process for preparing 6,8-diazabicyclo[3.2.2]nonane derivatives

Antibacterial agents

Antibacterial quinoline compounds

1,8-Naphthyridines and their use as antibacterial agents

Novel naphthyridine-, quinoline- and benzoxazine-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.

Certain thiazolidine or thiomorpholine substituted quinoline and pyridobenzoxazine compounds are antibacterial agents. Method for their preparation and use are disclosed.

Antibacterial thiazolidine or thiomorpholine substituted quinolines

Novel organic amide compounds which are N-[[(acylaminoacylamino or aminoacylamino)]-dihydro-oxo-3-quinolinylcarbonyl]cephalosporin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate cephalosporin or the acid addition salt or silylated derivative or complex thereof with a reactive derivative of the corresponding (acylaminoacylamino or aminoacylamino)dihydro-oxo-3-quinolinecarboxylic acid or (b) reacting the free amino acid 7-aminocephalosporanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[(acylaminoacylamino or aminoacylamino)dihydro-oxo-3-quinolinylcarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Cephalosporins

Novel organic amide compounds which are N-[[(acylaminoacylamino or aminoacylamino9]-dihydro-oxo-3-quinolinylcarbonyl]penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding (acylaminoacylamino or aminoacylamino)-dihydro-oxo-3-quinolinecarboxylic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[(acylaminoacylamino or aminoacylamino) dihydro-oxo-3-quinolinycarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Antibacterial amide compounds, compositions thereof and methods of using

Novel organic amide compounds which are N-[ureidodihydro-oxo-3-quinolinylcarbonyl]penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding ureido-dihydro-oxo-3-quinolinecarboxylic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[ureidodihydro-oxo-3-quinolinylcarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Antibacterial amide compounds, compositions, and methods of use

Novel organic amide compounds which are N-[2-(acylaminophenyl)-4-hydroxy-5-pyrimidinylcarbonyl]penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-2-(acylaminophenyl)-4-hydroxy-5-pyrimidine carboxylic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[2-(acylaminophenyl)-4-hydroxy-5-pyrimidinylcarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Antibacterial amide compounds and pharmaceutical compositions containing

Novel organic amide compounds which are N-[6-[(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinyl] penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(acylaminoacylamino or aminoacylamino)-phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(acylaminoacylamino or aminoacylamino) phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Antibacterial amide compounds and means for using the same

Novel organic amide compounds which are N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl] penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidine carboxylic acid or (b) reacting the free amino acid of 6-aminopenicillamic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Growing community of inventors

Saline, MI, United States of America

Marland P Hutt, Jr