PROCEDIMIENTO PARA LA PREPARACION DE DERIVADOS DE CEFALOSPORINAS

LA PRESENTE INVENCION SE REFIERE A NUEVOS DERIVADOS DE CEFALOSPOLINAS DE FORMULA DESCRITA EN LA INVENCION. SE REFIERE IGUALMENTE A UN PROCEDIMIENTO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN E INTERMEDIARIOS DE SINTESIS. DICHOS DERIVADOS PRESENTAN PROPIEDADES FARMACEUTICAS M...

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Hauptverfasser: SALHI, ALI, LABEEUW, BERNARD
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description LA PRESENTE INVENCION SE REFIERE A NUEVOS DERIVADOS DE CEFALOSPOLINAS DE FORMULA DESCRITA EN LA INVENCION. SE REFIERE IGUALMENTE A UN PROCEDIMIENTO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN E INTERMEDIARIOS DE SINTESIS. DICHOS DERIVADOS PRESENTAN PROPIEDADES FARMACEUTICAS MEJORADAS. New cephalosporin derivatives of formula: in which: - each of R1, R2 and R3 denotes a hydrogen atom or each of R1 and R2 denotes a hydrogen atom or a methyl group and R3 denotes a carboxyl group, or R1 and R2 taken together with the carbon atom to which they are linked form a cyclobutyl nucleus and R3 denotes a carboxyl group, - the 2 groups A are different: one denotes a hydroxyl group and the other denotes a -NH-SO2-Alk-NH2 group in which Alk denotes a C2-C4 lower alkylene group, and the pharmaceutically acceptable salts and esters of the said derivatives. The invention also relates to a process for their preparation, pharmaceutical compositions containing them and synthesis intermediates. The said derivatives exhibit improved pharmacokinetic properties.
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SE REFIERE IGUALMENTE A UN PROCEDIMIENTO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN E INTERMEDIARIOS DE SINTESIS. DICHOS DERIVADOS PRESENTAN PROPIEDADES FARMACEUTICAS MEJORADAS. New cephalosporin derivatives of formula: in which: - each of R1, R2 and R3 denotes a hydrogen atom or each of R1 and R2 denotes a hydrogen atom or a methyl group and R3 denotes a carboxyl group, or R1 and R2 taken together with the carbon atom to which they are linked form a cyclobutyl nucleus and R3 denotes a carboxyl group, - the 2 groups A are different: one denotes a hydroxyl group and the other denotes a -NH-SO2-Alk-NH2 group in which Alk denotes a C2-C4 lower alkylene group, and the pharmaceutically acceptable salts and esters of the said derivatives. The invention also relates to a process for their preparation, pharmaceutical compositions containing them and synthesis intermediates. 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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title PROCEDIMIENTO PARA LA PREPARACION DE DERIVADOS DE CEFALOSPORINAS
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