Roussel Uclaf

Aventis Pharma S.a.

Hoechst Marion Roussel

Oraxcell

Oroxcell

Denis, Alexis

Christophe Dini

Jozsef Aszodi

Jean-Francois Chantot

Patrick Fauveau

Daniel Humbert

Solange Gouin d'Ambrieres

Jean Pachot

Alexis Denis

Jidong Zhang

Solange G D'Ambrieres

Stanislas Didierlaurent

Jean-Claude Guillot

Nathalie Drochon

Daniel Hunbert

Ester derivatives of 2-amino-2-phenyl-alkanol of general formula (I) in which: Rforms with Rand the nitrogen and carbon atoms to which they are respectively attached, a heterocycle with 4 to 7 members, optionally substituted in the &#x3b1; position of the nitrogen atom by one or two Rand Rradicals being able to be independently of one another hydrogen or linear or branched alkyl (1 to 4C), and Ris H or a &#x2014;CO&#x2014;O&#x2014;CHR&#x2014;OCORradical for which Ris H or linear or branched alkyl (1 to 4C), and Ris alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by the remainder of an amino acid, or represents a heterocycle, or Ris linear or branched alkyl (1 to 4C), alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, NH, alkylamino, dialkylamino optionally forming with the nitrogen atom to which they are attached, a heterocycle with 5 or 6 members, it being understood that the substituted alkyl radical is linear or branched and comprises at least 2C between &#x3e;N&#x2014;Rand the substituent, unless specified otherwise, alkyl or acyl are linear or branched (1 to 7C), in their R or S forms or their mixtures, as well as its pharmaceutically acceptable salts, if any. 

2-amino-2-phenyl-alkanol derivatives, preparation thereof, and pharmaceutical compositions containing same

2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: Ris H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, Ris a &#x2014;CO&#x2014;R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or Ris a &#x2014;CO&#x2014;Y&#x2014;Rradical for which Y is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;NH&#x2014;, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and Ris alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by RCOO&#x2014; in which Ris alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or Ris alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino optionally forming, with the nitrogen atom to which they are attached, a 5- or 6-member heterocycle optionally having another heteroatom (O or N), or substituted by alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, it being understood that said straight or branched substituted alkyl radical comprises at least 2C between &#x3e;N&#x2014;Rand the substituent; and Ris alkyl (1 to 4C) straight or branched unless specifically mentioned, alkyl or acyl are straight or branched (1 to 7C), in their R or S forms or their mixtures, as well as their pharmaceutically acceptable salts when these exist. 

2-amino-2-phenyl-alkanol derivatives, their preparation and pharmaceutical compositions containing them

All possible isomeric forms of a compound of the formulawhere the substituents are defined as in the specification and its non-toxic, pharmaceutically acceptable salts useful as antibiotics.

Uridine derivatives as antibiotics

A compound having the formula selected from the group consisting of

Cephalosporins

Novel intermediates of the formula ##STR1## wherein the substituents are defined in the specification.

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an integral salt or their salts with organic or mineral acids wherein the substituents are as defined in the application and having antibacterial properties.

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are as set forth below.

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are defined as in the application having anti-bacterial properties.

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids, wherein the variables are herein below defined, having antibacterial properties.

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Le Plessis Pate, France

Christophe Dini