Roussel Uclaf

Aventis Pharma S.a.

Other

Hoechst Marion Roussel

Patrick Fauveau

Jozsef Aszodi

Jean-Francois Chantot

Lucien Nedelec

Constantin Agouridas

Laurent Schio

Daniel Humbert

Solange Gouin d'Ambrieres

Christophe Dini

Gilles Hamon

Astrid Markus

Claude Oberlander

Jean-Marc Michel

Olivier Courtin

Dominique Melon Manguer

Chantal Damais

Stephen Hawser

Gilles Lebourg

Jean-Claude Gasc

Andre Pierdet

Alain Corbier

Solange G D'Ambrieres

Nathalie Pietre-Dischamp

Daniel Hunbert

Pascale Vicat

Compounds of the formula wherein the substituents are as defined in the application useful as antifungal agents.

Echinocandin derivatives, their method of preparation and their application as anti-fungal agents

A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which The compounds of formula (I) have antifungal properties.

Derivatives of echinocandine, their preparation process and their use as antifungals

Compound of the formula wherein Ris &#x2014;CH&#x2014;CH&#x2014;NH, Ris &#x2014;CH, Ris &#x2014;OH, R is Z is methyl and salts thereof which are useful as antifungal agents.

A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I):in which The compounds of formula (I) have antifungal properties.

Echinocandin derivatives, method for preparing same and application as antifungal agents

A subject of the invention is the compounds of formula (I):in which The products have of the antifungal properties.

Echinocandin derivatives, method for preparing same and use as antifungal agents

A compound of Formula I in which R and R &equals;H, OH, alkyl optionally substituted, or NR forms with the carbon bearing NR R a double bond and R is Xra, X being O, NH or N-alkyl and Ra being H, alkyl optionally substituted; R&equals;a chain containing up to 10 carbon atoms, optionally comprising one or several heteroatoms, one or several heterocycles; T&equals;H, CH , CH CONH , CH C&equiv;, (CH ) NH ; Y&equals;H, OH, halogen; W&equals;H, OH; Z&equals;H or CH ; said products have antifungal properties.

Echinocandin derivatives, preparation method and application as anti-fungal agents

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.

The syn isomer of (R) or (S) or (R,S) mixture, in the form of internal salts or salts with acids or bases of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having a very good antibiotic activity.

7-benzyloxyimino-cephalosporins

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.

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## in the form of an internal salt or a non-toxic, pharmaceutically acceptable acid addition salt wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are individually defined in the specification, R.sub.4 is --OH or alkoxy of 1 to 8 carbon atoms, A and A' are individually selected from the group consisting of hydrogen, an equivalent of an alkali metal or alkaline earth metal, magnesium, ammonium and an organic amine, or one or two of --COOA or --COOA' ARE --CO.sub.2 --, the wavy line means --CH.sub.2 R.sub.6 can be in the E or Z position, R.sub.6 in the quaternary ammonium form is selected from the group consisting of ##STR2## X is defined as in the specification with the proviso that when R.sub.3 is --OH or alkoxy of 1 to 8 carbon atoms, at least one R.sub.1, R.sub.2 and R.sub.5 is other than hydrogen having antibacterial properties.

A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines represent a possible endo or exo double bond, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and ##STR2## R'.sub.2 is alkyl of 1 to 8 carbon atoms or aryl of 6 to 14 carbon atoms, X is --O-- or --NR--, R is selected from the group consisting of --OH, hydrogen, ##STR3## and --COOR', R' is hydrogen or alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, all optionally substituted with at least one halogen or --OH, with the proviso that if Y is --OH, X is not --NH-- and their non-toxic, pharmaceutically acceptable addition salts of acids or bases having antibacterial and immunological properties.

Growing community of inventors

Livry Gargan, France

Patrick Fauveau