Pierre Fabre Medicament

Centre National De La Recherche Scientifique

Other

Yves Guminski

Thierry Imbert

Jean-Marc Barret

Anna Kruczynski

Martial Grousseaud

Jean-Pierre Robin

Jean-Philippe Annereau

Alain Le Pape

Barbara Monse

Christophe Long

Arnaud Pillon

Bridget Hill

Frédéric Cantagrel

Joséphine Beck

Fadila Derguini

Sabrina Pesnel

Nicolas Guilbaud

Stéphanie Lerondel

The invention relates to fluorescent derivatives of cyanines conjugated with a polyamine group, having formula (I), or a pharmaceutically acceptable salt thereof. The invention also relates to the method for preparing said derivatives, diagnostic compositions containing same and the use thereof as a diagnostic probe for the detection of cancer tumors, in particular in vivo.

Fluorescent cyanine-polyamine derivatives as a diagnostic probe

The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.

(Poly) aminoacetamide derivatives of epipodophyllotoxin their process of preparation and their applications in therapeutics as anticancer agents

The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.

ngCycloartanone derivatives with anticancer activity

The present invention relates to a new process for the preparation of (poly)aminoalkylaminoacetamide derivatives of epipodophyllotoxin and salts thereof, characterized in that it comprises a step of peptide coupling of 4-amino-4'-demethylepipodophyllotoxin with an amine-containing reactant having protecting groups.

Process for the preparation of (poly) aminoalkylaminoacetamide derivatives of epipodophyllotoxin useful for their applications in therapeutics as anticancer agent

The invention relates to novel fluorescent derivatives of polyamines having a benzoxadiazole group, to a method for preparing the same and to the use thereof as diagnosis tools for emphasising the polyamine transport system in cancerous cells in order to adapt the treatment thereof, and thus for selecting patients carrying such tumors in order to adapt their treatment. The derivatives are of the formula (I) or a pharmaceutically acceptable salt thereof, in which: Ris one or more NOgroups in position 4 or 6, or a SOPh, SONMe, SONHor SOH group; Ris hydrogen, Calkyl, benzyl, a perfluoroalkyl group; the values of a, b, c range from 2 to 5 independently from each other and represent alkylene chains separating the amino groups, and the values of d and e can independently be 0 or 1.

Fluorescent derivatives of polyamines, method for preparing same and applications thereof as diagnosis tools in the treatment of cancerous tumors

The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent.

(Poly)Aminoalkylaminoalkylamide, alkyl-urea, or alkyl-sulfonamide derivatives of epipodophyllotoxin, a process for preparing them, and application thereof in therapy as anticancer agents

The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamidc, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: &#x2014;R represents hydrogen or Calkyl, &#x2014;A represents CO(CH)or CONH(CH)where n=2, 3, 4, or 5, &#x2014;R1 and R2 are as described herein. 

(Poly) aminoalkylaminoalkylamide, alkyl-urea, or alkyl-sulfonamide derivatives of epipodophyllotoxin, a process for preparing them, and application thereof in therapy as anticancer agents

The invention relates to a method for synthesizing 4&#x3b2;-amino-4'-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4&#x3b2;-halogenoacetamido-4&#x2032;-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4&#x3b2;-amino-4&#x2032;-demethyl-4-desoxypodophyllotoxin.

Method for preparing 4B-amino-4'-demethyl-4-desoxypodophyllotoxin

The present invention describes a new process for the preparation of (poly)aminoalkylaminoacetamide compounds of epipodophyllotoxin useful for their applications in therapeutics as anticancer agents. This process comprises a step of condensation of a primary-amine-containing reactant, whose amine functions are not protected, with &#x3b2;-chloroacetamido-4'-epipodophyllotoxin in a polar aprotic organic solvent.

Process for the synthesis of anticancer (poly) aminoalkylaminoacetamide derivatives of epipodophyllotoxin

The invention relates to a method for synthesizing 4.beta.-amino-4'-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4.beta.-halogenoacetamido-4&#x2032;-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4.beta.-amino-4&#x2032;-demethyl-4-desoxypodophyllotoxin. 

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Lagarrigue, France

Yves Guminski