Pierre Fabre Medicament

Other

Centre National De La Recherche Scientifique

Thierry Imbert

Yves Guminski

Jean-Marc Barret

Anna Kruczynski

Martial Grousseaud

Francis Colpaert

Barbara Monse

Jean-Pierre Robin

Wouter Koek

Jean-Pierre Rieu

Jean-Francois Patoiseau

Marc Marien

Patrice Mayer

Michael Briley

Robert Kiss

Jean-Philippe Annereau

Alain Le Pape

Philippe Maillos

Pierre Sokoloff

Jean-Louis Vidaluc

Bridget Hill

Arnaud Pillon

Jean-François Patoiseau

Jean-Claude Martel

Peters Pauwels

Ludovic Leriche

Sabrina Pesnel

Florence Cuisiat

Nicolas Guilbaud

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 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 chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.

Chromone derivatives, a process for their preparation and their therapeutic applications

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. 

Method for preparing 4&#x3b2;-amino-4'-demethyl-4-desoxypodophyllotoxin

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

The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C-Calkoxy group, a linear or branched C-Calkylthio group; R2 represents a linear, branched, cyclic C-Cgroup, a 2- or 3-thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C-Calkyl, C-Calkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents. 

3&#x3b2;-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof

Fluorinated imidazoline benzodioxane, preparation and therapeutic uses thereof

Use of efaroxan for producing medicine for treating huntington 's disease

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Viviers les Montagnes, France

Thierry Imbert