Centre National De La Recherche Scientifique

Institut National De La Sante Et De La Recherche Medicale

Roussel Uclaf

Institut Gustave Roussy

Université Paris-Sud 11

Bioalliance Pharma

Université Paris Sud-paris Xi

Bioalliance Pharma Sa

Universite De Paris 11 - Paris Sud

Societe De Coordination De Recherches Therapeutiques

Jean D'Angelo

Didier Desmaele

Robert Azerad

Fatima Zouhiri

Didier Buisson

Gilbert Revial

Jean-Francois Mouscadet

Christian Auclair

Hervé Leh

Michele Danet

Fr&egrave;d&egrave;ric Subra

Khalid Mekouar

Laurence Jeanson

Marie Bayle

Marc Le Bret

Philippe Collery

Christophe Benard

Jean-François Mouscadet

Sabine Bonnenfant

Catherine Dargemont

Aurélie Mousnier

Georges Morgant

The present invention is directed to a rhenium complex of general Formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X is Se; Y is NH, O or S or is a methylene group; Z is halogen; m=0, 1, or 2 and p=0, 1, or 2, provided that m and p are both different from zero when Y is NH, O or S; n=3; R' is a phenyl group or a group of general Formula &#x2014;(CH)&#x2014;COOH wherein q=1 or 2, a pharmaceutical composition comprising a therapeutically effective amount of at least one of such rhenium complex where X is additionally S or Te, a method for preparing said rhenium complex and a method for treating a proliferative growth related-disorder using a therapeutically effective amount of at least one of said rhenium complex where X is additionally S or Te. Also claimed is the use of compounds of formula (II) in the preparation of compounds of formula (I). 

Rhenium complexes and their pharmaceutical use

The invention relates to the use of 8-hydroxyquinoline 7-carboxylic acid derivatives in order to produce integrase-inhibiting medicaments, capable of blocking viral replication in the stages preceding integration, and if appropriate at the level of this integration stage, these medicaments being usable for the treatment of retroviral pathologies, in particular for the treatment of AIDS.

Use of quinoline derivatives with anti-integrase effect and applications thereof

The invention relates to derivatives corresponding to formula I: in which

Quinoline derivatives process of synthesis and medicaments containing these derivatives

The invention concerns quinoline derivatives of formula (I) in which: R , R and R , identical or different represent one or several substituents, themselves identical or different, in any position on the cycles, this or these substituents being selected among a &mdash;(CH ) &mdash;Y or &mdash;CH&boxH;CH&mdash;Y group, in which Y is halogen, &mdash;OH, &mdash;OR, &mdash;COH, &mdash;COR, &mdash;COOH, COOR, &mdash;COH, &mdash;COR, &mdash;CONH , &mdash;CON(R , R )&mdash;CH&boxH;NOH, &mdash;CO&mdash; &mdash;CH&boxH;NOH, &mdash;NH , &mdash;N(R , R ), &mdash;NO , &mdash;PO(OR) &mdash;SH , &mdash;SR, &mdash;SO R, &mdash;SO NHR, CN, or Z(R ) in which R is a C1-C8 alkyl, or aryl or a heterocyclic compound, R and R , identical or different are C1-C5 alkyl, an aryl or heterocyclic compound and n is nil or a whole number between 1 and 5 R can further represent a hydrogen, and when Y is &mdash;COOH or &mdash;COOR in R , Z, if it represents an aryl, comprises at least 3 substituents or the quinoline ring is trisubstituted; X is an ethylene double bond; a &mdash;(CH ) &mdash; group in which n is a whole number between 1 and 5: or a &mdash;CH(R &mdash;CH(R ) group, R and R , identical or different, representing a hydrogen, a halogen, hydroxy or epoxy; or a &mdash;(CH ) , &mdash;O&mdash;C&mdash;(CH ) &mdash;, &mdash;(CH ) , &mdash;C(O)&mdash;O&mdash;(CH ) , &mdash;(CH ) , &mdash;O&mdash;(CH ) &mdash;, (CH ) , &mdash;N(Q)&mdash;(CH ) &mdash;, or (CH ) , &mdash;S(O)&mdash;(CH ) &mdash;, group, in which n&equals;1 to 8, m&equals;0 to 8, t&equals;0, 1 or 2, and Q&equals;h, aryl or alkyl. The invention also concerns the pharmaceutically acceptable salts of these derivatives, the diastereoisomeric and the enantiomeric forms thereof. The invention is useful as medicines with HIV anti-integrase inhibiting effect.

Quinoline derivatives, having in particular antiviral properties, preparation and biological applications thereof

New tetra-alkyl-2,2,5,5-cyclohexanone-4-ol-1-compounds and their sulphonyl derivatives with the general formula: ##STR1## in which: each of R and R', identical or different, represents an alkyl radical (1-5 carbons) and R' represents a hydrogen atom or a radical SO.sub.2 R'' in which R'' represents an alkyl radical (1-5 carbons) or an aryl radical (6-14 carbons), the process and the intermediates for their preparation, as well as their use in the synthesis of cyclopropane lactones of cis structure.

Tetra-alkyl-2,2,5,5-cyclohexanone-4-01-1 compounds and their sulphonyl

##STR1## New tetra-alkyl-2,2,5,5 cyclohexanone-4-ol-1 and their sulfonated derivatives of the general formula (I), wherein R and R', which may be the same or different, represent an alkyl radical (1-5 atoms of carbon) and R' represents a hydrogen atom or a radical SO--R'' wherein R'' represents an alkyl radical (1-5 atoms of carbon) or an aryl radical (6-14 atoms of carbon), their preparation intermediaries and process, as well as their application to the synthesis of cyclopropanic lactones having the cis structure.

Tetra-alkyl-2,2,5,5-cyclohexanone-4-ol-1 and sulphonylated derivatives

Growing community of inventors

Massy, France

Jean D'Angelo