Ire-celltarg S.a.

Omnichem

Institut International De Pathologie Cellulaire Et Moleculaire

Omnichem, S.a.

Andre B Trouet

Jean A Hannart

Kandukuri S Rao

Jean-Paul Dejonghe

Roger M Baurain

Marie-Paule Collard

Philippe Pirson

Jean-Bernard Falmagne

Michele M Masquelier

Kandukuri S Bushana

Roger Baurain

Ksp Siva Rao

Bhushana K Rao

The invention relates to new quinoline derivatives containing a free amine group and having antimalarial properties, in particular new primaquine derivatives or their addition salts with acids, and to a method for preparing them. According to the invention, these new derivatives are represented schematically by the formula:

New compounds which are active against the tissue forms of malaria and

A description is given of conjugates of vinca alkaloid of the indole-dihydroindole type with a protein or a protein fragment, corresponding to the general formula ##STR1## in which R.sub.1 denotes a protein or a protein fragment;

Vinblastine derivatives, and pharmaceutical compositions containing them

The subject of the present invention is conjugates of vinca (indole-dihydroindole) derivatives carrying a detergent chain of at least 7 aliphatic carbon atoms in the C-3 position bonded via a covalent bond to a macromolecular carrier of polypeptide character, and also pharmaceutical compositions containing these conjugates and a process of preparation.

Conjugates of a vinca derivative carrying a detergent chain in the C-3

The present invention relates to microcrystals of a substance, which substance is insoluble in water and has an affinity for phospholipids, as well as a process for its preparation. According to the invention, one or more organic solvents are evaporated from a solution of phospholipids and substance, and the film obtained thereby, after evaporation of the one or more solvents, is suspended in an aqueous solution by vigorous stirring. The invention also relates to pharmaceutical compositions containing as active principle these microcrystals, particularly liquid pharmaceutical compositions packaged in injectable form or in sprayable form.

Microcrystals comprising an active substance having an affinity for

The invention relates to new conjugates of vinblastine and some of its known derivatives with proteins, fragments thereof, aminoacids or amines, which are useful as anti-tumor agents. The invention also relates to some intermediates which are active in chemotherapy, and amino derivatives thereof. These compounds correspond to the following general formula ##STR1## in which A represents an acetylamino-, trifluoroacetylamino- or carbobenzyloxyamino- substituted --CO(CH.sub.2).sub.n CO-- or ##STR2## in which n is 1 to 5, R.sub.1 represents an optionally modified protein radical,

Conjugates of vinblastine, a process for their preparation and their use

The invention relates to vinca (indole-dihydroindole) alkaloid derivatives, in which a fatty chain containing at least 7 aliphatic carbon atoms is present at least at the C.sup.3 /C.sup.4 -position. The derivatives according to the present invention are useful as drugs.

Vinblastine derivatives and pharmaceutical composition containing them

New conjugates of vinblastine and its derivatives, process for preparing

Vinblastine derivatives of the formula ##STR1## wherein R.sub.1 is an ester of a .alpha.-aminoacid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, glutamic acid, aspargine, glutamine, arginine, lysine, cysteine, cystine, methionine, phenylalanine, tyrosine, tryptophan, proline, histidine, hydroxy-lysine, hydroxyproline, or of a peptide consisting of 1-6 identical or different such amino-acids, and the ester group, which may be straight or branched, being a carboalkoxy group having 2-9 carbon atoms, and R.sub.2 is hydrogen or a C.sub.2 -C.sub.9 alkanoyl group, R.sub.5 is H or OH, R.sub.6 is CH.sub.3, CHO or H and X=H or Br and their pharmaceutically acceptable mineral or organic acid addition salts. The compounds are useful as antitumor drugs.

Vinblastin-23-oyl amino acid derivatives

Amino acid derivatives of vinblastine, including peptide derivatives, methods of their preparation and pharmaceutical compositions containing such vinblastine derivatives for use as antitumor agents are described.

Vinblastin-23-oyl amino acid derivatives for use as antitumor agents

The invention relates to a new pharmaceutical form of a medicament of the formula

Medicaments, their preparation and compositions containing same

New derivatives of doxorubicine of the formula ##STR1## wherein R represents a radical of the formula ##STR2## wherein R.sub.1 represents hydrogen, alkyl (possibly substituted with amino, alkylamino, dialkylamino, hydroxy, mercapto or methylthio), phenyl, benzyl (possibly substituted with one or more hydroxy) and R.sub.2 represents hydrogen or forms with R.sub.1 an alkylene radical, the salts thereof and pharmaceutical compositions containing said compounds. They are prepared according to methods known in peptidic chemistry by reacting a reactive form of an aminoacid of the formula ##STR3## with doxorubicine.

Derivatives of doxorubicine, their preparation and use

A complex of deoxyribonucleic acids (DNA) with an ester derived from daunorubicine of the formula ##STR1## in which R.sub.1 represents a radical of the formula ##STR2## in which each X represents oxygen or sulfur and each R.sub.3 represents alkyl, phenyl or both R.sub.3 form together with one another an alkylene group, R.sub.4 is hydrogen, alkyl or phenyl and R.sub.2 is hydrogen or trifluoracetyl. Said complexes are usable for treating cancerous tumors.

Growing community of inventors

Winksele, Belgium

Andre B Trouet