Abstract: 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;R.sub.2 is COO(C.sub.1-3 alkyl) or CO-R.sub.7 where R.sub.7 isNH.sub.2 or an amino acid ester or peptide ester;R.sub.3 is H, CH.sub.3 or CHO;when R.sub.5 and R.sub.6 are taken separately, R.sub.6 is H and one of R.sub.4 and R.sub.5 is ethyl and the other is H or OH;when R.sub.5 and R.sub.6 are taken together with the carbon atoms to which they are attached, they form an oxirane ring and R.sub.4 is ethyl, andA is a residue of a bifunctional organic derivative of the maleoylamino acid or maleoyl peptide or maleoylphenoxy type.

Abstract: 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.

Abstract: 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,R.sub.2 represents a methoxy group, an amino group or an alpha-aminoacid ester radical which is bonded via a bond of the amide type and in which the ester group contains 1 to 6 carbon atoms, and R.sub.3 represents hydrogen or hydroxyl.

Abstract: 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;R.sub.2 is COO(C.sub.1-3 alkyl) or CO--R.sub.7 where R.sub.7 is NH.sub.2 or an amino acid ester or peptide ester;R.sub.3 is H, CH.sub.3 or CHO;when R.sub.5 and R.sub.6 are taken separately, R.sub.6 is H and one of R.sub.4 and R.sub.5 is ethyl and the other is H or OH;when R.sub.5 and R.sub.6 are taken together with the carbon atoms to which they are attached, they form an oxirane ring and R.sub.4 is ethyl, and A is a residue of a bifunctional organic derivative of the maleoylamino acid or maleoyl peptide or maleoylphenoxy type.

Abstract: 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.

Abstract: 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.

Abstract: The invention relates to a new pharmaceutical form of a medicament of the formulaCarrier-Spacer arm-Drugin which"Drug" represents an active principle provided with a free amino function"Spacer arm" represents a peptidic chain of the X-L-Leu type and"Carrier" is a proteinic macromolecule adapted to the drug.

Abstract: 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.