Omnichem, S.a.

Omnichem

Jean A Hannart

Andre B Trouet

Kandukuri S Rao

Jean-Paul Dejonghe

Kandukuri S Bushana

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 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

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

The present invention is concerned with derivatives of 2,3,3a,4,5,6-hexahydro-1H-indolo(3,2,1-de)(1,5)naphthyridine of the formula ##STR1## in the form of base or acid addition salts, preferably with pharmaceutically acceptable acids, wherein one of the groups R1 and R2 represents a lower alkyl group and the other represents a hydrogen atom or R1 and R2 represent each independently an alkyl group or, together an alkanediyl group having from 4 to 6 carbon atoms. R3 represents a lower alkyl group, a hydrogen atom or a benzyl group. And either R5 represents a lower carboalkoxy group or a hydrogen atom and R6 represents with R4 an additional carbon-carbon bond; or R4 represents a hydrogen atom and R6 and R5 represent together an oxygen atom or respectively a hydrogen atom and a hydroxyl group.

4-alkylindolonaphthyridines and their therapeutical application

Compounds having the following general formula: ##STR1## wherein R is an alkyl or aminoalkyl group having 1 to 8 carbon atoms, or a hydrogen atom; R.sub.2 and R.sub.3 are either hydrogen atoms or, together, an additional carbon-carbon bond, as well as the mineral or organic acid addition salts thereof. These compounds are used as anti-arhythmic agents.

1,10-Dimethyl-2,7-dihydrooxayohimbanes an anti-arrhythmic use thereof

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.

Growing community of inventors

Dion-Valmont, Belgium

Jean A Hannart