Abstract: Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion.

Abstract: The invention relates to novel cytotoxic agents comprising taxanes and their therapeutic use as a result of delivering the taxanes to a specific cell population in a targeted fashion by chemically linking the taxane to a cell binding agent.

Abstract: Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion.

Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzodiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.

Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzothiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds and to intermediate precursors to such compounds.

Abstract: The present invention relates to dimers of artemisinin derivatives, to processes for the preparation of such dimers, to methods of treatment comprising administration of such dimers, and to intermediates to such dimers.

Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.

Abstract: The present invention relates in particular to novel chemical compounds, particularly to novel organophosphorus derivatives of indazoles, to the compositions containing them, and to the use thereof as medicinal products for treating cancers.

Abstract: The present invention is related to new tomaymycin derivatives, their process of preparation and their therapeutic uses.

Abstract: The invention relates to novel cytotoxic agents comprising taxanes and their therapeutic use as a result of delivering the taxanes to a specific cell population in a targeted fashion by chemically linking the taxane to a cell binding agent.

Abstract: New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them. In general formula (I), Ar represents an aryl radical, R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.

Abstract: The present invention relates in particular to novel chemical compounds, particularly to novel organophosphorus derivatives of indazoles, to the compositions containing them, and to the use thereof as medicinal products for treating cancers.

Abstract: The invention concerns novel derivatives of formula (I) wherein: R1 represents the stereoisomeric forms of the chain —(CHOH)3—CH2—O—COR (II) and either R2 represents a hydrogen atom and R3 represents the stereoisomeric forms of the chain —CH2—(CHOH)2—CH2—O—COR (III) or R2 represents the stereoisomeric forms of the chains —(CHOH)3—CH2—O—COR (II) or —CH2—(CHOH)2—CH2—O—COR (III) and R3 represents a hydrogen atom and R represents —(Alk)1—(Cycloalk) radical; i is equal to 0 or 1; Alk represents and alkyl radical, Cycloalk represents a cycloalkyl radical, and their salts with a inorganic or organic acid, their preparation and the medicines containing as active principle at least a product of general formula (I) or its salts with a inorganic or organic acid.

Abstract: Group A streptogramin derivatives of formula (I): the salts thereof, and mixtures of stereoisomers thereof, as well as processes for preparing them and pharmaceutical compositions comprising them are disclosed.

Abstract: The invention is directed to physiologically active compounds of formula (I): wherein R1 represents R3—Z3—, R3—L2—R4—Z3—, R3—L3—Ar1—L4—Z3— or R3—L3—Ar1—L2—R4—Z3—; R2 represents hydrogen, halogen, lower alkyl or lower alkoxy; A1 represents a straight chain C2-3alkylene linkage optionally substituted by one or more groups chosen from alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, imino, oxo, thioxo, or alkyl substituted by —ZR6, —NY1Y2, —CO2R6 or —C(═O)—NY1Y2; L1 represents a direct bond; an alkenylene, alkylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage each optionally substituted by (a) an acidic functional group, cyano, oxo, —S(O)mR9, R3, —C(═O)—R3, —C(═O)—OR3, —N(R8)—C(═O)—R9, —N(R8)—C(═O)—OR9, —N(R

Abstract: The invention is directed to physiologically active compounds of formula (I) wherein R1 represents R3—Z3—, R3—L2—R4—Z3—, R3—L3—Ar1—L4—Z3— or R3—L3—Ar1—L2—R4—Z3—; R2 represents hydrogen, halogen, lower alkyl or lower alkoxy; A1 represents a straight chain C1-3alkylene linkage optionally substituted by one or more groups chosen from alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, imino, oxo, thioxo, or alkyl substituted by —ZR6, —NY1Y2, —CO2R6 or —C(═O)—NY1Y2; L1 represents a direct bond; an alkenylene, alkylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage each optionally substituted by (a) an acidic functional group, cyano, oxo, —S(O)mR9, R3, —C(═O)—R3, —C(═O)—OR3, —N(R8)—C(═O)R9, —N(R8)—SO2—R9, —NY4Y5 or —[C

Abstract: Methods of preparing methylthiomethyloxy taxoids of formula (XXXIV) from baccatin and &bgr;-lactam are presented. These new taxoids display noteworthy anti-tumor and anti-leukemic properties.

Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them.

Abstract: The invention is directed to physiologically active compounds of formula (I): wherein one of A1, A2 and A3 represents NR2 and the others represent C(R3)(R4); R1 represents R5Z1—Het— or R6N(R7)—C(═O)—NH—Ar2—; Ar1 represents aryldiyl or heteroaryldiyl; L1 represents a —R12-R13— linkage (where R12 is a direct bond or an alkylene chain, an alkenylene chain or an alkynylene chain and R13 is a direct bond, cycloalkylene, heterocycloalkylene, aryldiyl, heteroaryldiyl, —C(═Z3)—NR11—, —NR11—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR11)—, —NR11—, —NR11—C(═Z3)—NR11—, —SO2—NR11—, —NR —SO2—, —O—C(═O)—, —C(═O)—O—, —NR11—C(═O)—O— or —O—C(═O)—NR11—); and their prodrugs, and pharmaceutically accepta

Abstract: A method for preparing an oxazolidinecarboxylic acid of general formula (I), which is useful for preparing therapeutically active taxoids of general formula (III), from an oxazolidinecarboxylic acid of general formula (II). In formulae (I), (II) and (III), R is a hydrogen atom or an acetyl radical; R1 is a benzyl radical or a radical of the general formula R2—O—CO—, wherein R2 is an optionally substituted alkyl radical, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl; each of R3 and R4, which are the same or different, is hydrogen, alkyl, alkoxy, optionally substituted aryl or optionally substituted aralkyl, or together they form a 4-7 membered ring; R5 is alkenyl, alkynyl, phenyl, formyl, alkanoyl, aroyl, hydroxymethyl, carboxy or alkyloxycarbonyl; and R′ is a hydrogen atom or an alkali or alkaline-earth metal atom or an alkyl radical with 1-4 carbon atoms optionally substituted by phenyl radical.