Abstract: This invention relates to transferase inhibitors of the formula (I), their preparation, and pharmaceutical compositions containing them. ##STR1## In formula (I), R.sub.1 is Y--S--A.sub.1 --(Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl radical, an alkoxycarbonyl radical, or an R.sub.4 --S-- radical in which R.sub.4 is an alkyl radical containing 1 to 4 carbon atoms optionally substituted by a phenyl radical or a radical of the formula (II) ##STR2## in which A.sub.1 is an alkylene radical containing 1 to 4 carbon atoms optionally substituted at the position a in the grouping >C(X.sub.1)(Y.sub.1) with an amino, alkylamino, dialkylamino, alkanoylamino, or alkoxycarbonylamino radical); X.sub.1 and Y.sub.1 are each a hydrogen atom or form, together with the carbon atom to which they are connected, a >C.dbd.O grouping; R'.sub.1 is hydrogen or methyl; R.sub.

Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. ##STR1## In general formula (I), for example, Ar represents an aryl radical,R represents an alkoxyacetyl radical,R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 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 to new process for the preparation of .beta.-phenylisoserine and its analogues of general formula: ##STR1## which are particularly useful for preparing taxane derivatives which have remarkable antitumour and antileukaemic activities.

Abstract: Novel farnesyl transferase inhibitors of general formula (I) ##STR1## preparation thereof and pharmaceutical compositions containing same. In general formula (I), R.sub.1 is Y--S--A.sub.1 -- (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, or an alkyl or alkoxycarbonyl radical, and A.sub.1 is a C.sub.1-4 alkylene radical optionally .alpha.-substituted in the >C(X.sub.1) (Y.sub.1,) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical wherein the alkyl or alkanoyl portion contains 1-6 carbon atoms; each of X.sub.1 and Y.sub.1 is a hydrogen atom or X.sub.1 and Y.sub.1, taken toether with the carbon atom to which they are attached, form a >C.dbd.O grouping; R'.sub.1 is hydrogen or a C.sub.1-6 alkyl radical; X is an oxygen or sulphur atom; R.sub.2 is a C.sub.1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl.

Abstract: This invention relates to a process for the preparation of 7-hydroxy taxanes of general formula (I) from 7-trialkylsilyl taxanes of general formula (II), wherein R.sub.1 is hydrogen, alkoxy, acyloxy, or alkoxyacetoxy, and Z is a hydrogen atom or a radical of general formula (III), wherein R.sub.2 is an optionally substituted benzyl radical or an R'.sub.2 --O--CO-- radical wherein R'.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical, R.sub.3 is an aromatic alkyl, alkenyl, alkynyl, cycloalyl, phenyl, naphthyl or heterocyclyl radical and either R.sub.4 is a hydrogen atom and R.sub.5 is a hydroxyl function protecting group, or R.sub.4 and R.sub.5 together form a saturated 5- or 6-membered heterocylic ring. In general formula (II), each R, which are the same or different, is an alkyl radical optionally substituted by a phenyl radical.

Abstract: This invention relates to a method of preparing taxane derivatives of formula (I) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. The products of formula (I) have remarkable antitumor and antileukemia properties. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is a benzoyl radical or an R.sub.2 --O--CO-- radical in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1.

Abstract: This invention relates to a process for preparing taxoid derivatives of formulae II and XI: ##STR1## in which Ar represents an aryl radical; R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl, or saturated or unsaturated heterocyclic radical; R.sub.3 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, saturated or unsaturated heterocyclic, or aryl radial, but not a phenyl radical; R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydroxyl-protecting group or R.sub.4 and R.sub.5 together form a heterocyclic group; G.sub.1 represents a hydroxyl-protecting group; and G.sub.

Abstract: Method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetyl-baccatine III by means of an acid of general formula (VII), deprotection of the side chain and elimination of the hydroxy function protection groupings. In general formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 --O--CO-- in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, and R.sub.3 is hydrogen, alkoxy, optionally substituted aryl.

Abstract: This invention relates to a method of preparing taxane derivatives of formula (I) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. The products of formula (I) have remarkable antitumor and antileukemia properties. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is a benzoyl radical or an R.sub.2 --O--CO-- radical in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1.

Abstract: This invention relates to a method for the preparation of taxane derivatives having the formula (I) and pharmaceutical compositions which contain the derivatives thus obtained. In formula (I), R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 --O--CO wherein R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl and Het is a 5-membered optionally substituted aromatic heterocycle (thiophene, tiazole, furan, pyrrole, imidazole, oxazole, isoxazole, pyrazole). The products of formula (I) have remarkable antitumor and antileukemia properties.

Abstract: Taxoids having a 1,3-oxazole containing moiety at the 13-position of the taxane nucleus.

Abstract: The invention relates to a process for preparing taxoids of formula I herein that includes the steps of esterifying a baccatin III derivative of the formula VI herein, acylating the compound obtained, and optionally removing a protecting group to give the desired taxoid product.

Abstract: New Baccatin III derivatives are disclosed for use in making taxoid compounds having formula (I) illustrated herein that exhibit antitumor activity.

Abstract: The invention relates to a process for preparing taxoids of formula I herein that includes comprising the steps of esterifying a baccatin III derivative of the formula VI herein, treating the compound obtained in acidic medium, and optionally removing a protecting group to give the desired taxoid product.

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,R.sub.1 represents a benzoyl radical or a radical of formulaR.sub.2 --O--CO-- in which R.sub.2 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 antitumour activity.

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,R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 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: New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I),Ar represents an aryl radicalR represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical,R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radicalThe new products of general formula (I) have a remarkable antitumour activity.

Abstract: A method for preparing taxane derivatives having general formula (I), novel derivatives thereby obtained and compositions containing same. In general formula (I), R is t.butoxy or phenyl, R.sub.1 is hydrogen or acetyl, and Ar is substituted phenyl or optionally substituted .alpha. or .beta.-naphthyl. These novel taxane derivatives are useful as antileukemic and antitumoral agents.