Abstract: The invention concerns the use of aromatic compounds capable of binding with G-quadruplex structures to produce medicines with anti-telomerase effect. Said compounds correspond to formula (I) wherein: R1, R2 and R3, identical or different, represent a hydrogen atom, or a —CH2—NH—(CH2)n—X group, wherein n is an integer from 2 to 4, and X is selected among —NH2—, —N(CH3)2 radicals, a heterocyclic radical such as piperidyl, imidazolyl, morpholinyl radical, or an indole-type condensed heterocyclic radical, —Z represents CH or N, each compound comprising two nitrogen atoms in the Z positions. The invention is useful for producing anticancer medicines.

Abstract: The present invention deals with a method for the generation of a dynamic combinatorial library of ligands for a given target, capable of binding at least two functionalities, which method comprises the following steps: (i) selecting a set of n molecules carrying functionalities which may bind to the target, which molecules are capable of reversibly binding to each other under formation of an entity, n being an integer ≧1: (ii) mixing together said set of said n molecules: (iii) subjecting the mixture to conditions allowing a reversible bond formation and cleavage under formation of entities carrying different combinations of functionalities, until equilibrium is reached: (iv) optionally transforming the said entities into ligands: (v) repeating steps (i) to (iv) n-times, each time a different molecule of said set of n molecules being omitted: (vi) assessing the ability of each of the mixtures obtained to bind to a given target.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphospahte (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering inositol hexaphospahte (IHP) to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: Transfecting compounds which include an aminoglycoside linked to a lipid via a spacer, and their polyguanidylated derivatives are provided. These compounds are useful for the in vitro, ex vivo, or in vivo transfection of nucleic acids into various cell types.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering inositol hexaphospahte (IHP) to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: Novel amidinium derivatives of formula (I), wherein R1 is a cholesterol derivative or an alkylamino-NR′R″ grouping, and each of R2 and R3 is independently a hydrogen atom or a grouping of formula (II), wherein each of R4 and R5 is independently a hydrogen atom or a grouping of formula (III), are disclosed. The corresponding pharmaceutical compositions, which are particularly useful in gene therapy for transferring therapeutic genes into cells, are also disclosed.

Abstract: Novel amidinium derivatives of formula (I), wherein R1 is a cholesterol derivative or an alkylamino-NR'R" grouping, and each of R2 and R3 is independently a hydrogen atom or a grouping of formula (II), wherein each of R4 and R5 is independently a hydrogen atom or a grouping of formula (III), are disclosed. The corresponding pharmaceutical compositions, which are particularly useful in gene therapy for transferring therapeutic genes into cells, are also disclosed.

Abstract: The invention relates to rare earth cryptates consisting of at least one rare earth salt complexed by a macropolycyclic compound corresponding to one of formulae I or II below, in which:the ring ##STR1## is the N.sub.2 O.sub.4 macrocycle, the N.sub.2 O.sub.3 macrocycle or the bis--bipyridine macrocycle;Y is a spacer arm or group which consists of a divalent organic radical selected from linear or branched C.sub.1 to C.sub.20 alkylene groups optionally containing one or more double bonds and/or optionally being interrupted by one or more heteroatoms such as oxygen, nitrogen, sulfur or phosphorus, or from C.sub.5 to C.sub.8 cycloalkylene groups or C.sub.6 to C.sub.14 arylene groups, the said alkylene or arylene groups optionally being substituted by alkyl, aryl or sulfonate groups;Z is a functional group capable of bonding covalently with a biological substance;R is a methyl group or represents the group --Y--Z; andR' is hydrogen or a group --COOR", in which R" is a C.sub.1 to C.sub.

Abstract: The invention relates to rare earth cryptates consisting of at least one rare earth salt complexed by a macropolycyclic compound corresponding to one of formulae I or II below, in which:the ring ##STR1## is the N.sub.2 O.sub.4 macrocycle, the N.sub.2 O.sub.3 macrocycle or the bis-bipyridine macrocycle;Y is a spacer arm or group which consists of a divalent organic radical selected from linear or branched C.sub.1 to C.sub.20 alkylene groups optionally containing one or more double bonds and/or optionally being interrupted by one or more heteroatoms such as oxygen, nitrogen, sulfur or phosphorus, or from C.sub.5 to C.sub.8 cycloalkylene groups or C.sub.6 to C.sub.14 arylene groups, the said alkylene or arylene groups optionally being substituted by alkyl, aryl or sulfonate groups;Z is a functional group capable of bonding covalently with a biological substance;R is a methyl group or represents the group --Y--Z; andR' is hydrogen or a group --COOR", in which R" is a C.sub.1 to C.sub.

Abstract: The invention relates to macrocyclic rare earth complexes which consist of at least one rare earth salt complexed by a macrocyclic compound of formula (I): ##STR1## in which: the bivalent radicals A, B, C and D, which are identical or different, are hydrocarbon chains optionally containing one or more heteroatoms, at least one of said radicals containing at least one molecular unit or essentially consisting of a molecular unit possessing a triplet energy greater than the energy of the emission level of the complexed rare earth ion, at least one of said radicals consisting of a substituted or unsubstituted nitrogen-containing heterocyclic system in which at least one of the nitrogen atoms carries an oxy group, and it being possible for one of the radicals C or D not to exist; andX.sub.1 and X.sub.2, which are identical or different, are hydrogen or a hydrocarbon chain (CH.sub.2).sub.

Abstract: The invention relates to macropolycyclic rare earth complexes, namely cryptates which are useful as fluorescent tracers.

Abstract: The invention relates to rare earth cryptates consisting of at least one rare earth salt complexed by a macropolycyclic compound corresponding to one of formulae I or II below, in which:the ring ##STR1## is the N.sub.2 O.sub.4 macrocycle, the N.sub.2 O.sub.3 macrocycle or the bis-bipyridine macrocycle;Y is a spacer arm or group which consists of a divalent organic radical selected from linear or branched C.sub.1 to C.sub.20 alkylene groups optionally containing one or more double bonds and/or optionally being interrupted by one or more heteroatoms such as oxygen, nitrogen, sulfur or phosphorus, or from C.sub.5 to C.sub.8 cycloalkylene groups or C.sub.6 to C.sub.14 arylene groups, the said alkylene or arylene groups optionally being substituted by alkyl, aryl or sulfonate groups;Z is a functional group capable of bonding covalently with a biological substance;R is a methyl group or represents the group --Y--Z; andR' is hydrogen or a group --COOR", in which R" is a C.sub.1 to C.sub.

Abstract: The invention relates to pharmaceutical compositions for peroral administration comprising (a) pharmaceutically useful methanediphosphonic acid derivatives, e.g. those of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the specification, or pharmaceutically acceptable salts thereof, (b) specific macrocyclic polyethers and optionally (c) pharmaceutically acceptable adjuvants. The pharmaceutical compositions are prepared in a manner known per se. A method of treating hypercalcemia and osteolytic bone metastases with these compositions is also disclosed herein.

Abstract: The invention relates to macropolycyclic rare earth complexes, namely cryptates which are useful as fluorescent tracers.

Abstract: The invention relates to rare earth cryptates consisting of at least one rare earth salt complexed by a macropolycyclic compound corresponding to one of formulae I or II below, in which:the ring ##STR1## is the N.sub.2 O.sub.4 macrocycle, the N.sub.2 O.sub.3 macrocycle or a bis-bipyridine macrocycle;Y is a spacer arm or group which consists of a divalent organic radical selected from linear or branched C.sub.1 to C.sub.20 alkylene groups optionally containing one or more double bonds and/or optionally being interrupted by one or more heteroatoms such as oxygen, nitrogen, sulfur or phosphorus, or from C.sub.5 to C.sub.8 cycloalkylene groups or C.sub.6 to C.sub.

Abstract: The invention relates to macropolycyclic rare earth complexes, namely cryptates which are useful as fluorescent tracers.

Abstract: A process for the anionic polymerization or copolymerization of olefinic monomers, dienic monomers, vinyl monomers and heterocyclic monomers is described which comprises reacting at least one monomer which is an olefinic monomer, a vinyl monomer or an heterocyclic monomer with a catalyst capable of inducing anionic polymerization and an aprotic macroheterocyclic cryptant, said at least one monomer being the only medium for the reaction.The macroheterocyclic complexing agent has general formula ##STR1## in which: R.sub.1 is hydrogen, a hydrocarbon radical or alkoxycarbonyl, or the two R.sub.1 together can form a group of the general formula: ##STR2## in which A is a hydrocarbon radical,D is oxygen, sulfur, or a hydrocarbon radical, with the proviso that at leat two of the D groups are oxygen or sulfur and that if R.sub.1 is hydrogen, a hydrocarbon radical or alkoxycarbonyl, one of these two D groups is oxygen or sulfur and the other is oxygen, andn and p are integers from 1 to 3 and m is 2 or 3.

Abstract: Novel macrocyclic (monocyclic and bicyclic) compounds having nitrogen bridgehead atoms and having in the hydrocarbon bridging chains at least two additional hetero atoms selected from the group consisting of sulfur, oxygen, and nitrogen, when admixed with a compatible cation-donor compound form stable cation-containing macrocyclic complexes which, in turn, can be conveniently dissociated by addition of acid or a quaternizing agent. The novel macrocyclics are valuable for use in the same way and for the same purposes as chelating agents.

Abstract: A novel process for polymerization or copolymerization of monomers is described, according to which the reaction is carried out in the presence of an anionic initiator and a macroheterocyclic complexing agent of formula ##STR1## in which: EACH R.sub.1 is a hydrogen atom, a hydrocarbon group or an alkoxycarbonyl group, or the two R.sub.1 together can form a group of the general formula: ##STR2## THAT IS TO SAY FORMING A THIRD BRIDGE BETWEEN THE TWO NITROGEN ATOMS IN THE MOLECULE, A is a hydrocarbon group,D is an oxygen or sulfur atom or a hydrocarbon group, with the proviso that at least two of the groups D are oxygen or sulfur atoms and that, if each R.sub.1 is hydrogen, a hydrocarbon group or an alkoxycarbonyl group, one of these two groups D is oxygen or sulfur and the other is oxygen,n and p are integers ranging from 1 to 3, andm is 2 or 3.