Abstract: The use of isoquinolones for preparing drugs, including novel isoquinolones as well as their synthesis method. In particular, isoquinolone derivatives used in the treatment of pathological angiogenesis, and more particularly of cancer.

Abstract: The use of isoquinolones for preparing drugs, including novel isoquinolones as well as their synthesis method. In particular, isoquinolone derivatives used in the treatment of pathological angiogenesis, and more particularly of cancer.

Abstract: The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) wherein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoid of sulfydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.

Abstract: The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) whrein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoidof sulfydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.

Abstract: The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) wherein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoid of sulfhydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.

Abstract: The present invention relates to the use of a Shiga toxin B-subunit moiety as carrier for therapeutic agents, for example, anti-cancer agents such as anti-cancer agents that require intracellular uptake to exert their anti-cancer effects. In particular, the present invention provides conjugates comprising a Shiga toxin moiety covalently linked to an anti-cancer agent through a self-immolative spacer, and methods of using such conjugates to increase cellular uptake and/or specificity for cancer cells of the anti-cancer drug. Also provided are methods of treatment involving administration of such conjugates, and pharmaceutical compositions and kits useful for carrying out such methods of treatment.

Abstract: The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) wherein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoid of sulfhydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.

Abstract: The present invention concerns novel dibenzo[c,h][1,5]naphthyridine of formula (I) and their use as DNA probes, as well as the methods for marking DNA using the same.

Abstract: The invention relates to new compounds for cancer therapy or diagnosis and to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein-STxB is the Shiga Toxin B subunit or a functional equivalent thereof, -Z(n) wherein n is 0 or 1, Z is an amino-acid residue devoid of sulfydryl groups, or is a polypeptide, -T is a molecule linked by a covalent bound to the S part of Cys, selected from: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, - Y(m) wherein m is 0 or 1, Y is a linker between T and Cys, which is either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into cells.

Abstract: The present invention concerns novel dibenzo[c,h][1,5]naphthyridine of formula (I) and their use as DNA probes, as well as the methods for marking DNA using the same.

Abstract: The present invention relates to methods for the preparation of toxin conjugates that are useful in vaccination and other therapies and diagnostics. In particular, methods are provided that involve a [3+2] cycloaddition between a first reactive unsaturated group on a toxin moiety and a second reactive unsaturated group on a bioactive moiety. Also provided are conjugates that are formed through this conjugation method, pharmaceutical compositions comprising these conjugates, and methods of using these pharmaceutical compositions for the treatment or diagnostic of antigen-related conditions, including tumors and infections.

Abstract: The invention relates to new compounds for cancer therapy or diagnosis and to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein—STxB is the Shiga Toxin B subunit or a functional equivalent thereof, —Z(n) wherein n is 0 or 1, Z is an amino-acid residue devoid of sulfydryl groups, or is a polypeptide, —T is a molecule linked by a covalent bound to the S part of Cys, selected from: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, —Y(m) wherein m is 0 or 1, Y is a linker between T and Cys, which is either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into cells.

Abstract: Glycosyl-spacer-drugs compounds (prodrugs), their preparation and their use as pharmaceuticals are described.

Abstract: Glycosyl-spacer-drugs compounds (prodrugs), their preparation and their use as pharmaceuticals are described.

Abstract: Compounds of the formula Iglycosyl-Y?--C(.dbd.Y)--X--!.sub.p --W(R).sub.n --Z--C(.dbd.Y)-active compound (I)are described which are suitable for the treatment of carcinomatous diseases, autoimmune diseases and chronic inflammatory diseases such as rheumatoid arthritis.

Abstract: Substrate-spacer-prodrug compounds (pro-prodrugs) suited for site specific delivery of drugs, a process of preparing them and their use are described.

Abstract: Enzymatically clearable prodrugs with reduced Michaelis-Menten constant (Km) are described.

Abstract: Glycosylated prodrugs, a preparation method therefor, and their use with tumor-specific immunoenzymatic conjugates for the treatment of cancer, are described. These anthracycline prodrugs have formula (I).

Abstract: The present invention relates to new tetralins and their use for the preparation of anthracyclinones and anthracyclins. These tetralins contain at least one chiral carbon atom and correspond to the formula (V) below: ##STR1## in which: R.sub.1 and R.sub.2 denote a hydrogen atom, or a halogen atom or the group OCH.sub.3, provided that one of the two substituents (R.sub.1 or R.sub.2) must denote OCH.sub.3, andR.sub.3 denotes a hydrogen atom or the OR' group, R' being hydrogen or a hydroxyl-protecting group. Application: synthesis of glycosides of great therapeutic value.