摘要:
The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.
摘要:
The invention relates to novel fluorescent derivatives of polyamines having a benzoxadiazole group, to a method for preparing the same and to the use thereof as diagnosis tools for emphasising the polyamine transport system in cancerous cells in order to adapt the treatment thereof, and thus for selecting patients carrying such tumours in order to adapt their treatment. The derivatives are of the formula (I) or a pharmaceutically acceptable salt thereof, in which: R1 is one or more NO2 groups in position 4 or 6, or a SO2Ph, SO2NMe2, SO2NH2 or SO3H group; R2 is hydrogen, C1-6 alkyl, benzyl, a perfluoroalkyl group; the values of a, b, c range from 2 to 5 independently from each other and represent alkylene chains separating the amino groups, and the values of d and e can independently be 0 or 1.
摘要:
The invention relates to compounds of general formula (1) in which R1=H, F or OCH3 and may occupy the 2, 3, 4 or 5 position on the aromatic carbocycle, R2=H or CH3, R3=H, CH3, OH or OCH3, R4=H and R3 and R4 together can be a carbonyl group (C=0), the addition salts and optionally the hydrates of additional salts with pharmaceutically-acceptable mineral or organic acids and the isomers and tautomers thereof.
摘要:
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.
摘要:
Compound of the formula (I) in which R' is a hydrogen atom or a radical R and R is an acyl residue. The invention also concerns the use of said compounds in the treatment of cancer and pharmaceutical compositions comprising said compounds. ##STR1##
摘要:
The present invention relates to a new process for the preparation of (poly)aminoalkylaminoacetamide derivatives of epipodophyllotoxin and salts thereof, characterized in that it comprises a step of peptide coupling of 4-amino-4′-demethylepipodophyllotoxin with an amine-containing reactant having protecting groups.
摘要:
The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamidc, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C1-4alkyl, —A represents CO(CH2)n or CONH(CH2)n where n=2, 3, 4, or 5, —R1 and R2 are as described herein.
摘要:
The invention relates to novel fluorescent derivatives of polyamines having a benzoxadiazole group, to a method for preparing the same and to the use thereof as diagnosis tools for emphasising the polyamine transport system in cancerous cells in order to adapt the treatment thereof, and thus for selecting patients carrying such tumours in order to adapt their treatment. The derivatives are of the formula (I) or a pharmaceutically acceptable salt thereof, in which: R1 is one or more NO2 groups in position 4 or 6, or a SO2Ph, SO2NMe2, SO2NH2 or SO3H group; R2 is hydrogen, C1-6 alkyl, benzyl, a perfluoroalkyl group; the values of a, b, c range from 2 to 5 independently from each other and represent alkylene chains separating the amino groups, and the values of d and e can independently be 0 or 1.
摘要:
The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C1-4alkyl, —A represents CO(CH2)n or CONH(CH2)n where n=2, 3, 4, or 5, —R1 and R2 are as described herein.
摘要:
The invention relates to a method for synthesizing 4β-amino-4′-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4β-halogenoacetamido-4′-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4β-amino-4′-demethyl-4-desoxypodophyllotoxin.