摘要:
The present invention relates to hydroxy-bisphosphonic acid derivatives corresponding to general formula (I): in which: - n and m denote, independently of one another, an integer ranging from 1 to 4, - X denotes an oxygen atom or an N-R3 group, - R1 and R3 denote, independently of one another, a linear or branched C1 to C6 alkyl group, and - R2 denotes a residue of a molecule of therapeutic or diagnostic interest, or pharmaceutically acceptable salts of said derivatives, and also the method for the preparation thereof and the therapeutic or diagnostic use thereof.
摘要:
The present invention relates to a method for preparing a hydroxy-bisphosphonic acid derivative or a salt thereof, from the corresponding carboxylic acid, comprising the following steps: - activation of the carboxylic acid function in the form of the boronate derivative thereof through the action of a borane, then - reaction with tris(trimethylsilyl)phosphite, under Arbuzov conditions - treatment with an alcohol, chosen in particular from an aliphatic alcohol or trifluoromethanol, and - separation of the hydroxy-bisphosphonic acid derivative formed, from the reaction medium.
摘要:
The present invention concerns a compound having the following formula (I):
wherein: - A is in particular -N(R' a )-C(=O)-R, R' a being H or a (C 1 -C 6 )alkyl group, and R being preferably a group having the following formula (II):
- X is in particular chosen from the group consisting of: -SO 2 -N(R' b )-, R' b being H or a (C 1 -C 6 )alkyl group, -N(R" b )-SO 2 -, R" b being H or a (C 1 -C 6 )alkyl group, -CO-NH-, and -NH-CO-, for use for the treatment of cancers, such as metastatic cancers.