New (aminopropyl)methylphosphinic acids

C - Chemistry – Metallurgy – 07 – F

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Details

C07F 9/30 (2006.01) A61K 31/662 (2006.01) A61P 1/04 (2006.01)

Patent

CA 2393510

Novel compounds of formula (I), with the exception of i) the racemate of (3- amino-2-hydroxypropyl)methylphosphinic acid; ii) S-(3-amino-2- hydroxypropyl)methylphosphinic acid; iii) R-(3-amino-2- hydroxypropyl)methylphosphinic acid; iv) (3-amino-2- hydroxypropyl)difluoromethylphosphinic acid; and v) (3-amino-2- oxopropyl)methylphosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

La présente invention concerne des composés représentés par la formule générale (I), à l'exception i) du racémate de l'acide (3-amino-2-hydroxypropyl)méthylphosphinique, ii) de l'acide S-(3-amino-2-hydroxypropyl)méthylphosphinique, iii) de l'acide R-(3-amino-2-hydroxypropyl)méthylphosphinique, iv) de l'acide (3-amino-2-hydroxypropyl)difluorométhylphosphinique, et v) de l'acide (3-amino-2-oxopropyl)méthylphosphinique, lesquels composés présentent une affinité envers l'un au moins des récepteurs GABA¿B?. L'invention concerne également certains de leurs sels pharmaceutiquement admis, leurs solvats et leurs stéréoisomères, ainsi qu'un procédé permettant leur élaboration. L'invention concerne enfin des compositions pharmaceutiques contenant ces composés thérapeutiquement actifs, et l'utilisation thérapeutique de ces composés actifs.

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