New phosphonates, process for preparing the same and...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/59 (2006.01) A61K 31/675 (2006.01) C07F 9/553 (2006.01) C07F 9/572 (2006.01)

Patent

CA 2271814

Compounds have the formula (I), in which R1, R2 are the same or different and represent a hydrogen atom, an alkyl group, a cycloalkyl group, an hydroxyalkyl group, an alkenyl group, an alkinyl group or an aralkyl group or R1 and R2 form together an alkylene radical which forms with the bonded oxygen atoms and the phosphorus atom that carries the oxygen atoms a saturated 5- to 8-membered ring; R3 is an optionally substituted amino group, an alkyl group, a cycloalkyl radical or an optionally substituted aryl radical; n is an integer between 1 and 4. Also disclosed are hydrates, solvates and physiologically tolerable salts of these compounds, their optically active forms, processes for preparing the same and medicaments with factor Xa-inhibiting properties containing these compounds.

Ces composés répondent à la formule (I), dans laquelle R?1¿, R?2¿ sont identiques ou différents et désignent un atome d'hydrogène, un groupe alkyle, un groupe cycloalkyle, un groupe hydroxyalkyle, un groupe alcényle, un groupe alcinyle ou un groupe aralkyle ou R?1¿ et R?2¿ forment ensemble un radical alcylène qui forme avec les atomes d'oxygène liés et l'atome de phosphore qui porte les atomes d'oxygène un anneau saturé à 5 ou 8 membres; R?3¿ est un groupe amine le cas échéant substitué, un groupe alkyle, un radical cycloalkyle ou un radical aryle le cas échéant substitué; n est un nombre entier entre 1 et 4. L'invention concerne également les hydrates, les solvates et les sels physiologiquement admissibles de ces composés, leurs formes optiquement actives, leurs procédés de préparation et des médicaments à propriétés inhibitrices du facteur Xa qui contiennent ces composés.

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