NEW CARBAMOYL-AND THIOCARBAMOYL-PHOSPHONATES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM

The present invention provides a compound of the following formula (I): R3-N H- C(=X)-P(=O)OR1OR2including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrica l isomers and optically activeforms of the compounds of formula I and p...

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Hauptverfasser: BREUER, ELI, GOLOMB, GERSHON, KATZ, YIFFAT, REICH, REUVEN
Format: Patent
Sprache:eng ; fre
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Zusammenfassung:The present invention provides a compound of the following formula (I): R3-N H- C(=X)-P(=O)OR1OR2including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrica l isomers and optically activeforms of the compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates and polymorphs of said isomers and forms, wherein R' and R2 may be the same or different and are ea ch selected from hydrogen, acyloxyalkyl and aryl or R1 and R2 may form together with the oxygen and phosphorus atoms a dioxaphosphacycloalkane ring; X is 0 or S; and R3 is selected, when X is 0, from bicycloalkyl, cycloalkylalkyl and substituted cycloalkyl by at least one of alkyl, amino, amidino and guanidin o; and R3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino a nd guanidino; with the proviso that when X is O, R3 is not cyclohexylmethyl, an d when X is S, R3 is not cyclohexyl. The invention further provides pharmaceutical compositions comprising the above compounds and their use in medicine.