C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 9/38 (2006.01) A61K 31/662 (2006.01) A61P 19/02 (2006.01) A61P 35/00 (2006.01) C07F 9/40 (2006.01)
Patent
CA 2521384
The present invention provides a compound of the following formula (I): R3-NH- C(=X)-P(=O)OR1OR2including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrical 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 each 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 guanidino; and R3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino and guanidino; with the proviso that when X is O, R3 is not cyclohexylmethyl, and when X is S, R3 is not cyclohexyl. The invention further provides pharmaceutical compositions comprising the above compounds and their use in medicine.
La présente invention a trait à un composé de formule (I) : R?3¿-NH-C(=X)-P(=O)OR?1¿OR?2¿ y compris des sels, solvates, hydrates et polymorphes pharmaceutiquement acceptables des composés de formule (I), ainsi que des isomères géométriques et des formes optiquement actives des composés de formule (I) et des sels, solvates, hydrates et polymorphes desdits isomères et formes, dans laquelle : R?1¿ et R?2¿, identiques ou différents, sont choisis chacun parmi hydrogène, acyloalkyle et aryle ou R?1¿ et R?2¿ peuvent ensemble former avec les atomes d'oxygène et de phosphore un noyau dioxaphosphacycloalcane ; X est O ou S ; et R?3¿ est choisi, lorsque X est O, parmi bicycloalkyle, cycloalkylalkyle, et cycloalkyle substitué par au moins un parmi alkyle, amino et guanidino ; et R?3¿ est choisi, lorsque X est S, parmi bicycloalkyle, cycloalkylalkyle et cycloalkyle éventuellement substitué par au moins un parmi alkyle, amino, amidino et guanidino ; à condition que lorsque X est O, R?3¿ n'est pas cyclohexylméthyle, et lorsque X est S, R?3¿ n'est pas cyclohexyle. L'invention a également trait à des compositions pharmaceutiques comprenant lesdits composés et leur utilisation en médecine.
Breuer Eli
Golomb Gershon
Katz Yiffat
Reich Reuven
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
Yissum Research Development Company Of The Hebrew University Of
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