C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 9/24 (2006.01) A61K 31/66 (2006.01) A61K 47/48 (2006.01) C07K 4/00 (2006.01)
Patent
CA 2215264
The composition, synthesis, and applications of tumor associated protease activated prodrugs of phosphoramide mustard, isophosphoramide mustard and analogs with detoxification functionalities are described. These drugs release a cytotoxic phosphoramide mustard analog following activation by tumor associated proteases and esterases. The general structure for these drugs is (I), wherein R1 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; wherein X is a good leaving group such as a halogen; R2 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; or an amino group (NH2) which may optionally be substituted. Wherein A is a benzyloxy derivative with one or more acyloxy or acylamino groups in para or ortho positions relative to the phosphoester; and wherein the acyloxy or acylamino groups are not (substituted or unsubstituted)p-guanidino-benzoyloxy groups or p-guanidino-benzoylamino groups.
L'invention porte sur la composition, la synthèse et les applications de prodrogues de la moutarde phosphoramidique, de la moutarde isophosphoramidique et de leurs analogues possédant des fonctions de détoxification, qui sont activées par les protéases tumorales. Ces drogues libèrent un analogue cytotoxique de la moutarde phosphoramidique après activation par des protéases et des estérases tumorales. Ces drogues possèdent la structure générale (I), dans laquelle R1 est un groupe bêta-X-éthyl-amino dont les atomes d'azote ou de carbone peuvent facultativement porter des substituants; dans lequel X est un bon groupe nucléofuge tel un halogène; R2 est un groupe bêta-X-éthyl-amino dont les atomes d'azote ou de carbone peuvent facultativement porter des substituants; ou un groupe amino (NH2) pouvant facultativement porter des substituants. Dans laquelle A est un dérivé benzyloxy possédant un ou plusieurs groupes acyloxy ou acylamino en position para ou ortho par rapport au phosphoester; et dans lequel les groupes acyloxy ou acylamino ne sont pas des groupes p-guanidino-benzoyloxy ou p-guanidino-benzoylamino (substitués ou non substitués).
Borden Ladner Gervais Llp
Drug Innovation & Design Incorporated
LandOfFree
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