C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 275/32 (2006.01) A61K 31/27 (2006.01) A61K 39/395 (2006.01) A61K 48/00 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2496470
This invention pertains to certain enzyme (CPG2) activated self-immolative nitrogen mustard prodrugs, which are useful in enzyme prodrug therapy (EPT), such as ADEPT and GDEPT, for the treatment of proliferative conditions, such as cancer, and which have the following formula: wherein RN is independently C1-7alkyl; X1 is independently -I, -Br, or Cl; X2 is independently -I, -Br, or -Cl; the group -N(CH2CH2X1)(CH2CH2X2) is independently attached at the 2- position or at the 4-position; each RG is independently -H or an ester substituent; n is independently an integer from 0 to 4; each RP, if present, is independently a phenyl substituent; m is independently an integer from 0 to 4; each RM, if present, is independently a mustard substituent; and pharmaceutically acceptable salts, solvates, amides, and esters thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds; such compounds and compositions for use in methods of treatment of the human or animal body by therapy; the use of such compounds and compositions for the manufacture of medicaments for the treatment of proliferative conditions; and the like.
L'invention se rapporte à certains promédicaments activés par une enzyme (CPG2) auto-immolateurs à base de moutarde d'azote que l'on utilise dans la thérapie par promédicaments d'enzyme (EPT), dont ADEPT et GDEPT, pour le traitement d'états prolifératifs, dans le cancer, et ayant la formule suivante : dans laquelle R<SP>N</SP> désigne, pris indépendamment, alkyle C¿1-7?; X?1¿ désigne, pris indépendamment, -I, -Br, ou Cl; X?2¿ désigne, pris indépendamment, -I, -Br, ou -Cl; le groupe -N(CH¿2?CH¿2?X?1¿)(CH¿2?CH¿2?X?2¿) est fixé indépendamment à la position 2 ou à la position 4 ; chaque R<SP>G</SP> désigne, pris indépendamment, -H ou un substituant de l'ester; n désigne, pris indépendamment, un entier allant de 0 à 4; chaque R<SP>P</SP>, s'il y en a, désigne, pris indépendamment, un substituant phényle, m désigne, pris indépendamment, un entier allant de 0 à 4 ; chaque R<SP>M</SP>, s'il y a eu lieu, désigne pris indépendamment un substituant de moutarde ; et leurs sels, solvates, amides et esters pharmaceutiquement acceptables. La présente invention se rapporte également à des compositions pharmaceutiques contenant lesdits composés, lesdits composés et les compositions étant utilisés dans les méthodes de traitement du corps humain ou animal par thérapie ; à l'utilisation desdits composés et compositions pour la fabrication de médicaments destinés à traiter les états prolifératifs ; et analogues.¿ ?
Niculescu-Duvaz Dan M.
Niculescu-Duvaz Ion
Springer Caroline Joy
Cancer Research Technology Limited
Kirby Eades Gale Baker
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