C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 275/34 (2006.01) A61K 31/265 (2006.01) A61K 31/27 (2006.01) A61K 31/275 (2006.01) C07C 271/28 (2006.01) C07C 271/54 (2006.01) C07C 275/32 (2006.01) C07C 309/66 (2006.01) C07C 309/73 (2006.01) C07C 309/77 (2006.01) C07C 323/34 (2006.01)
Patent
CA 2210347
The invention provides compounds of formula (I) and (II) wherein X and Y are independently chlorine, bromine, iodine, a mesyl group CH3SO3 or a tosyl group OSO2phenyl (wherein phenyl is optionally substituted by 1, 2, 3, 4 or 5 substituents independently selected from C1-4alkyl, halogen, cyano or nitro; R1 and R2 are independently 1 to 4 optional substituents; Z1 and Z2 are each independently -O- or -NH-; R3 is hydrogen, t-butyl or allyl; Z3 is a hydrocarbyl group such as carboxyethyl, optionally containing heteroatoms, and physiologically acceptable derivatives thereof. The compounds can be converted in situ into nitrogen mustard agents by the actions of enzymes such as carboxypeptidase or nitroreductase and are useful for the treatment of cancer.
L'invention concerne des composés de formules (I) et (II), ainsi que leurs dérivés physiologiquement acceptables, formules dans lesquelles X et Y représentent indépendemment chlore, brome, iode, CH3SO3 à groupes mésyle ou OSO2 phényle à groupes tosyle (ou phényle est éventuellement substitué par 1, 2, 3, 4 ou 5 substituants indépendemment choisis parmi alkyle C1-4, halogène, cyano ou nitro; R<1> et R<2> représentent indépendemment 1 à 4 substituants facultatifs; Z<1> et Z<2> représentent chacun indépendemment -O- ou -NH-; R<3> représente hydrogène, <u>t</u>butyle ou allyle; Z<3> représente un groupe hydrocarbyle tel que carboxyéthyle, contenant éventuellement des hétéroatomes. Ces composés peuvent être transformés in situ en agents contenant des moutardes azotées par les interventions d'enzymes telles que la carboxy-peptidase ou la nitroréductase, et ils se révelent utiles dans le traitement du cancer.
Niculescu-Duvaz Ion
Springer Caroline Joy
Cancer Research Campaign Technology Limited
Mccarthy Tetrault Llp
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