Cancer Research Campaign Technology Limited

Lawrence C Davies

Caroline Joy Springer

This invention pertains to nitrogen mustard compounds (Formula (II)) and prodrugs therefor (Formula (I)), methods for their preparation, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in therapy and treatment, for example, of cancer, wherein: Rand Rare independently &#x2014;Cl, &#x2014;Br, &#x2014;I, &#x2014;OSOCH, or &#x2014;OSOPh; R, R, R, and Rare independently &#x2014;H, a Calkyl group, or a Chaloalkyl group; Ris &#x2014;F, &#x2014;Cl, &#x2014;Br, &#x2014;I, &#x2014;OCHF, &#x2014;C&#x2261;CH, &#x2014;OCF, &#x2014;CH, &#x2014;CF, &#x2014;SF, &#x2014;SCF, or &#x2014;CFCF; Ris &#x2014;H or as defined for R, Ris &#x2014;H or &#x2014;F; Ris &#x2014;H, &#x2014;C(CH), or &#x2014;CH&#x2014;CH&#x2014;CH; Z is &#x2014;CH&#x2014;T&#x2014;W; T is &#x2014;CH&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;(S&#x2550;O)&#x2014;, or &#x2014;(SO)&#x2014;; W is one of: (1) &#x2014;COOH; (2)&#x2014;(C&#x2550;O)OR; (3) &#x2014;(C&#x2550;O)NRR; (4) &#x2014;SONHR, (5) SOOR; (6)&#x2014;PORR; (7) a tetrazol-5-yl group; (8) &#x2014;CONH&#x2014;SOR; and, (9)-M-Het.

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Surrey, United Kingdom

Lawrence C Davies