Syntarga Bv

Ralph Koekkoek

Patrick Henry Beusker

Dick De Vos

Franciscus Marinus Hendrikus De Groot

Johannes Wilhelm Scheeren

Carsten Albrecht

Leonardus Wilhelmus Adriaan Van Berkom

Guuske Frederike Busscher

Antoinette Eugenie Seelen

Franciscus Marinus De Groot

Leonardus Wilhelmus Van Berkom

This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V&#x2014;(W)&#x2014;(X)&#x2014;A&#x2014;Z, wherein: V is a specifier; (W)&#x2014;(X)&#x2014;A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclization elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: &#x2014;when A is (Y): k+l+m&#x2267;1, and if k+l+m=1; &#x2014;when A is U: k+l&#x2267;1.

Elongated and multiple spacers in activatible prodrugs

Growing community of inventors

Beuningen, Netherlands

Ralph Koekkoek