公开(公告)号：EP1370298A1

公开(公告)日：2003-12-17

申请号：EP02727513.0

申请日：2002-03-25

申请人： Syntarga B.V.

发明人： DE GROOT, Franciscus, Marinus, Hendrikus ,  BEUSKER, Patrick, Henry ,  SCHEEREN, Johannes, Wilhelm ,  DE VOS, Dick ,  VAN BERKOM, Leonardus, Wilhelmus, Adriaan ,  BUSSCHER, Guuske, Frederike ,  SEELEN, Antoinette, Eugenie ,  KOEKKOEK, Ralph ,  ALBRECHT, Carsten

IPC分类号： A61K47/48

CPC分类号： B82Y5/00 ,  A61K47/65 ,  A61K47/67 ,  A61K47/6889 ,  A61K47/6899

摘要： 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-(W)k-(X)1-A-Z, wherein: V is a specifier; (W)k-(X)1-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)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclisation elimination spacer; Z is a therapeutic drug; k, 1 and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: - when A is (Y)m: k+1+m ≥ 1, and if k+1+m = 1; - when A is U: k+1 ≥ 1.

公开(公告)号：EP1370298B1

公开(公告)日：2008-10-08

申请号：EP02727513.0

申请日：2002-03-25

申请人： Syntarga B.V.

发明人： DE GROOT, Franciscus, Marinus, Hendrikus ,  BEUSKER, Patrick, Henry ,  SCHEEREN, Johannes, Wilhelm ,  DE VOS, Dick ,  VAN BERKOM, Leonardus, Wilhelmus, Adriaan ,  BUSSCHER, Guuske, Frederike ,  SEELEN, Antoinette, Eugenie ,  KOEKKOEK, Ralph ,  ALBRECHT, Carsten

IPC分类号： A61K47/48

CPC分类号： B82Y5/00 ,  A61K47/65 ,  A61K47/67 ,  A61K47/6889 ,  A61K47/6899

摘要： 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-(W)k-(X)1-A-Z, wherein: V is a specifier; (W)k-(X)1-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)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclisation elimination spacer; Z is a therapeutic drug; k, 1 and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: - when A is (Y)m: k+1+m ≥ 1, and if k+1+m = 1; - when A is U: k+1 ≥ 1.