公开(公告)号：EP0724576A1

公开(公告)日：1996-08-07

申请号：EP94929152.0

申请日：1994-09-15

申请人： CYTOGEN CORPORATION

发明人： BELINKA, Benjamin, A., Jr. ,  COUGHLIN, Daniel, J.

IPC分类号： C07D255 ,  C07F9

CPC分类号： C07F9/6524 ,  C07F9/025 ,  C07F9/3817

摘要： A process for the purification of aminophosphonic acids under non-alkaline conditions is described. In particular, aminophosphonic acids are slurred in neutral or acidic water, heated to reflux, cooled and then filtered. Product purities approaching 100 % are thus obtained.

公开(公告)号：EP0724576B1

公开(公告)日：2002-03-20

申请号：EP94929152.0

申请日：1994-09-15

申请人： CYTOGEN CORPORATION

发明人： BELINKA, Benjamin, A., Jr. ,  COUGHLIN, Daniel, J.

IPC分类号： C07F9/38 ,  C07F9/6524

CPC分类号： C07F9/6524 ,  C07F9/025 ,  C07F9/3817

摘要： A process for the purification of aminophosphonic acids under non-alkaline conditions is described. In particular, aminophosphonic acids are slurred in neutral or acidic water, heated to reflux, cooled and then filtered. Product purities approaching 100 % are thus obtained.

公开(公告)号：EP0635001A1

公开(公告)日：1995-01-25

申请号：EP93911594.0

申请日：1993-04-08

申请人： CYTOGEN CORPORATION

发明人： COUGHLIN, Daniel, J. ,  BELINKA, Benjamin, A., Jr.

IPC分类号： G01N33 ,  A61K39 ,  A61K47 ,  A61K51 ,  C07C335 ,  C07C337 ,  C07D207 ,  C07D213 ,  C09K3

CPC分类号： C07D207/452 ,  A61K47/50 ,  A61K51/082 ,  A61K51/088 ,  A61K51/1093 ,  A61K2121/00 ,  A61K2123/00 ,  C07C335/22 ,  C07C337/06 ,  C07D213/71

公开(公告)号：EP0635001B1

公开(公告)日：1997-08-20

申请号：EP93911594.5

申请日：1993-04-08

申请人： CYTOGEN CORPORATION

发明人： COUGHLIN, Daniel, J. ,  BELINKA, Benjamin, A., Jr.

IPC分类号： C07C337/06 ,  C07C335/22 ,  C07D207/44 ,  C07D213/71

CPC分类号： C07D207/452 ,  A61K47/50 ,  A61K51/082 ,  A61K51/088 ,  A61K51/1093 ,  A61K2121/00 ,  A61K2123/00 ,  C07C335/22 ,  C07C337/06 ,  C07D213/71

摘要： This invention relates to chelating agents of formula (I), in which L is a linker; D is an alkyl backbone, cyclic alkyl backbone or aryl backbone group substituted with the NHCSNHR groups: and R is hydrogen or a substituent of general formula (1) in which a = 0 or 1; b = 0-10; c = 0 or 1; if c = 1, Y = S, O or H2; d = 0-2; e = 0-10; and Z = H, N+(R')3X-, SO3H, CO2H, OH, H2PO3; in which X- is a counterion such as a halide or an acid anion and R' is a C¿1? to C4 lower alkyl, useful for coupling metal ions to biologically active molecules. In particular, substantial thioureas for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.