公开(公告)号：EP1027351A1

公开(公告)日：2000-08-16

申请号：EP98967153.2

申请日：1998-10-26

申请人： FIBROGEN, INC. ,  ZENECA LIMITED

发明人： EDWARDS, Philip Neil ,  LARGE, Michael Stewart ,  HALES, Neil, James ,  MARTIN, George, R. ,  HUANG, Xinfan

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  A61K31/4745

摘要： The present invention provides a phenanthroline derivative of formula (I) wherein, for example, R1 is hydrogen, carboxy, cyano, nitro, (1-4C)alkyl, (1-6C)alkoxycarbonyl, (1-4C)alkylamino, (2-4C)alkanoyl, (1-4C)alkoxy-(2-4C)alkoxy-(2-4C)alkoxycarbonyl or N-[amino-(2-8C)alkyl]carbamoyl; R2 is, for example, hydrogen, carboxy, (1-6C)alkoxycarbonyl, carbamoyl, N-(1-8C)alkylcarbamoyl, N,N-di-(1-8C)alkylcarbamoyl, N-(1-4C)alkylcyclohexylcarbamoyl, 1,2,3,4,-tetrahydro-isoquinolin-2-ylcarbonyl or N,N-[di-(1-4C)alkyl]thiocarbamoyl; R?3 and R4¿, which may be the same or different, are, for example, hydrogen or halo; and R5 is, for example, hydrogen, di-(1-4C)alkylamino or halo; or a pharmaceutically-acceptable salt thereof. The invention further provides pharmaceutical compositions comprising phenanthroline derivatives, processes for making the same and their use in producing an anti-fibroproliferative effect.

公开(公告)号：EP1027351B1

公开(公告)日：2003-12-03

申请号：EP98967153.2

申请日：1998-10-26

申请人： FibroGen, Inc. ,  Syngenta Limited

发明人： EDWARDS, Philip Neil ,  LARGE, Michael Stewart ,  HALES, Neil, James ,  MARTIN, George, R. ,  HUANG, Xinfan

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  A61K31/4745

公开(公告)号：EP0820591A1

公开(公告)日：1998-01-28

申请号：EP96908266.0

申请日：1996-04-01

申请人： ZENECA LIMITED

发明人： HALES, Neil, James ,  CLAYTON, Edward

IPC分类号： G01N33 ,  B01J20 ,  G01N30

CPC分类号： G01N33/68 ,  G01N33/538

摘要： An assay method for determining the affinity of low molecular weight ligands for a biological of interest under physiologically relevant conditions, which method comprises immobilising the biological of interest on a solid phase matrix, contacting this with a mixture comprising the ligands, removing any unbound ligands from the matrix, eluting the ligands from the matrix and establishing their affinity for the biological of interest by reference to their order of retention on the column.

公开(公告)号：EP0907653A1

公开(公告)日：1999-04-14

申请号：EP97928361.0

申请日：1997-06-24

申请人： ZENECA LIMITED

发明人： GALLAGHER, Timothy, Charles ,  HALES, Neil, James ,  WISEDALE, Richard ,  PLANCHENAULT, Denis

IPC分类号： C07D499 ,  A61K31 ,  C07D263

CPC分类号： C07D499/88 ,  C07D499/00 ,  Y02P20/55

摘要： The invention provides a process for the preparation of compounds of formula (I) wherein R?1, R2, R3, R4 and R5¿ are as defined in the specification; and wherein any functional groups are optionally protected; and salts thereof; which process includes the step of reacting the intermediate formed by heating a compound of formula (II), in an inert solvent, with a compound of the formula S=C(R3)R4 wherein R?1, R2, R3, R4 and R5¿ are as defined in the specification and functional groups are optionally protected; and thereinafter, if necessary, removing any protecting groups. The compounds of the formula (I) are useful as intermediates in the preparation of penems and may possess antibacterial properties and/or inhibit β-lactamase in their own right.