公开(公告)号：EP1019371B1

公开(公告)日：2003-05-02

申请号：EP96938012.0

申请日：1996-09-11

申请人： Forschungszentrum Jülich GmbH ,  Forschungsverbund Berlin e.V.

发明人： BAUER, Paul, J. ,  HAGEN, Volker

IPC分类号： C07D207/44 ,  C08J3/24

CPC分类号： C07D207/452 ,  C08F8/30

摘要： The invention concerns novel dimaleinimido-substituted dihydroxyalkanes, a process for their preparation and their use as crosslinking reagents. The disadvantage with the cleavable bismaleinimido derivatives used hitherto which react with SH groups is that the subsequent cleavage of the crosslinking reagents from the proteins has to be carried out in acid or alkaline media. The object of the invention is to prepare novel cleavable crosslinking reagents which react with SH groups and do not require subsequent cleavage of the crosslinking reagents from the proteins in acid or alkaline media. This object is achieved by dimaleinimido-substituted dihydroxyalkanes of the general formula given in figure 3.

公开(公告)号：EP1019371A2

公开(公告)日：2000-07-19

申请号：EP96938012.0

申请日：1996-09-11

申请人： FORSCHUNGSZENTRUM JÜLICH GMBH ,  Forschungsverbund Berlin e.V.

发明人： BAUER, Paul, J. ,  HAGEN, Volker

IPC分类号： C07D207/44 ,  C08J3/24

CPC分类号： C07D207/452 ,  C08F8/30

摘要： The invention concerns novel dimaleinimido-substituted dihydroxyalkanes, a process for their preparation and their use as crosslinking reagents. The disadvantage with the cleavable bismaleinimido derivatives used hitherto which react with SH groups is that the subsequent cleavage of the crosslinking reagents from the proteins has to be carried out in acid or alkaline media. The object of the invention is to prepare novel cleavable crosslinking reagents which react with SH groups and do not require subsequent cleavage of the crosslinking reagents from the proteins in acid or alkaline media. This object is achieved by dimaleinimido-substituted dihydroxyalkanes of the general formula given in figure 3.

公开(公告)号：EP1276749B1

公开(公告)日：2005-08-24

申请号：EP01929464.4

申请日：2001-03-26

申请人： Forschungsverbund Berlin e.V. ,  FORSCHUNGSZENTRUM JÜLICH GMBH

发明人： HAGEN, Volker ,  KAUPP, Ulrich, Benjamin ,  BENDIG, Jürgen ,  WIESNER, Burghard

IPC分类号： C07H19/20 ,  A61K31/7076 ,  A61K31/708

CPC分类号： C07H19/20

摘要： The invention relates to novel, photo-labile cumarinylmethyl esters of cyclic nucleotides of general formula (I): axial isomer (Ia), equatorial isomer (Ib); wherein R represents hydrogen, bromine or p-chlorophenylthio, R represents 7-carboxymethoxy, 6,7-, 5,7- or 7,8- bis(car-boxymethoxy), 7-C1-C3-alkoxycarbonylmethoxy, 6,7-bis(C1-C3-alkoxycarbonylmethoxy), 5,7-bis(C1-C3-alkoxycarbonylmethoxy) or 7,8-bis(C1-C3-alkoxy-carbonylmethoxy), R represents -NH2 and R is hydrogen (adenine radical) or R denotes -OH and R denotes -NH2 (guanine radical). The inventive compounds are biologically inactive and have a high solvolysis resistance, exhibiting high solubility in aqueous buffer solutions, high photocleavage and quick release kinetics.

公开(公告)号：EP0853628B1

公开(公告)日：2002-10-02

申请号：EP96927617.9

申请日：1996-07-29

申请人： Forschungsverbund Berlin e.V. ,  Forschungszentrum Jülich GmbH

发明人： HAGEN, Volker ,  KAUPP, Ulrich, Benjamin

IPC分类号： C07H19/20

CPC分类号： A61K41/0042 ,  C07H19/20

摘要： The invention concerns photolabile 8-substituted guanosine-3',5'-cyclomonophosphate esters and 8-substituted adenosine-3',5'-cyclomonophosphate esters of formula (I) and methods of preparing these compounds by reacting the appropriate 8-substituted cyclic nucleotides with substituted diazoalkanes or substituted bromoalkanes or by substitution reactions at the 8-position of the appropriate 8-bromoguanosine-3',5'-cyclomonophosphate esters or 8-bromoadenosine-3',5'-cyclomonophosphate esters. The invention also concerns the use of such compounds. The compounds are suitable for use in the investigation of processes dependent on cyclic nucleotides. Fields of application are biological, biochemical, biophysical, physiological and medical research (formula (I)).

公开(公告)号：EP0853628A1

公开(公告)日：1998-07-22

申请号：EP96927617.0

申请日：1996-07-29

申请人： Forschungsverbund Berlin e.V. ,  FORSCHUNGSZENTRUM JÜLICH GMBH

发明人： HAGEN, Volker ,  KAUPP, Ulrich, Benjamin

IPC分类号： A61K31 ,  A61K41 ,  A61P43 ,  C07H19

CPC分类号： A61K41/0042 ,  C07H19/20

摘要： The invention concerns photolabile 8-substituted guanosine-3',5'-cyclomonophosphate esters and 8-substituted adenosine-3',5'-cyclomonophosphate esters of formula (I) and methods of preparing these compounds by reacting the appropriate 8-substituted cyclic nucleotides with substituted diazoalkanes or substituted bromoalkanes or by substitution reactions at the 8-position of the appropriate 8-bromoguanosine-3',5'-cyclomonophosphate esters or 8-bromoadenosine-3',5'-cyclomonophosphate esters. The invention also concerns the use of such compounds. The compounds are suitable for use in the investigation of processes dependent on cyclic nucleotides. Fields of application are biological, biochemical, biophysical, physiological and medical research (formula (I)).

公开(公告)号：EP1276749A1

公开(公告)日：2003-01-22

申请号：EP01929464.4

申请日：2001-03-26

申请人： Forschungsverbund Berlin e.V. ,  Forschungszentrum Jülich GmbH

发明人： HAGEN, Volker ,  KAUPP, Ulrich, Benjamin ,  BENDIG, Jürgen ,  WIESNER, Burghard

IPC分类号： C07H19/20 ,  A61K31/7076 ,  A61K31/708

CPC分类号： C07H19/20

摘要： The invention relates to novel, photo-labile cumarinylmethyl esters of cyclic nucleotides of general formula (I): axial isomer (Ia), equatorial isomer (Ib); wherein R1 represents hydrogen, bromine or p-chlorophenylthio, R4 represents 7-carboxymethoxy, 6,7-, 5,7- or 7,8- bis(car-boxymethoxy), 7-C¿1?-C3-alkoxycarbonylmethoxy, 6,7-bis(C1-C3-alkoxycarbonylmethoxy), 5,7-bis(C1-C3-alkoxycarbonylmethoxy) or 7,8-bis(C1-C3-alkoxy-carbonylmethoxy), R?2¿ represents -NH¿2? and R?3¿ is hydrogen (adenine radical) or R2 denotes -OH and R3 denotes -NH¿2? (guanine radical). The inventive compounds are biologically inactive and have a high solvolysis resistance, exhibiting high solubility in aqueous buffer solutions, high photocleavage and quick release kinetics.