公开(公告)号：EP1060171A2

公开(公告)日：2000-12-20

申请号：EP99907497.4

申请日：1999-02-04

申请人： Max-Planck-Gesellschaft zur Förderungder Wissenschaften e.V. ,  Byk Gulden Lomberg Chemische Fabrik GmbH

发明人： BODE, Wolfram ,  MORODER, Luis ,  PEREIRA, Pedro Jose Barbosa ,  BERGNER, Andreas ,  HUBER, Robert ,  SOMMERHOFF, Christian ,  SCHASCHKE, Norbert ,  BÄR, Thomas ,  MARTIN, Thomas ,  STADLWIESER, Josef ,  ULRICH, Wolf-Rüdiger ,  DOMINIK, Andreas ,  THIBAUT, Ulrich ,  BUNDSCHUH, Daniela ,  BEUME, Rolf ,  GOEBEL, Karl-Josef

IPC分类号： C07D295/20 ,  A61K31/485 ,  C07D211/58 ,  A61K31/445 ,  C07D279/18 ,  A61K31/155 ,  C07C237/10 ,  A61K31/16 ,  C07D213/44 ,  C07D213/82

CPC分类号： C07D213/81 ,  C07C237/22 ,  C07C279/16 ,  C07D211/58 ,  C07D213/82 ,  C07D295/185 ,  C07D295/215 ,  C07D401/14

摘要： The invention relates to bifunctional inhibitors of human tryptase of formula (I), to human tryptase in crystalline form, to a method for producing human tryptase in crystalline form, to pharmaceutical compositions comprising a bifunctional inhibitor of human tryptase, and to a method for developing and identifying tryptase inhibitors. The tryptase inhibitors are characterized in that both head groups K1 and K2 are the same or different and each comprises a group Q which can interact with a carboxylate group. The linker L can assume a conformation such that the groups Q of both head groups are situated at a distance ranging from 20 to 45 Å, such that the dimension of the head groups and of the linker permit the inhibitor to penetrate into a cavity with the dimensions 52 Å X 32 Å X 40 Å, and such that L represents formula (II) wherein A1 and A2 are the same or different, and represent -C(O)-, NH-, -O- (oxygen), -S- (sulfur), -S(O)2-, -S(O)2-NH-, -NH-S(O)2-, -C(O)-NH-, -NH-C(O)-, -O-C(O)-, -C(O)-O- or a bond. A3 and A4 are the same or different and represent -C(O)-, -C(S)-, -O-, -S-, -NH-, -O-C(O)-, -C(O)-O-, -C(O)-NH-, -NH-C(O)- or a bond, or are selected from the group A5, A6, M, B1-B6 as stated in the description.

公开(公告)号：EP1060175A2

公开(公告)日：2000-12-20

申请号：EP99910192.6

申请日：1999-02-04

申请人： Max-Planck-Gesellschaft zur Förderungder Wissenschaften e.V. ,  Byk Gulden Lomberg Chemische Fabrik GmbH

发明人： BODE, Wolfram ,  MORODER, Luis ,  PEREIRA, Pedro, Jose, Barbosa ,  BERGNER, Andreas ,  HUBER, Robert ,  SOMMERHOFF, Christian ,  SCHASCHKE, Norbert ,  BÄR, Thomas ,  MARTIN, Thomas ,  STADLWIESER, Josef ,  ULRICH, Wolf-Rüdiger ,  DOMINIK, Andreas ,  THIBAUT, Ulrich ,  BUNDSCHUH, Daniela ,  BEUME, Rolf ,  GOEBEL, Karl-Josef

IPC分类号： C07D401/12 ,  C07D295/192 ,  A61K31/44

CPC分类号： C07D213/81 ,  C07C279/16 ,  C07D211/58 ,  C07D213/82 ,  C07D295/185 ,  C07D295/215 ,  C07D401/14

摘要： The invention relates to compounds of formula (I), wherein M, A1, A2, A3, A4, A5, A6, B1, B2, B3, B4, B5, B6, K1 and K2 have the meanings given in the description. Said compounds are novel effective inhibitors of human tryptase.

摘要翻译： 本发明涉及式（I）的化合物，其中M，A1，A2，A3，A4，A5，A6，B1，B2，B3，B4，B5，B6，K1和K2具有在说明书中给出的含义。 所述化合物是人类类胰蛋白酶的新型有效抑制剂。

公开(公告)号：EP1216236A1

公开(公告)日：2002-06-26

申请号：EP00962476.8

申请日：2000-09-12

申请人： Byk Gulden Lomberg Chemische Fabrik GmbH

发明人： BÄR, Thomas ,  STADLWIESER, Josef ,  ULRICH, Wolf-Rüdiger ,  DOMINIK, Andreas ,  BUNDSCHUH, Daniela ,  ZECH, Karl ,  SOMMERHOFF, Christian ,  MARTIN, Thomas

IPC分类号： C07D295/205 ,  C07D295/215 ,  C07C271/20 ,  C07C235/10 ,  C07C237/20 ,  C07D307/42 ,  C07D333/16 ,  A61K31/495 ,  A61K31/16 ,  A61K31/381 ,  A61K31/341 ,  A61P11/00

CPC分类号： C07D295/205 ,  C07D295/215

摘要： Compounds of formula (I), in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description are novel effective tryptase inhibitors.

公开(公告)号：EP1115731A2

公开(公告)日：2001-07-18

申请号：EP99942928.5

申请日：1999-08-27

申请人： Byk Gulden Lomberg Chemische Fabrik GmbH

发明人： STADLWIESER, Josef ,  ULRICH, Wolf-Rüdiger ,  DOMINIK, Andreas ,  BUNDSCHUH, Daniela ,  ELTZE, Manfrid ,  ZECH, Karl ,  SOMMERHOFF, Christian ,  MARTIN, Thomas ,  BÄR, Thomas

IPC分类号： C07H1/00

CPC分类号： C07H13/12 ,  C07H15/203

摘要： The invention relates to compounds of formula (I), wherein M, A1, A2, A3, A4, A5, A6, B1, B2, B3, B4, B5, B6, K1 and K2 have the meanings given in the description. Said compounds are novel, effective tryptase inhibitors.

公开(公告)号：EP1208089A2

公开(公告)日：2002-05-29

申请号：EP00960418.2

申请日：2000-08-09

申请人： Byk Gulden Lomberg Chemische Fabrik GmbH

发明人： BAER, Thomas ,  MARTIN, Thomas ,  STADLWIESER, Josef ,  DOMINIK, Andreas ,  BUNDSCHUH, Daniela ,  ZECH, Karl ,  SOMMERHOFF, Christian ,  ULRICH, Wolf-Rüdiger

IPC分类号： C07D245/02

CPC分类号： A61K31/395 ,  C07D245/02

摘要： Compounds of formula (I) in which M is the following central building block (a) are novel effective trypase-inhibitors.