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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.
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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。
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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
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.
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4.发明公开BENZAMIDE MIT TETRAHYDROFURANYLOXY-SUBSTITUENTEN ALS INHIBITOREN DER PHOSPHODIESTERASE 4 有权与四氢呋喃氧基取代基苯甲酰作为抑制剂磷酸二酯酶4
公开(公告)号：EP1086096A1
公开(公告)日：2001-03-28
申请号：EP99926441.9
申请日：1999-05-27
发明人： MARTIN, Thomas , ULRICH, Wolf-Rüdiger , AMSCHLER, Hermann , GUTTERER, Beate , FLOCKERZI, Dieter , HATZELMANN, Armin , BOSS, Hildegard , BEUME, Rolf , KILIAN, Ulrich , KLEY, Hans-Peter , BÄR, Thomas
IPC分类号： C07D405/12 , A61K31/44 , A61K31/34 , A61K31/35 , C07D493/10 , C07D307/20 , C07D309/10
CPC分类号： C07D405/12 , C07D493/10
摘要： Compounds of formula (I), wherein R1, R2, R3, R4, R5, m and n have the meanings cited in the description, are novel and effective PDE inhibitors.
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公开(公告)号：EP1075476A1
公开(公告)日：2001-02-14
申请号：EP99920814.3
申请日：1999-04-29
发明人： MARTIN, Thomas , ULRICH, Wolf-Rüdiger , AMSCHLER, Hermann , GUTTERER, Beate , FLOCKERZI, Dieter , HATZELMANN, Armin , BOSS, Hildegard , BEUME, Rolf , KILIAN, Ulrich , KLEY, Hans-Peter , BÄR, Thomas
IPC分类号： C07D413/00 , A61K31/42 , A61K31/415 , C07D405/04 , C07D413/04 , C07D413/14
CPC分类号： C07D405/04 , C07D413/04 , C07D413/14
摘要： The invention relates to compounds of formula (I) wherein R1, R2, R3, R4 and Y have the meanings given in the description. Said compounds are novel active bronchial therapeutic agents.
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公开(公告)号：EP0920426A1
公开(公告)日：1999-06-09
申请号：EP97940080.0
申请日：1997-08-13
发明人： AMSCHLER, Hermann , MARTIN, Thomas , FLOCKERZI, Dieter , GUTTERER, Beate , THIBAUT, Ulrich , HATZELMANN, Armin , BOSS, Hildegard , HÄFNER, Dietrich , KLEY, Hans-Peter , BEUME, Rolf , BÄR, Thomas , ULRICH, Wolf-Rüdiger
CPC分类号： C07D417/04 , C07D417/14
摘要： Compounds having the formula (I), in which R1, R2, R3, R4 and n have the meanings given in the description, are new effective bronchotherapeutic agents (phosphodiesterase IV inhibitors).
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公开(公告)号：EP0828728A1
公开(公告)日：1998-03-18
申请号：EP96916048.0
申请日：1996-05-11
发明人： AMSCHLER, Hermann , BÄR, Thomas , GUTTERER, Beate , FLOCKERZI, Dieter , MARTIN, Thomas , THIBAUT, Ulrich , HATZELMANN, Armin , BEUME, Rolf , BOSS, Hildegard , HÄFNER, Dietrich , KLEY, Hans-Peter , ULRICH, Wolf-Rüdiger
CPC分类号： C07D307/94 , C07D307/86
摘要： Compounds having the formula (I), in which R1, R2, R3, R4 and R5 have the meanings given in the description, are new and powerful PDE inhibitors.
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8.发明公开OPTISCH REINES R-(-)-NIGULDIPIN UND DESSEN DERIVATE ZUR BEHANDLUNG VON TUMORERKRANKUNGEN 失效光学纯DEXNIGULDIPIN及其衍生物对肿瘤疾病的治疗。
公开(公告)号：EP0401256A1
公开(公告)日：1990-12-12
申请号：EP89902511.0
申请日：1989-02-16
发明人： KLEMM, Kurt , ULRICH, Wolf-Rüdiger , FLOCKERZI, Dieter , SANDERS, Karl , BELLER, Klaus-Dieter , SCHUDT, Christian , BOER, Rainer , GIETZEN, Klaus Abt. Pharmakologie und Toxikologie
CPC分类号： A61K31/445
摘要： Des composés de diaryl optiquement purs de formule (I), où les substituants et symboles ont les notations indiquées dans la description, sont proposés à titre de principes actifs dans des médicaments pour traiter des affections tumorales.
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公开(公告)号：EP1368317A1
公开(公告)日：2003-12-10
申请号：EP02722097.9
申请日：2002-02-19
发明人： MARTIN, Thomas , BÄR, Thomas , STADLWIESER, Josef , ULRICH, Wolf-Rüdiger , DOMINIK, Andreas , BUNDSCHUH, Daniela , ZECH, Karl , SOMMERHOFF, Christian, P.
IPC分类号： C07D213/30 , A61K31/44 , A61P11/00
CPC分类号： C07D213/30
摘要： Compounds of the formula (I), in which M is a central building block selected from the group below in which A1, A2, K1 and K2 are as defined in the description, are novel effective tryptase inhibitors.
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公开(公告)号：EP1192184A1
公开(公告)日：2002-04-03
申请号：EP00935162.8
申请日：2000-06-02
IPC分类号： C07K14/785 , A61K38/17 , A61P11/00
CPC分类号： C07K14/785 , A61K38/00
摘要： Novel surfactant protein C esters suitable for preparing pharmaceutical compositions for the treatment of infant respiratory distress syndrome and adult respiratory distress syndrome are described.
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