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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：EP1377574B1
公开(公告)日：2005-01-19
申请号：EP02722110.0
申请日：2002-02-21
发明人： FLOCKERZI, Dieter , Schmidt, Beate , GRUNDLER, Gerhard , HATZELMANN, Armin , BEUME, Rolf , BUNDSCHUH, Daniela , KLEY, Hans-Peter , NAVE, Rüdiger , ZECH, Karl , REUTTER, Felix
IPC分类号： C07D471/04 , A61K31/47 , A61P11/16
CPC分类号： C07D471/04 , A61K31/47 , Y02A50/409 , Y02A50/411
摘要： Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in the description, are novel effective PDE3/4 Inhibitors.
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4.发明授权FLUORALKOXY SUBSTITUIERTE BENZAMIDE UND IHRE VERWENDUNG ALS ZYKLISCH-NUKLEOTID PHOSPHODIESTERASE-INHIBITOREN 失效氟烷氧基取代的苯甲酰胺及其作为环核苷酸磷酸二酯酶抑制剂的用途
公开(公告)号：EP0706513B1
公开(公告)日：2002-05-15
申请号：EP94924713.4
申请日：1994-07-02
发明人： AMSCHLER, Hermann , FLOCKERZI, Dieter , GUTTERER, Beate , HATZELMANN, Armin , SCHUDT, Christian , BEUME, Rolf , KILIAN, Ulrich , WOLF, Horst, P., O.
IPC分类号： C07D213/75 , A61K31/44 , C07C235/56 , A61K31/165
CPC分类号： C07D213/75 , C07C235/56
摘要： Compounds of formula (I), in which one of the substituents R1 or R2 stands for hydrogen, 1-6C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, benzyloxy or totally or partially fluorine-substituted 1-4C-alkoxy, and the other stands for totally or partially fluorine-substituted 1-4C-alkoxy, and R3 stands for phenyl, pyridyl, R31, R32 and R33- substituted phenyl or R34, R35, R36 and R37- substituted pyridyl, in which R31 stands for hydroxy, halogen, cyano, carboxyl, trifluoromethyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonyloxy, amino, mono- or di-1-4C-alkylamino or 1-4C-alkylcarbonylamino; R32 stands for hydrogen, hydroxy, halogen, amino, trifluoromethyl, 1-4C-alkyl or 1-4C-alkoxy; R33 stands for hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy; R34 stands for hydroxy, halogen, cyano, carboxyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl or amino; R35 stands for hydrogen, halogen, amino or 1-4C-alkyl; R36 stands for hydrogen or halogen; and R37 stands for hydrogen or halogen. These compounds constitute new effective bronchotherapeutic drugs.
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公开(公告)号：EP1147087A1
公开(公告)日：2001-10-24
申请号：EP00901089.3
申请日：2000-01-12
发明人： FLOCKERZI, Dieter , AMSCHLER, Hermann DI , HATZELMANN, Armin , BUNDSCHUH, Daniela , BEUME, Rolf , BOSS, Hildegard , KLEY, Hans-Peter , GUTTERER, Beate
IPC分类号： C07D221/12 , A61K31/435 , A61P11/08
CPC分类号： C07D221/12
摘要： The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.
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6.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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公开(公告)号：EP1377574A1
公开(公告)日：2004-01-07
申请号：EP02722110.0
申请日：2002-02-21
发明人： FLOCKERZI, Dieter , GUTTERER, Beate , GRUNDLER, Gerhard , HATZELMANN, Armin , BEUME, Rolf , BUNDSCHUH, Daniela , KLEY, Hans-Peter , NAVE, Rüdiger , ZECH, Karl , REUTTER, Felix
IPC分类号： C07D471/04 , A61K31/47 , A61P11/16
CPC分类号： C07D471/04 , A61K31/47 , Y02A50/409 , Y02A50/411
摘要： Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in the description, are novel effective PDE3/4 Inhibitors.
摘要翻译： 其中R 1，R 2，R 3，R 4和R 5具有说明书中所示含义的式（I）化合物是新型有效的PDE3 / 4抑制剂。
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