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公开(公告)号：EP1169338A2
公开(公告)日：2002-01-09
申请号：EP00920597.2
申请日：2000-03-28
发明人： HILLEN, Heinz , SCHMIDT, Martin , MACK, Helmut , SEITZ, Werner , HAUPT, Andreas , ZECHEL, Johann-Christian , KLING, Andreas
IPC分类号： C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07D409/12 , A61K38/55 , A61P7/02 , C07K5/06
CPC分类号： C07D401/12 , A61K38/00 , C07B43/00 , C07K5/06078
摘要： The invention relates to peptidic substances, to the production of said substances and to their use as complement inhibitors. In particular, the invention relates to substances with a guanidine or amidine radical as the terminal group, especially inhibitors of the complement proteases C1s and C1r.
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2.发明授权DIPEPTIDISCHE P-AMIDINOBENZYLAMIDE MIT N-TERMINALEN SULFONYL- BZW. AMINOSULFONYLRESTEN 失效DIPEPTIDISCHE对氨基苯甲酰胺MIT N-TERMINALEN SULFONYL-BZW. AMINOSULFONYLRESTEN
公开(公告)号：EP0796271B1
公开(公告)日：2000-02-02
申请号：EP95941015.0
申请日：1995-11-25
发明人： BÖHM, Hans Joachim , KOSER, Stefan , MACK, Helmut , PFEIFFER, Thomas , SEITZ, Werner , HÖFFKEN, Hans Wolfgang , HORNBERGER, Wilfried , ZIERKE, Thomas
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/06026 , C07K5/06043 , C07K5/06078 , C07K5/06113
摘要： The invention pertains to compounds of formula (I), wherein R1, A and B are as indicated in the description, and to their preparation. The new compounds can be used for combatting diseases.
摘要翻译： 本发明涉及式（I）的化合物及其制备方法，其中R1，A和B如说明书中所示。 新化合物可用于对抗疾病。
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公开(公告)号：EP0956294A1
公开(公告)日：1999-11-17
申请号：EP97936672.0
申请日：1997-07-29
发明人： BAUCKE, Dorit , LANGE, Udo , MACK, Helmut , SEITZ, Werner , ZIERKE, Thomas , HÖFFKEN, Hans, Wolfgang , HORNBERGER, Wilfried
CPC分类号： C07K5/06078 , A61K38/00
摘要： Compounds having formula (I) wherein A, B, E and D have the m eanings indicated in the description, are described, in addition to the production thereof. The substances can be used to combat illnesses.
摘要翻译： 描述了式（I）的化合物，其中A，B，E和D具有在说明书中指出的含义。 这些物质可以用来对抗疾病。
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4.发明公开NEUE DIPEPTIDISCHE P-AMIDINOBENZYLAMIDE MIT N-TERMINALEN SULFONYL- BZW. AMINOSULFONYLRESTEN 失效NEUE DIPEPTIDISCHE P-AMIDINOBENZYLAMIDE MIT N-TERMINALEN SULFONYL-BZW. AMINOSULFONYLRESTEN
公开(公告)号：EP0796271A1
公开(公告)日：1997-09-24
申请号：EP95941015.0
申请日：1995-11-25
发明人： BÖHM, Hans Joachim , KOSER, Stefan , MACK, Helmut , PFEIFFER, Thomas , SEITZ, Werner , HÖFFKEN, Hans Wolfgang , HORNBERGER, Wilfried , ZIERKE, Thomas
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/06026 , C07K5/06043 , C07K5/06078 , C07K5/06113
摘要： The invention pertains to compounds of formula (I), wherein R1, A and B are as indicated in the description, and to their preparation. The new compounds can be used for combatting diseases.
摘要翻译： 本发明涉及式（I）的化合物及其制备方法，其中R1，A和B如说明书中所示。 新化合物可用于对抗疾病。
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公开(公告)号：EP1165601A2
公开(公告)日：2002-01-02
申请号：EP00920661.6
申请日：2000-04-05
发明人： BAUCKE, Dorit , MACK, Helmut , SEITZ, Werner , HORNBERGER, Wilfried , BACKFISCH, Gisela , DELZER, Jürgen
CPC分类号： C07K5/06078 , A61K38/00 , C07B43/00 , C07K5/0222
摘要： The invention relates to prodrugs of pharmacologically active, five-membered heterocyclic amidines from which in vivo compounds are obtained, these compounds being competitive inhibitors of trypsin-type serin proteases, especially thrombin and kininogenases such as kallikrein. The invention also relates to the production of these prodrugs and to their use as medicaments, to pharmaceutical compositions that contain the prodrugs of the active compounds as components, and to the use of the compounds as thrombin inhibitors, anticoagulants and anti-inflammatory agents.
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公开(公告)号：EP1049673A1
公开(公告)日：2000-11-08
申请号：EP99903676.7
申请日：1999-01-23
发明人： BAUCKE, Dorit , LANGE, Udo , MACK, Helmut , SEITZ, Werner , HÖFFKEN, Hans, Wolfgang , HORNBERGER, Wilfried
IPC分类号： C07D205/04 , C07K5/06
CPC分类号： C07D405/12 , C07D409/12 , C07D417/12 , C07K5/0222
摘要： The invention relates to compounds of the formula A-B-D-E-F, in which A, B, D, E and F have the meanings given in the description, and to their production. These new compounds are suitable for producing medicines.
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公开(公告)号：EP0773955A1
公开(公告)日：1997-05-21
申请号：EP95923231.0
申请日：1995-06-06
发明人： BÖHM, Hans-Joachim , KOSER, Stefan , MACK, Helmut , PFEIFFER, Thomas , SEITZ, Werner , HÖFFKEN, Hans, Wolfgang , HORNBERGER, Wilfried
CPC分类号： C07K5/0812 , A61K38/00 , A61K47/64 , C07D205/04 , C07D207/16 , C07D207/48 , C07D211/60 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06104 , C07K5/06113
摘要： Compounds having the formula (I) are disclosed, in which the substituents have the meanings given in the description, as well as their salts with physiologically acceptable acids and their stereoisomers, and intermediate products for producing the same. These compounds are useful for treating diseases.
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公开(公告)号：EP1202988A2
公开(公告)日：2002-05-08
申请号：EP00958347.7
申请日：2000-08-01
发明人： KLING, Andreas , GENESTE, Hervé , LANGE, Udo , LAUTERBACH, Arnulf , GRAEF, Claudia, Isabella , SUBKOWSKI, Thomas , HOLZENKAMP, Uta , MACK, Helmut , SADOWSKI, Jens , HORNBERGER, Wilfried , LAUX, Volker
IPC分类号： C07D401/12 , A61K31/55 , A61P43/00 , C07D401/14 , C07D213/73 , C07D403/12 , C07D491/04 , C07D409/14
CPC分类号： C07D401/06 , C07D223/20 , C07D243/38 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/12 , C07D409/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14
摘要： The invention relates to novel compounds of formula (I) which bind to integrin receptors, wherein G and L have the following meaning: L is a structural element of formula IL, wherein T represents a COOH group or a radical that can be hydrolyzed to obtain COOH and U- represents (XL)a-(CRL1RL2)b-, -CR¿L?1=CRL2-, ethylene or =CR¿L?1-, wherein a is 0 or 1; b is 0, 1 or 2; X¿L? represents CRL?3R¿L4, NRL5, oxygen or sulfur and G is a structural element of formula I¿G?, wherein the insertion of structural element G can occur in both orientations and XO represents nitrogen or CRG?1¿. The invention also relates to the production of said compounds and to their use as medicaments.
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公开(公告)号：EP1051431A1
公开(公告)日：2000-11-15
申请号：EP99908818.0
申请日：1999-01-23
发明人： BAUCKE, Dorit , LANGE, Udo , MACK, Helmut , SEITZ, Werner , HÖFFKEN, Hans, Wolfgang , HORNBERGER, Wilfried
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/06078
摘要： The invention relates to compounds of the formula A-B-D-E-F, in which A, B, D, E and F have the meanings given in the description, and to their production. These new compounds are suitable for producing medicines.
摘要翻译： 本发明涉及式A-B-D-E-F的化合物，其中A，B，D，E和F具有在说明书中给出的含义及其制备。 这些新化合物适用于生产药物。
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公开(公告)号：EP0915844A1
公开(公告)日：1999-05-19
申请号：EP97933675.0
申请日：1997-07-14
发明人： MACK, Helmut , PFEIFFER, Thomas , SEITZ, Werner , ZIERKE, Thomas , BALKENHOHL, Friedhelm , LANGE, Udo
CPC分类号： C07D207/22
摘要： A process is disclosed for preparing 3-pyrroline-2-carboxylic acid derivatives of formula (I), in which R1 stands for H, C¿1?-C6-alkyl, benzyl, benzyl substituted at the phenyl radical, allyloxycarbonyl, C1-C6-alkyloxycarbonyl, benzyloxycarbonyl, in which the benzyl radical can be substituted by OCH3 radicals, or for C1-C4-alkylcarbonyl; or R?1¿ stands for an amino acid radical which can be alkylated or acylated at the nitrogen and is linked by the C-terminal; and R2 stands for OH, C¿1?-C4-alkyloxy, benzyloxy or an N?3R4¿ group, in which R?3 and R4¿ represent independently from each other H, C¿1?-C4-alkyl, benzyl, phenyl or pyridyl, in which the aromatic compounds in R?3 and R4¿ can be substituted by up to three identical or different substituents selected from the group composed of methyl, methoxy, hydroxy, cyano or halogen. According to this process, the sulphonic acid radical is eliminated by means of a base from a compound having the formula (II), in which R?1 and R2¿ have the above meanings and R5 stands for C¿1?-C6-alkyl, benzyl, trifluoromethyl, naphthyl or phenyl optionally substituted by radicals from the group composed of methyl, nitro and halogen.
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