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公开(公告)号：CA2328435A1
公开(公告)日：1999-10-28
申请号：CA2328435
申请日：1999-04-19
Applicant: BASF AG
Inventor： TREIBER HANS-JORG , KNOPP MONIKA , MOLLER ACHIM , LUBISCH WILFRIED
IPC: A61K31/196 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/47 , A61K31/517 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P43/00 , C07C233/76 , C07C237/22 , C07C311/21 , C07D213/56 , C07D215/36 , C07D239/70 , C07D239/96 , A61K31/19 , A61K31/195 , A61K31/44 , A61K31/505 , C07C237/52 , C07C235/82
Abstract: The invention relates to amides of general formula (I) and their tautomeric and isomeric forms, their possible enantiomeric and diastereomeric forms and possible physiologically compatible salts, where the variables have the following meanings: R1 is C1-C6 alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, whereby the rings can still be substituted with up to 2 R4 rests; R2 is -(CH2)m-R8, where R8 is phenyl, cyclohexyl or indolyl and m is 1 to 6; X is a bond, -CH2-, -CH2CH2-, -CH=CH-, CC-, -CONH-, -, -SO2NH-, and R1-X together can also be formula (a), R3 is hydrogen and CO-NR6R7; R4 is hydrogen, branched or unbranched C1-C4 alkyl and O-C1-C4-alkyl; R5 is hydrogen, branched or unbranched C1-C4 alkyl and O-C1-C4-alkyl; R6 is hydrogen, branched or unbranched C1-C6 alkyl; R7 is hydrogen, branched or unbranched C1-C6 alkyl; and n is 0, 1 or 2. The amides of formula (I) are inhibitors of enzymes, especially cysteine proteases such as calpains (calcium dependent cysteine proteases) and their isoenzymes and cathepsins, such as B and L.
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公开(公告)号：CA2328430A1
公开(公告)日：1999-10-28
申请号：CA2328430
申请日：1999-04-19
Applicant: BASF AG
Inventor： TREIBER HANS-JORG , KNOPP MONIKA , MOLLER ACHIM , LUBISCH WILFRIED
IPC: C07D295/08 , A61K31/18 , A61K31/27 , A61K31/4409 , A61K31/4418 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C233/78 , C07C235/42 , C07C237/34 , C07C311/21 , C07D213/56 , C07D295/096 , A61K31/44
Abstract: The invention relates to benzamides of general formula (I) and their tautomeric forms, as well as to possible enantiomeric and diastereomeric forms, to their E and Z forms and to possible physiologically compatible salts, where the variables R1, R2, R3, A and B have the meanings given in claim 1. The invention also relates to their use as inhibitors of cysteine proteases.
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公开(公告)号：CA2328396A1
公开(公告)日：1999-10-28
申请号：CA2328396
申请日：1999-04-20
Applicant: BASF AG
Inventor： LUBISCH WILFRIED , TREIBER HANS-JORG , MOLLER ACHIM , KNOPP MONIKA
IPC: C07D295/08 , A61K31/16 , A61K31/166 , A61K31/27 , A61K31/395 , A61K31/40 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C229/38 , C07C237/20 , C07C237/22 , C07C237/32 , C07C237/36 , C07D209/14 , C07D213/82 , C07D233/64 , C07D237/32 , C07D237/36 , C07D295/14 , C07D295/155
Abstract: The invention relates to cysteine protease inhibitors of the general formula (I), in which A is -(CH2)p-R1, where R1 can be pyrrolidine, morpholine, piperidine, -NR5R6 and formula (a) and p can be 1 or 2; B can be possibly substituted phenyl, pyridyl, pyrimidyl and pyridazyl; D is a bond, -(CH2)m-, - CH=CH-, -CC-; R2 is chlorine, bromine, fluorine, alkyl, NHCO alkyl, NHSO2 alkyl, NO2, -O-alkyl and NH2; R3 is an alkyl which can carry a possibly substituted phenyl ring, indolyl ring and cyclohexyl ring; and Y is phenyl, pyridine, pyrimidine and pyrazine; R4 is hydrogen, COOR9 and CO-Z, where Z i s NR10R11 and and formulae (b), (c), (d); n is 0, 1 or 2 and m is 0, 1, 2, 3 o r 4.
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公开(公告)号：TR9901282T2
公开(公告)日：1999-10-21
申请号：TR9901282
申请日：1997-11-28
Applicant: BASF AG
Inventor： LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS-JORG
IPC: A61K31/403 , A61K31/4035 , A61K31/405 , A61K31/4439 , A61K31/496 , A61K31/517 , A61K31/519 , A61K31/5377 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07D209/48 , C07D209/66 , C07D239/70 , C07D239/96 , C07D401/12 , C07D471/04 , C07D475/02 , A61K31/40 , A61K31/505
CPC classification number: C07D471/04 , C07D209/66 , C07D239/70 , C07D239/96 , C07D475/02
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公开(公告)号：ID22490A
公开(公告)日：1999-10-21
申请号：ID990486
申请日：1997-11-28
Applicant: BASF AG
Inventor： LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS JORG
IPC: A61K31/403 , A61K31/4035 , A61K31/405 , A61K31/4439 , A61K31/496 , A61K31/517 , A61K31/519 , A61K31/5377 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07D209/48 , C07D209/66 , C07D239/70 , C07D239/96 , C07D401/12 , C07D471/04 , C07D475/02 , A61K31/505 , A61K31/40
Abstract: Heterocyclically substituted benzamides of the formula Iare described, where R1, R2, R3, R4, R5, X, m and n have the meanings given in the description. The novel compounds are useful for controlling diseases.
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Patent Agency Ranking
公开(公告)号：AU5481498A
公开(公告)日：1998-06-22
申请号：AU5481498
申请日：1997-11-11
Applicant: BASF AG
Inventor： LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS-JORG
IPC: A61K31/16 , A61K31/166 , A61K31/18 , A61K31/4045 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61P9/10 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P27/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C233/76 , C07C235/42 , C07C235/46 , C07C235/58 , C07C235/60 , C07C235/84 , C07C237/42 , C07C311/08 , C07C311/21 , C07C317/44 , C07C323/42 , C07C323/60 , C07D209/14 , C07D209/16 , C07D213/30 , C07D213/56 , C07D213/71 , C07D213/82 , C07D215/36 , C07D215/14
Abstract: Compounds of the formulawhere R1, R2, R3, X and n are as defined in the description, are inhibitors of cysteine protease.
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公开(公告)号：CA2274464C
公开(公告)日：2007-01-02
申请号：CA2274464
申请日：1997-11-28
Applicant: BASF AG
Inventor： TREIBER HANS-JORG , LUBISCH WILFRIED , MOLLER ACHIM
IPC: C07C233/87 , C07D295/12 , A61K31/16 , A61K31/166 , A61K31/381 , A61K31/40 , A61K31/4164 , A61K31/4402 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4468 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/28 , A61P35/00 , A61P43/00 , C07C237/22 , C07C237/36 , C07C237/42 , C07C311/19 , C07C311/21 , C07D211/58 , C07D213/56 , C07D215/12 , C07D215/36 , C07D215/48 , C07D233/54 , C07D233/61 , C07D241/42 , C07D241/44 , C07D295/02 , C07D295/13 , C07D333/38 , C07D333/56 , C07D333/60 , C07D401/12 , C07D521/00 , C07K5/02
Abstract: The invention concerns ketobenzamides of formula (I) in which R1, R2, R3, R4, X and n have the meanings given in the description. The invention further concerns their preparation. The novel compounds are suitable for combating diseases.
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公开(公告)号：PL353004A1
公开(公告)日：2003-09-22
申请号：PL35300400
申请日：2000-06-07
Applicant: BASF AG
Inventor： DEAR NEIL T , BOHM THOMAS , MOLLER ACHIM
IPC: G01N33/50 , A61K38/57 , A61K45/00 , A61P15/00 , A61P15/08 , C12N9/64 , C12N15/09 , C12Q1/37 , G01N33/15 , C12N15/57
Abstract: The invention relates to a novel mammalian calpain CAPN11, to the synthesis and to the use thereof.
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公开(公告)号：CZ292391B6
公开(公告)日：2003-09-17
申请号：CZ174399
申请日：1997-11-28
Applicant: BASF AG
Inventor： LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS-JORG
IPC: A61K31/403 , A61K31/4035 , A61K31/405 , A61K31/4439 , A61K31/496 , A61K31/517 , A61K31/519 , A61K31/5377 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07D209/48 , C07D209/66 , C07D239/70 , C07D239/96 , C07D401/12 , C07D471/04 , C07D475/02 , A61K31/505 , A61K31/40
Abstract: In the present invention there is disclosed a benzamide derivative substituted with heterocyclic groups of the general formula I, in which X represents a group -NH-CO-, -N=CH-, -CHi2-CHi2-, -CH=CH-, -SOi2-, -CHi2-, -CO- or -CHi2-CO-, tautomeric and isomeric forms thereof and optionally its physiologically acceptable salts. These compounds are inhibitors of cysteine proteases and are thus suitable for treating states in which increased activity of calpain occurs and in which interleukin-1 increased level takes place, in particular for treating neurodegenerative diseases and neuronal damage, but also epilepsy and tumors as well as metastases thereof.
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公开(公告)号：SK18262001A3
公开(公告)日：2002-09-10
申请号：SK18262001
申请日：2000-06-07
Applicant: BASF AG
Inventor： DEAR NEIL T , BOHM THOMAS , MOLLER ACHIM
IPC: G01N33/50 , A61K38/57 , A61K45/00 , A61P15/00 , A61P15/08 , C12N9/64 , C12N15/09 , C12Q1/37 , G01N33/15 , C12N9/00
Abstract: The invention relates to a novel mammalian calpain CAPN11, to the synthesis and to the use thereof.
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