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公开(公告)号:HU0200312A2
公开(公告)日:2002-11-28
申请号:HU0200312
申请日:1999-10-28
Applicant: BASF AG
Inventor: HOERGER THOMAS , KOCK MICHAEL , LUBISCH WILFRIED
IPC: G01N33/53 , A61K31/00 , A61K31/4184 , A61K31/4427 , A61K31/454 , A61K31/496 , A61K31/55 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P25/08 , A61P25/10 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07C237/30 , C07D235/18 , C07D401/10 , C07D403/10 , C07D521/00 , C12Q1/48 , G01N33/00 , G01N33/15 , G01N33/573 , G01N33/577
Abstract: 2-Phenyl-benzimidazolecarboxamide derivatives (I) and (II) are new. 2-Phenyl-benzimidazolecarboxamide derivatives of formulae (I) and (II) and their tautomers, enantiomers, diastereomers, prodrugs and salts, are new: [Image] R 1>H or alkyl optionally substituted with OH, alkoxy, amino (optionally mono- or disubstituted) or optionally substituted piperidino, piperazino, pyrrolidino, hexahydroazepino, morpholino or 4,5-dihydropyridino; R 2>H, Cl, Br, I, F, CF 3, NO 2, NHCOR 2> 1>, NR 2> 2>R 2> 3>, OH, alkoxy, alkoxy-Ph, NH 2, or Ph; R 2> 1>, R 2> 2>alkyl; R 2> 3>H, alkyl, or optionally substituted phenyl; x : 0-2; R 3>D-(F 1>) p-(E) q-(F 2>) r-G, E-(D) u-(F 2>) s-(G) v or B; R 4>H, Cl, F, Br, I, alkyl, OH, NO 2, CF 3, CN, NR 4> 4>R 4> 2>, NHCOR 4> 3>, or alkoxy; R 4> 1>, R 4> 2>H or alkyl; R 4> 3>H, alkyl, alkyl-phenyl, or phenyl; D : O or S; E : phenyl, imidazole, pyrrole, thiophene, pyridine, pyrimidine, piperazine, pyrazine, furan, thiazole, isoxazole, pyrrolidine, piperidine or optionally substituted trihydroazepine ring; F 1>, F 2>1-8C chain optionally substituted with OH or alkoxy; p-v : 0 or 1, but p, q and r are not simultaneously 0; G : NR 5> 1>R 52>or optionally substituted pyrrolidinyl, piperidinyl, 1,2,5,6-tetrahydropyridyl, piperizinyl, azepinyl, morpholinyl or 1,4-diazepanyl; R 5> 1>alkyl or (CH 2) t-K; B : optionally substituted pyrrolidinyl, piperidinyl, 1,2,5,6-tetrahydropyridyl, piperizinyl, azepinyl, morpholinyl or 1,4-diazepanyl; t : 0-4; K : optionally substituted phenyl, NR 4> 1>R 4> 2>, phenyl-alkyl-NH, pyrrolidino, piperidino, 1,2,5,6-tetrahydropyridino, morpholino, trihydroazepino, or piperazino or homopiperazino (both optionally substituted with alkyl); R 5>H, alkyl, NR 7>R 9>, or optionally substituted pyrrolidinyl, piperidinyl, 1,2,5,6-tetrahydropyridyl, piperizinyl, azepinyl, morpholinyl or 1,4-diazepanyl; The full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are also included for the following: (i) aminobenzamide intermediates of formulae (III) and (IV) and their salts; (ii) preparation of compounds (III) and (IV); (iii) an in vitro method for the detection of poly(ADP-ribose)polymerase (PARP) inhibitors comprising: (a) incubating a poly-ADP-ribosylable target (optionally bonded to a carrier) with a reaction mixture comprising a PARP, a PARP activator and a PARP inhibitor or an analyte in which one or more PARP inhibitors is presumed to exist; (b) carrying out a poly-ADP-ribosylation reaction; and (c) qualitatively or quantitatively determining the poly-ADP-ribosylation with an anti-poly-(ADP-ribose) antibody. [Image] ACTIVITY : None given. MECHANISM OF ACTION : Poly(ADP-ribose)polymerase (PARP) inhibitor.
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公开(公告)号:HU0200859A2
公开(公告)日:2002-11-28
申请号:HU0200859
申请日:2000-04-11
Applicant: BASF AG
Inventor: GRANDEL ROLAND , HOERGER THOMAS , KOCK MICHAEL , LUBISCH WILFRIED , MUELLER REINHOLD , SCHULT SABINE
IPC: C07D235/08 , A61K31/4184 , A61K31/4427 , A61K31/4523 , A61K31/496 , A61K31/551 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/04 , A61P43/00 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/16 , C07D401/08 , C07D403/08 , C07D235/06
Abstract: Compounds of the formula I or IIand their tautomeric forms, possible enantiomeric and diastereomeric forms, possible cistrans isomers on the rings in A and prodrugs thereof, pharmaceutical compositions containing these compounds and methods of treating neurodegenerative diseases or neuronal damage with these compounds.
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