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    142.
    发明专利
    未知

    公开(公告)号：ID28787A

    公开(公告)日：2001-07-05

    申请号：ID20011198

    申请日：1999-10-28

    Applicant: BASF AG

    Inventor： LUBISCH WILLFRIED ,  KOCK MICHAEL ,  HOGER THOMAS

    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.

    New heterocyclyl-benzimidazole carboxamide derivatives, useful for treating e.g. neurodegenerative diseases, epilepsy, ischemic damage, myocardial infarction, tumors, inflammation and diabetes
    149.
    发明专利
    New heterocyclyl-benzimidazole carboxamide derivatives, useful for treating e.g. neurodegenerative diseases, epilepsy, ischemic damage, myocardial infarction, tumors, inflammation and diabetes 未知

    公开(公告)号：DE19916460A1

    公开(公告)日：2000-10-19

    申请号：DE19916460

    申请日：1999-04-12

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOEGER THOMAS

    IPC: C07D235/30 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  A61K31/415 ,  C07D235/18

    Abstract: 2-Heterocyclyl-benzimidazolecarboxamide derivatives (Ia) and (Ib) and their tautomers, enantiomers, diastereoisomers, prodrugs and salts are new. 2-Heterocyclyl-benzimidazolecarboxamide derivatives of formula (Ia) and (Ib) and their tautomers, enantiomers, diastereoisomers, prodrugs and salts are new: R = H; 1-6C alkyl optionally monosubstituted by OR , oxo or NR R ; R = H or 1-4C alkyl; R , R = H or 1-4C alkyl optionally monosubstituted by R ; or NR R forms a 4-8 membered ring optionally monosubstituted by R ; R = as for R ; R = H; 1-6C alkyl; Cl; Br; F; NO2; CN; NR8aR9a; NHCOR ; or OR a; R a, R a = H or 1-4C alkyl; or NR aR9a forms a 4-8 membered ring optionally monosubstituted by 1-6C alkyl, 3-7C cycloalkyl-1-4C alkyl, COR , COOR or phenyl; R = H; 1-4C alkyl; or phenyl; R = as for R ; A = saturated or mono-unsaturated 4-8 membered heterocycle containing 1 or 2 N atoms and optionally 1 O or S atom and optionally substituted by R and R ; R = H; 1-8C alkyl optionally substituted by R and optionally monosubstituted by oxo; 3-7C cycloalkyl-1-4C alkyl; -CO-(NH)0-2-R ; COOR ; or phenyl; R = H or 1-6C alkyl, 3-7C cycloalkyl-1-4C alkyl, Ph-1-4C alkyl, 3-7C cycloalkyl or Ph optionally substituted by -(CH2)0-2-R ; Ph = phenyl optionally mono-, di- or trisubstituted by halo, 1-4C alkyl, NO2, CF3, CN, -(CH2)0-2-NR R , NHCOR , OR , COOR , SO2-1-4C alkyl, SO2-phenyl, SO2NH; NHSO2-1-4C alkyl, NHSO2-phenyl or CF3; R , R = H or 1-4C alkyl; or NR R forms a 4-8 membered ring optionally monosubstituted by 1-6C alkyl, COR , COOR or phenyl; R = H; 1-6C alkyl; 3-7C cycloalkyl-1-4C alkyl, phenyl-1-4C alkyl, 3-7C cycloalkyl or phenyl; R = NR R ; R , R = H; 1-6C alkyl; or 0-4C alkyl-Ph ; or NR R forms a 3-8 membered ring optionally containing a further hetero atom (e.g. O, N or S) and optionally monosubstituted by 1-4C alkyl or phenyl-1-4C alkyl; Ph = phenyl optionally mono-, di- or trisubstituted by halo, 1-4C alkyl, CF3, CN, SO2-1-4C alkyl, SO2-phenyl, NO2, NH2, NHCO-1-4C alkyl, NHCO-phenyl, OH, 1- 4C alkoxy or phenyl-1-4C alkoxy; R = H; 1-8C alkyl optionally monosubstituted by Ph ; or 3-7C cycloalkyl-1-4C alkyl or 3-7C cycloalkyl (both optionally substituted by 1-6C alkyl and optionally monosubstituted by Ph ); Ph = phenyl optionally mono-, di- or trisubstituted by Cl, F, Br, I, 1-4C alkyl, NO2, CF3, CN, (CH2)o-2-NR R , NHCOR , OR , COOR , SO2-1-4C alkyl, SO2Ph, CH3, SO2NH, NHSO2-1-4C alkyl, NHSO2-phenyl or CF3; R , R = H or 1-4C alkyl; or NR R forms a 4-8 membered ring optionally monosubstituted by 1-6C alkyl, 3-7C cycloalkyl-1-4C alkyl, COR , COOR or phenyl; R = as for R .

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