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    Novel heterocyclically substituted amides, process of their preparation and use
    42.
    发明专利
    Novel heterocyclically substituted amides, process of their preparation and use 未知

    公开(公告)号：CZ20004381A3

    公开(公告)日：2001-09-12

    申请号：CZ20004381

    申请日：1999-05-25

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  MOLLER ACHIM ,  TREIBER HANS-JORG ,  KNOPP MONIKA

    IPC: C07D215/08 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61P9/08 ,  A61P9/10 ,  A61P13/12 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/28 ,  A61P27/12 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D209/14 ,  C07D209/44 ,  C07D215/06 ,  C07D217/06 ,  C07D217/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D217/04 ,  A61K31/40 ,  A61K31/44 ,  A61K31/495

    Abstract: Fused heterocyclic-substituted (hetero)aromatic carboxylic acid alkylamides (I) are new. Amides of formula (I) and their tautomers, enantiomers, diastereomers, E- and Z-isomers and salts are new. [Image] A : fused cyclic group such as 1,2,3,4-tetrahydroquinolin-1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, isoindolin-2-yl or indolin-1-yl, all substituted by (R 4) n in the benzene ring; B' : phenyl, naphthyl, pyridyl, pyrimidyl, pyrazyl, pyridazyl, quinolyl, quinazyl, quinoxalyl, thienyl, benzothienyl, benzofuranyl, furanyl or indolyl; R 1H, alkyl, alkoxy, alkenyl, alkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, OH, halo, CF 3, NO 2, NH 2, CN, COOH, COOT, NHC(O)T, NHC(O)Ph, C(O)NHR 11, NHSO 2T, NHSO 2Ph, SO 2T or SO 2Ph; T : 1-4C alkyl; R 2alkyl (optionally substituted by phenyl, cyclohexyl, pyridyl, thienyl, indolyl or naphthyl, themselves all optionally substituted by 1 or 2 R 1 groups); R 3H, COOR 5 or C(O)Z; Z : NR 6R 7, 4-(R 15)-piperazino, R 15-substituted pyrrolidino or R 15-substituted piperidino; R 4H, (CH 2) mNR 8R 9, (CH 2) mQ or O(CH 2) mQ'; Q : 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 15-substituted pyrrolidino, R 15-substituted piperidino, morpholino, 4-(R 8)-1-piperidinyl or R 8-substituted hexamethyleneimino; Q' : 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 8-substituted pyrrolidino, R 15-substituted piperidino, morpholino or 4-(R 8)-1-piperidinyl; R 5, R 8, R 9alkyl (optionally substituted by phenyl, itself optionally substituted by 1 or 2 R 10); R 6H or alkyl; R 7H or alkyl (optionally substituted by phenyl or pyridyl (both optionally substituted by R 10) or by 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 15-substituted pyrrolidino, R 15-substituted piperidino, R 8-substituted 1-imidazolyl, morpholino, 4-(R 8)-1-piperidinyl or -(CH 2) oNR 8R 9); R 10H, T, OT, OH, halo, CF 3, NO 2, NH 2, CN, CONH 2, COOH, COOT, NHC(O)T, NHC(O)Ph, NHSO 2T, NHSO 2Ph, SO 2T or SO 2Ph; R 11H or alkyl; R 15H or as R 8; m : 1-6; n : 0-2; o : 0-4; unless specified otherwise alkyl moieties have 1-6C and alkenyl or alkynyl moieties 2-6C. ACTIVITY : Neuroprotective; spasmolytic; antiischemic; cytoprotective; cardiovascular; antitumor; antiinflammatory; antirheumatic. MECHANISM OF ACTION : Cystiene protease inhibitor; calpain inhibitor; cathepsin inhibitor; interleukin-1 antagonist. No results of biological activity tests are given, although test procedures are described.

    SUBSTITUTED BENZAMIDES, THEIR PRODUCTION AND THEIR USE AS CYSTEINE PROTEASE INHIBITORS
    46.
    发明专利
    SUBSTITUTED BENZAMIDES, THEIR PRODUCTION AND THEIR USE AS CYSTEINE PROTEASE INHIBITORS 未知

    公开(公告)号：PL343466A1

    公开(公告)日：2001-08-13

    申请号：PL34346699

    申请日：1999-04-19

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  TREIBER HANS-JOERG ,  KNOPP MONIKA

    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: Benzamides of the formula Iand its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings:R1-C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, -O-C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO-C1-C4-alkyl, NHCO-C1-C4-alkyl, andR2 can be NR5CO-R6 and NHR5SO2-R6, andR3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO-C1-C4-alkyl, NHSO2-C1-C4-alkyl, NO2, -O-C1-C4-alkyl, CN, COOH, CONH2, COO-C1-C4-alkyl, SO2-C1-C4-alkyl, -SO2Ph, SO2NH-C1-C4-alkyl, iodine, SO2NH2 and NH2, andA can be aromatic rings and heteroaromatic rings such as naphthyl, quinolyl, quinoxyl, benzimidazolyl, benzothienyl, quinazolyl, phenyl, thienyl, imidazolyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by by [sic] R9 and up to 2 R8 radicals, andB a bond, -(CH2)m-, -(CH2)m-O-(CH2)o-, -(CH2)o-S-(CH2)m-, -(CH2)o-SO-(CH2)m-, -(CH2)o-SO2-(CH2)m-, -CH=CH-, -C=C-, -CO-CH=CH-, -(CH2)o-CO-(CH2)m-, -(CH2)m-NHCO-(CH2)o-, -(CH2)m-CONH-(CH2)o-, -(CH2)m-NHSO2-(CH2)o-, -NH-CO-CH=CH-, -(CH2)m-SO2NH-(CH2)o-,A-B together alsoR5 hydrogen and C1-C4-alkyl andR6 is hydrogen, phenyl, naphthyl, C1-C6-alkyl, linear or branched, it being possible for a C atom in the chain to be substituted by a phenyl ring which itself may also be substituted by one or two R4 radicals, andR8 can be hydrogen, C1-C4-alkyl, branched or unbranched, -O-C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO-C1-C4-alkyl, -NHCO-C1-C4-alkyl, phenyl, NHCO-phenyl, -NHSO2-C1-C4-alkyl, -NHSO2-phenyl, -SO2-C1-C4-alkyl, pyridine [sic] and SO2-phenyl,R9 hydrogen, -CHR14-(CH2)p-R12 where R12 pyrrolidine [sic], morpholine [sic], piperidine [sic], hexahydroazepine [sic], homopiperazine [sic], and R10 [lacuna] C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring which is in turn substituted by by [sic] a maximum of two R11 radicals, where R11 is hydrogen, C1-C4-alkyl, branched or unbranched, -O-C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO-C1-C4-alkyl, NHCO-C1-C4-alkyl, -NHSO2-C1-C4-alkyl and -SO2-C1-C4-alkyl; andR13 is hydrogen and C1-C6-alkyl, branched or unbranched, andn,p is [sic], independently of one another, a number 0, 1 or 2, andm,o is [sic], independently of one another, a number 0, 1, 2, 3 or 4.

    47.
    发明专利
    未知

    公开(公告)号：BR9915013A

    公开(公告)日：2001-08-07

    申请号：BR9915013

    申请日：1999-10-28

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  GER THOMAS H

    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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