公开(公告)号：BR9915701A

公开(公告)日：2001-08-14

申请号：BR9915701

申请日：1999-11-23

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  GER THOMAS H ,  SCHULT SABINE ,  GRANDEL ROLAND ,  LLER REINHOLD M

IPC: A61K20060101 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/496 ,  A61P20060101 ,  A61P3/12 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D235/30 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

Abstract: Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.

公开(公告)号：BR9915381A

公开(公告)日：2001-08-14

申请号：BR9915381

申请日：1999-11-05

Applicant: BASF AG

Inventor： LUBIDCH WILFRIED ,  KOCK MICHAEL ,  GER THOMAS H

IPC: C07D235/18 ,  A61K20060101 ,  A61K31/10 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/454 ,  A61P20060101 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P13/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07D20060101 ,  C07D209/14 ,  C07D235/04

Abstract: 2-Phenylbenzimidazoles and 2-phenylindoles of formula IwhereinA is N or CH,R1 is hydrogen or alkyl which optionally carries an OR11 group,R11 is hydrogen or alkyl,R2 is hydrogen, chlorine, fluorine, bromine, iodine, alkyl, nitro, CF3, CN, NR21R22, NH-CO-R23, OR21,R21 and R22 are each hydrogen or alkyl,R23 is hydrogen, alkyl or phenyl,R3 is -(CH2)q-NR31R32,q is 0, 1, 2 or 3,R31 is hydrogen, alkyl, (CH2)rNR33R34,R32 is (CH2)rNR33R34,r is 2, 3, 4, 5 or 6,R33 and R34 are each hydrogen, alkyl or phenylalkyl wherein the phenyl ring is optionally substituted, orR33 and R34 and the nitrogen atom form a 3- to 8-membered ring,R4 is hydrogen, alkyl, chlorine, bromine, fluorine, nitro, cyano, NR41R42, NH-CO-R43, OR41,R41 and R42 are each hydrogen or alkyl, andR43 is alkyl or phenyl,are useful as inhibitors of poly(ADP-ribose)polymerase and for the production of drugs.

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.