-
公开(公告)号:CA2349227C
公开(公告)日:2008-02-05
申请号:CA2349227
申请日:1999-10-28
Applicant: BASF AG
Inventor: HOGER THOMAS , KOCK MICHAEL , LUBISCH WILFRIED
IPC: C07D235/18 , 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 , C07D401/10 , C07D403/10 , C07D521/00 , C12Q1/48 , G01N33/00 , G01N33/15 , G01N33/573 , G01N33/577
Abstract: The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the producti on of said compounds and to their use.
-
公开(公告)号:CA2371174C
公开(公告)日:2007-02-20
申请号:CA2371174
申请日:2000-04-11
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , HOGER THOMAS , KOCK MICHAEL , SCHULT SABINE , MULLER REINHOLD , GRANDEL ROLAND
IPC: C07D235/06 , 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
Abstract: The invention relates to a compound of formula (I) or (II), wherein A represents a saturated or mono-unsaturated carbocycle containing 3 to 8 carb on atoms which can also have a condensed benzol ring, whereby the rings can als o be substituted with one or two different or identical radicals; R1 represent s hydrogen, chlorine, fluorine, bromine, iodine, branched and unbranched C1-C6 - alkyl, OH, nitro, CF3, CN, NR11R12, NH-CO-R13, O-C1-C4 alkyl; and R2 represents hydrogen, branched and unbranched C1-C6 alkyl, C1-C4 alkyl-phenyl . The invention also relates to the tautomeric forms, possible enantiomeric an d diastereomeric forms, possible cis-trans isomers on the rings in A and their prodrugs. The substituted benzimidazoles of general formulas (I) and (II) ar e inhibitors of poly(ADP-ribose) polymerase (PARP), or poly(ADP-ribose) syntha se (PARS), as it is also known and can be used for the treatment or prophylaxis of diseases which are associated with the increased enzyme activity of this enzyme.
-
公开(公告)号:CA2350734C
公开(公告)日:2006-10-10
申请号:CA2350734
申请日:1999-11-05
Applicant: BASF AG
Inventor: HOGER THOMAS , KOCK MICHAEL , LUBISCH WILFRIED
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: The invention relates to the use of 2-phenyl-benzimidazoles and 2- phenylindoles of general formula (I), wherein A means N or CH, R1 means hydrogen, branched and unbranched C1-C6 alkyl and a C-atom of the alkyl radical can also carry an OR11 or a group R5, R2 means hydrogen, chlorine, fluorine, bromine, iodine, branched and unbranched C1-C6 alkyl, nitro, CF3, CN, NR21R22, NH-CO-R23, OR21, R3 means(CH2)q-NR31R32 and q can be 0, 1, 2 or 3 and R4 means hydrogen, branched and unbranched C1-C6 alkyl, chlorine, bromine, fluorine, nitro, cyano, NR41R42, NH-CO-R43, OR41; as inhibitors of the enzym e poly(ADP-ribose)-polymerase for producing medicaments.
-
公开(公告)号:NZ514930A
公开(公告)日:2003-10-31
申请号:NZ51493000
申请日:2000-04-11
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , KOCK MICHAEL , HOGER THOMAS , RANDEL ROLAND , SCHULT SABINE , MULLER REINHOLD
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 , C07D2 , C07D40
Abstract: Compounds of formula I, or formula II, wherein the variables are defined herein. The compounds are used in the manufacture of medicaments for the treatment of disorders mediated by the inhibition of the enzyme poly(ADP-ribose) polymerase or PARP.
-
公开(公告)号:SK15952001A3
公开(公告)日:2002-08-06
申请号:SK15952001
申请日:2000-05-03
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , SADOWSKI JENS , KOCK MICHAEL , HOGER THOMAS
IPC: C07D237/32 , A61K31/502 , A61P1/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/10 , A61P25/12 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/04 , A61P37/00 , A61P41/00 , A61P43/00 , C07D401/12 , C07D403/12 , A61K31/00
Abstract: The present invention relates to the use of phthalazine derivatives as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30), to the use as inhibitors of PARP-homologous enzymes and, in particular, these phthalazine derivatives also show a selective inhibition of PARP-homologous enzymes.
-
公开(公告)号:HK1042084A1
公开(公告)日:2002-08-02
申请号:HK02103400
申请日:2002-05-04
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , KOCK MICHAEL , HOGER THOMAS , SCHULT SABINE , GRANDEL ROLAND , MULLER REINHOLD
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 , C07D , A61K , A61P
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:SK6742001A3
公开(公告)日:2001-12-03
申请号:SK6742001
申请日:1999-11-05
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , KOCK MICHAEL , HOGER THOMAS
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:SK5952001A3
公开(公告)日:2001-12-03
申请号:SK5952001
申请日:1999-10-28
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , 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.
-
公开(公告)号:PT775113E
公开(公告)日:2001-09-28
申请号:PT95926973
申请日:1995-07-22
Applicant: BASF AG
Inventor: STEINER GERD , UNGER LILIANE , TESCHENDORF HANS-JUERGEN , MUNSCHAUER RAINER , HOGER THOMAS
IPC: A61K31/40 , A61K31/403 , A61P25/18 , A61P43/00 , C07D209/44 , C07D409/12 , C07D209/52 , C07D209/90 , C07D209/92 , C07D403/06
Abstract: PCT No. PCT/EP95/02912 Sec. 371 Date Feb. 3, 1997 Sec. 102(e) Date Feb. 3, 1997 PCT Filed Jul. 22, 1995 PCT Pub. No. WO96/04245 PCT Pub. Date Feb. 15, 1996A compound of the formula in which A, R1 and n have the meanings stated in the description are described. The novel compounds are suitable for controlling diseases.
-
公开(公告)号:CZ20010465A3
公开(公告)日:2001-08-15
申请号:CZ20010465
申请日:1999-07-20
Applicant: BASF AG
Inventor: STEINER GERD , HOGER THOMAS , UNGER LILIANE , TESCHENDORF HANS-JURGEN , JUCHELKA FRIEDER
IPC: A61K31/4184 , A61P25/20 , A61P25/24 , A61P25/30 , C07D403/06
CPC classification number: C07D403/06
-
-
-
-
-
-
-
-
-