公开(公告)号：NO20012570L

公开(公告)日：2001-07-13

申请号：NO20012570

申请日：2001-05-25

Applicant: BASF AG

Inventor： LUBISCH WILFRED ,  KOCK MICHAEL ,  HOEGER THOMAS ,  SCHULT SABINE ,  GRANDEL ROLAND ,  MUELLER 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

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：CA2371645A1

公开(公告)日：2000-11-16

申请号：CA2371645

申请日：2000-04-27

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  MULLER REINHOLD ,  GRANDEL ROLAND ,  HOGER THOMAS ,  KOCK MICHAEL ,  SCHULT SABINE ,  HOLZENKAMP UTA

IPC: C07D235/20 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07D235/18 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D209/00 ,  C07D213/00 ,  C07D235/00

Abstract: The present invention relates to novel benzimidazoles, the production thereo f and the utilisation as inhibitors of the enzyme poly(ADP-ribose)polymerase o r PARP (EC 2.4.2.30) for producing medicaments.

公开(公告)号：CA2371645C

公开(公告)日：2007-04-17

申请号：CA2371645

申请日：2000-04-27

Applicant: BASF AG

Inventor： MULLER REINHOLD ,  LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOGER THOMAS ,  GRANDEL ROLAND ,  HOLZENKAMP UTA ,  SCHULT SABINE

IPC: C07D235/18 ,  C07D235/20 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07D209/00 ,  C07D213/00 ,  C07D235/00 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04

Abstract: The present invention relates to novel benzimidazoles, the production thereo f and the utilisation as inhibitors of the enzyme poly(ADP-ribose)polymerase o r PARP (EC 2.4.2.30) for producing medicaments.

公开(公告)号：CA2352554C

公开(公告)日：2006-10-10

申请号：CA2352554

申请日：1999-11-23

Applicant: BASF AG

Inventor： KOCK MICHAEL ,  HOGER THOMAS ,  LUBISCH WILFRIED ,  SCHULT SABINE ,  GRANDEL ROLAND ,  MULLER REINHOLD

IPC: C07D401/04 ,  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 ,  C07D401/14 ,  C07D403/04

Abstract: The invention relates to compounds of general formula (1a) or (1b) wherein R 1 and R4 are hydrogen or defined substituents, A is a saturated or monoethenoid heterocyclic ring with 4 to 8 members which contains one or two nitrogen atoms, wherein additionally one oxygen or sulfur atom can be present. Said ring can be further substituted. The invention also relates to their tautomer forms, possible enantiomer and diastereomer forms, their prodrugs, as well as possible physiologically acceptable salts. The invention also relates to the use of said compounds for treating diseases related to a pathologically increased activity of PARP.

公开(公告)号：ZA200104196B

公开(公告)日：2002-07-25

申请号：ZA200104196

申请日：2001-05-23

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOEGER THOMAS ,  GRANDEL ROLAND ,  MUELLER REINHOLD ,  SCHULT SABINE

IPC: A61K31/5517 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P11/00 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07D487/06 ,  C07D519/00 ,  C07D ,  A61K ,  A61P

公开(公告)号：CO5170517A1

公开(公告)日：2002-06-27

申请号：CO00032472

申请日：2000-05-05

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  MCIHAEL KOCK ,  HOGER THOMAS ,  GRANDEL ROLAND ,  UTA HOLZENKAMP ,  SCHULT SABINE ,  MULLER REINHOLD

IPC: C07D235/20 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07D235/18 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04

Abstract: Compuesto de la fórmula I ó II dondeA significa naftalina, indol, benzimidazol, pirrol, imidazol, furano, tiofeno, benzotiofeno, benzofurano, pirazol, tiazol, benzotiazol, ftalamida, indazol, benzotriazol, ftalicina, indolina, isoindolina, piridina, quinolina, pirimidina, piridacina, isoquinolina, quinoxalina, quinozolina, isoxazol, oxasol, imidazopiridina, piracina, y pudiendo A estar sustituido todavía por hasta tres radicales R3 idénticos o diferentes y adicionalmente por un radical R4 yR1 significa hidrógeno, cloro, fluoro, bromo, yodo, C1-C6-alquilo ramificado o sin ramificar, OH, nitro, CF3, CN, NR11R12, NH-CO-R13, O-C1-C4-alquilo, pudiendo R11 R12 significar independientemente hidrógeno o C1-C4-alquil-fenilo o fenilo, yR2 significa hidrógeno, C1-C6-alquilo ramificado o sin ramificar yR3 significa hidrógeno, cloro, bromo, yodo, fluoro, CF3, OCF3, nitro, NH2, CO-R8, CO2-R8, SO2-R8, OH, OC1-C4-alquilo, O-C0-C4-alquil-fenilo, una cadena de 1 a 6 átomos de carbono, que puede estar saturada no saturada o parcialmente insaturada, y estar sustituida adicionalmente por un radical R33, fenilo, pudiendo los anillos fenilo estar sustituidos por hasta tres radicales R31 idénticos o diferentes, y piridilo, que puede estar sustituido por hasta tres radicales R132, yR31 significa OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro yodo, fluoro, CF3, nitro, NH2, yR32 significa OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro, NH2, CN, yR33 significa CO-NH-R8, OH, OC1-C6-alquilo, O-CO-R8, yR4 significa -(D)p-(E)s,-(CH2)q -B, dondeD significa S, NR43 y 0E significa fenilo ys es 0 y 1 y ...

公开(公告)号：BG105993A

公开(公告)日：2002-05-31

申请号：BG10599301

申请日：2001-10-09

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOEGER THOMAS ,  GRANDEL ROLAND ,  SCHULT SABINE ,  MUELLER 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 ,  C07D235/06

Abstract: The invention relates to a compound of formula or wherein A represents a saturated or mono-unsaturated carbocycle containing 3 to 8 carbon atoms which can also have a condensed benzol ring, whereby the rings can also be substituted with one or two different or identical radical; R1 represents 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 and diasteometric forms, possible cis-trans isomers on the rings in A and their prodrugs. The submitted benzimidazoles are inhibitors of poly(ADP-ribose)polymerase (PARP), or poly(ADP-ribose)synthase (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. 20 claims

公开(公告)号：BR0014326A

公开(公告)日：2002-05-28

申请号：BR0014326

申请日：2000-09-15

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOEGER THOMAS ,  GRANDEL ROLAND ,  MUELLER REINHOLD ,  SCHULT SABINE

IPC: A61K31/5517 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P11/00 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07D487/06 ,  C07D519/00 ,  C07D487/00

公开(公告)号：BR0010342A

公开(公告)日：2002-05-28

申请号：BR0010342

申请日：2000-04-27

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOEGER THOMAS ,  GRANDEL ROLAND ,  HOLZENKAMP UTA ,  SCHULT SABINE ,  MUELLER REINHOLD

IPC: C07D235/20 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07D235/18 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04

Abstract: The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.

公开(公告)号：ZA200104118B

公开(公告)日：2002-05-21

申请号：ZA200104118

申请日：2001-05-21

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOEGER THOMAS ,  SCHULT SABINE ,  GRANDEL ROLAND ,  MUELLER 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.