公开(公告)号：CA2499383A1

公开(公告)日：2004-04-01

申请号：CA2499383

申请日：2003-09-18

Applicant: AVENTIS PHARMA INC

Inventor： MEHDI SHUJAATH ,  LI ZHUYIN JULIE

IPC: C07D20060101 ,  C07D201/00 ,  C12Q1/48 ,  C12Q1/68 ,  G01N21/64 ,  G01N33/483

Abstract: Provided herein is a novel and useful method for determining whether a compound or agent decreases or inhibits the activity of a poly(ADP-ribose)- polymerase (PARP).

公开(公告)号：PE20060285A1

公开(公告)日：2006-05-08

申请号：PE2005000326

申请日：2005-03-22

Applicant: AVENTIS PHARMA INC

Inventor： WEINTRAUB PHILIP MARVIN ,  EASTWOOD PAUL ,  STEFANY DAVID WILLIAM ,  MOORCROFT NEIL DAVID ,  JIANG ZIQI JOHN ,  PEUKERT STEFAN ,  SCHWAHN UWE ,  RUTTEN HARTMUT ,  LIM SUNGTAEK ,  MUSICK KWON YON ,  MEHDI SHUJAATH

IPC: A61K31/44 ,  A61P9/00 ,  A61P9/10 ,  A61P25/28 ,  C07D213/62 ,  C07D213/64 ,  C07D217/24 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14

Abstract: REFERIDA A UN COMPUESTO DE FORMULA I DONDE R ES H O ALQUILO C1-C6; R1 ES ALQUILO C1-C4, ALQUENILO C1-C4, ENTRE OTROS; R2 ES Ar-Y, EN EL QUE Ar ES ARILO, ARILOILO, ENTRE OTROS; Y ES H, -SO2NR5R6, -C(O)R9, ENTRE OTROS; R3 ES H, ALQUILOC1-C4, ALQUENILO C1-C4, ENTRE OTROS; R4 ES ALQUILOC1-C6, ALQUENILO C1-C6, CICLOALQUILO C3-C8, ENTRE OTROS; R3 Y R4 TOMADOS CONJUNTAMENTE CON LOS ATOMOS DE CARBONO A LOS CUALES ESTAN UNIDOS FORMAN UN ANILLO CICLOALQUILO C4-C8 O UN ANILLO BENCENO; R5, R6, R7 Y R8 SON H, ALQUILO C1-C10, CICLOALQUILO C3-C8, ENTRE OTROS; R9 ES H, ALQUILO C1-C6, FENILO, ENTRE OTROS; R11 ES OH, ALCOXI C1-C3, -O-FENILO, ENTRE OTROS; n ES UN NUMERO ENTERO DESDE 1 A 4. TAMBIEN ESTA REFERIDA A COMPOSICIONES QUE COMPRENDEN ESTOS COMPUESTOS CUYOS PREFERIDOS SON 3-(5-ETIL-2-METIL-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL)BENZONITRILO, 3-(2,5-DIMETIL-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL)BENZONITRILO, 3-(5-CICLOPROPIL-2-METIL-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL)BENZONITRILO, ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE LA POLI(ADENOSINA 5'-DIFOSFATO RIBOSA)-POLIMERASA (PARP) Y SON UTILES PARA EL TRATAMIENTO Y/O PREVENCION DE UNA DIVERSIDAD DE ENFERMEDADES, INCLUYENDO ENFERMEDADES ASOCIADAS CON EL SISTEMA NERVIOSO CENTRAL Y TRASTORNOS CARDIOVASCULARES

公开(公告)号：PE02852006A1

公开(公告)日：2006-05-08

申请号：PE0003262005

申请日：2005-03-22

Applicant: AVENTIS PHARMA INC

Inventor： WEINTRAUB PHILIP MARVIN ,  EASTWOOD PAUL ,  STEFANY DAVID WILLIAM ,  MOORCROFT NEIL DAVID ,  JIANG ZIQI JOHN ,  PEUKERT STEFAN ,  SCHWAHN UWE ,  RUTTEN HARTMUT ,  LIM SUNGTAEK ,  MUSICK KWON YON ,  MEHDI SHUJAATH

IPC: A61K31/44 ,  A61P9/00 ,  A61P9/10 ,  A61P25/28 ,  C07D213/62 ,  C07D213/64 ,  C07D217/24 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14

CPC classification number: C07D213/64 ,  C07D217/24 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14

Abstract: REFERIDA A UN COMPUESTO DE FORMULA I DONDE R ES H O ALQUILO C1-C6; R1 ES ALQUILO C1-C4, ALQUENILO C1-C4, ENTRE OTROS; R2 ES Ar-Y, EN EL QUE Ar ES ARILO, ARILOILO, ENTRE OTROS; Y ES H, -SO2NR5R6, -C(O)R9, ENTRE OTROS; R3 ES H, ALQUILOC1-C4, ALQUENILO C1-C4, ENTRE OTROS; R4 ES ALQUILOC1-C6, ALQUENILO C1-C6, CICLOALQUILO C3-C8, ENTRE OTROS; R3 Y R4 TOMADOS CONJUNTAMENTE CON LOS ATOMOS DE CARBONO A LOS CUALES ESTAN UNIDOS FORMAN UN ANILLO CICLOALQUILO C4-C8 O UN ANILLO BENCENO; R5, R6, R7 Y R8 SON H, ALQUILO C1-C10, CICLOALQUILO C3-C8, ENTRE OTROS; R9 ES H, ALQUILO C1-C6, FENILO, ENTRE OTROS; R11 ES OH, ALCOXI C1-C3, -O-FENILO, ENTRE OTROS; n ES UN NUMERO ENTERO DESDE 1 A 4. TAMBIEN ESTA REFERIDA A COMPOSICIONES QUE COMPRENDEN ESTOS COMPUESTOS CUYOS PREFERIDOS SON 3-(5-ETIL-2-METIL-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL)BENZONITRILO, 3-(2,5-DIMETIL-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL)BENZONITRILO, 3-(5-CICLOPROPIL-2-METIL-6-OXO-1,6-DIHIDRO-PIRIDIN-3-IL)BENZONITRILO, ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE LA POLI(ADENOSINA 5'-DIFOSFATO RIBOSA)-POLIMERASA (PARP) Y SON UTILES PARA EL TRATAMIENTO Y/O PREVENCION DE UNA DIVERSIDAD DE ENFERMEDADES, INCLUYENDO ENFERMEDADES ASOCIADAS CON EL SISTEMA NERVIOSO CENTRAL Y TRASTORNOS CARDIOVASCULARES

公开(公告)号：PT802909E

公开(公告)日：2002-03-28

申请号：PT95943478

申请日：1995-12-15

Applicant: AVENTIS PHARMA INC

Inventor： PEET NORTON PAUL ,  MEHDI SHUJAATH ,  LINNIK MATTHEW D ,  KIM HWA-OK ,  ANGELASTRO MICHAEL R

IPC: C07D263/06 ,  A61K31/42 ,  A61K31/421 ,  A61K31/535 ,  A61K31/5377 ,  A61K38/00 ,  A61P9/08 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D263/04 ,  C07D263/18 ,  C07K5/062

Abstract: This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

公开(公告)号：DE69523072D1

公开(公告)日：2001-11-08

申请号：DE69523072

申请日：1995-12-15

Applicant: AVENTIS PHARMA INC

Inventor： PEET P ,  MEHDI SHUJAATH ,  LINNIK D ,  ANGELASTRO R ,  KIM HWA-OK

IPC: C07D263/06 ,  A61K31/42 ,  A61K31/421 ,  A61K31/535 ,  A61K31/5377 ,  A61K38/00 ,  A61P9/08 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D263/04 ,  C07D263/18 ,  C07K5/062

Abstract: This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

公开(公告)号：NO309267B1

公开(公告)日：2001-01-08

申请号：NO973216

申请日：1997-07-10

Applicant: AVENTIS PHARMA INC

Inventor： PEET NORTON PAUL ,  MEHDI SHUJAATH ,  LINNIK MATTHEW D ,  ANGELASTRO MICHAEL RICHARD ,  KIM HWA-OK

IPC: C07D263/06 ,  A61K31/42 ,  A61K31/421 ,  A61K31/535 ,  A61K31/5377 ,  A61K38/00 ,  A61P9/08 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D263/04 ,  C07D263/18 ,  C07K5/062

Abstract: This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

公开(公告)号：BRPI0414136A

公开(公告)日：2006-10-31

申请号：BRPI0414136

申请日：2004-09-01

Applicant: AVENTIS PHARMA INC

Inventor： JIANG JOHN Z ,  KOEHL JACK R ,  MEHDI SHUJAATH ,  MOORCROFT NEIL ,  MUSICK KWON YON ,  WEINTRAUB PHILIP MARVIN ,  EASTWOOD PAUL R

IPC: A61K31/404 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/503 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61P9/10 ,  C07D209/40 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D471/04 ,  C07D487/08

Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

公开(公告)号：AU2004270187A1

公开(公告)日：2005-03-17

申请号：AU2004270187

申请日：2004-09-01

Applicant: AVENTIS PHARMA INC

Inventor： MUSICK KWON YON ,  EASTWOOD PAUL R ,  KOEHL JACK R ,  MOORCROFT NEIL ,  MEHDI SHUJAATH ,  WEINTRAUB PHILIP M ,  JIANG JOHN Z

IPC: A61K31/404 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/503 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61P9/10 ,  C07D209/40 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D471/04 ,  C07D487/08

Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

公开(公告)号：AT206413T

公开(公告)日：2001-10-15

申请号：AT95943478

申请日：1995-12-15

Applicant: AVENTIS PHARMA INC

Inventor： PEET NORTON P ,  MEHDI SHUJAATH ,  LINNIK MATTHEW D ,  ANGELASTRO MICHAEL R ,  KIM HWA-OK

IPC: C07D263/06 ,  A61K31/42 ,  A61K31/421 ,  A61K31/535 ,  A61K31/5377 ,  A61K38/00 ,  A61P9/08 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D263/04 ,  C07D263/18 ,  C07K5/062

Abstract: This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

公开(公告)号：CA2561280A1

公开(公告)日：2005-10-20

申请号：CA2561280

申请日：2005-03-29

Applicant: AVENTIS PHARMA INC

Inventor： WEINTRAUB PHILIP M ,  MEHDI SHUJAATH ,  PEUKERT STEFAN ,  EASTWOOD PAUL R ,  STEFANY DAVID W ,  LIM SUNGTAEK ,  SCHWAHN UWE ,  MOORCROFT NEIL ,  MUSICK KWON YON ,  JIANG JOHN Z ,  RUTTEN HARTMUT

IPC: C07D213/62 ,  A61K31/44 ,  A61P9/00 ,  A61P9/10 ,  A61P19/02 ,  A61P25/28 ,  A61P29/00 ,  C07D213/64 ,  C07D217/24 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14

Abstract: The present invention discloses and claims a series of 2,3,5-substituted pyridone derivatives as defined herein. This invention also relates to metho ds of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5'-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or preventi on of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.