公开(公告)号：WO2005028480A3

公开(公告)日：2005-06-02

申请号：PCT/US2004028663

申请日：2004-09-03

Applicant: NEUROGEN CORP ,  AVENTIS PHARMA INC ,  HODGETTS KEVIN J ,  JOHN STANLY ,  MOORCROFT NEIL ,  SHUTSKE GREG ,  KAISER BERND ,  YAMAGUCHI YASUCHIKA ,  GE PING ,  HORVATH RAYMOND F

Inventor： HODGETTS KEVIN J ,  JOHN STANLY ,  MOORCROFT NEIL ,  SHUTSKE GREG ,  KAISER BERND ,  YAMAGUCHI YASUCHIKA ,  GE PING ,  HORVATH RAYMOND F

IPC: A61K31/519 ,  A61K31/53 ,  C07D471/04 ,  C07D487/02 ,  C07D487/04 ,  C07D519/00 ,  A61K31/437 ,  A61P25/18 ,  A61P25/22

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: 5-aryl-Pyrazolo[4,3-d] pyrimidines, 6-aryl-Pyrazolo[3,4-d]pyrimidines and related compounds, as well as other chemically related compounds, that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRIF receptor binding. Methods of using the compounds in receptor localization studies are given.

Abstract translation: 提供了作为CRF 1受体的选择性调节剂的5-芳基 - 吡唑并[4,3-d]嘧啶，6-芳基 - 吡唑并[3,4-d]嘧啶和相关化合物以及其它化学相关化合物 。 这些化合物可用于治疗许多中枢神经系统和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。 还提供了治疗这种疾病以及包装的药物组合物的方法。 本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRIF受体结合的测定中的标准物。 给出了在受体定位研究中使用化合物的方法。

公开(公告)号：WO2005023806A2

公开(公告)日：2005-03-17

申请号：PCT/US2004028899

申请日：2004-09-03

Applicant: NEUROGEN CORP ,  AVENTIS PHARMA INC

Inventor： GE PING ,  HORVATH RAYMOND F ,  ZHANG LU YAN ,  YAMAGUCHI YASUCHIKA ,  KAISER BERND ,  ZHANG XUECHUN ,  ZHANG SUOMING ,  ZHAO HE ,  JOHN STANLY ,  MOORCROFT NEIL ,  SHUTSKE GREG

IPC: A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D471/00

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

Abstract translation: 提供了作为CRF 1受体的选择性调节剂的取代的杂芳基稠合的吡啶，吡嗪和嘧啶化合物。 这些化合物可用于治疗许多中枢神经系统和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。 还提供了治疗这种疾病以及包装的药物组合物的方法。 本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。 给出了在受体定位研究中使用化合物的方法。

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.

公开(公告)号：AU2004274403A1

公开(公告)日：2005-03-31

申请号：AU2004274403

申请日：2004-09-03

Applicant: AVENTIS PHARMA INC ,  NEUROGEN CORP

Inventor： HORVATH RAYMOND F ,  KAISER BERND ,  GE PING ,  MOORCROFT NEIL ,  JOHN STANLY ,  SHUTSKE GREG ,  YAMAGUCHI YASUCHIKA ,  HODGETTS KEVIN J

IPC: C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/53 ,  A61P25/18 ,  A61P25/22 ,  C07D231/00 ,  C07D239/00 ,  C07D241/00 ,  C07D249/00 ,  C07D471/04 ,  C07D487/02 ,  C07D519/00

Abstract: 5-aryl-Pyrazolo[4,3-d]pyrimidines, 6-aryl-Pyrazolo[3,4-d]pyrimidines and related compounds, as well as other chemically related compounds, that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

公开(公告)号：MA28086A1

公开(公告)日：2006-08-01

申请号：MA28916

申请日：2006-04-05

Applicant: NEUROGEN CORP ,  AVENTIS PHARMA INC

Inventor： ZHAO HE ,  HORVATH RAYMOND F ,  ZHANG LU YAN ,  YAMAGUCHI YASUCHIKA ,  KAISER BERND ,  ZHANG XUECHUN ,  ZHANG SUOMING ,  JOHN STANLY ,  MOORCROFT NEIL ,  SHUTSKE GREG ,  GE PING

IPC: A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D471/00

Abstract: DEPOSANT Sociétés dites: AVENTIS PHARMA.CEUTICALS INC. NEUROGEN CORPORATION REVENDICATION DE PRIORITES QS 5 Septembre 2003 60/500,414 Voir en annexe le titre de l'invention et le texte de l'abrégé Pyridines, pyrazines et pyrimidines condensées avec un noyau héréroaryle, servant de ligands du récepteur CRF1 Des pyridines, pyrazines et pyrimidines condensées avec un noyau hétéroaryle substitué qui jouent le rôle de modulateurs sélectifs des récepteurs CRF1 sont proposées. Ces composés sont utiles dans le traitement d'un certain nombre de troubles du système nerveux central (SNC) et de troubles périphériques, en particulier du stress, de l'anxiété, de la dépression, de troubles cardiovasculaires et de troubles du comportement alimentaire. Il est proposé également des méthodes pour le traitement de ces troubles ainsi que des compositions pharmaceutiques emballées. Des composés de la présente invention sont également utiles comme sondes pour la localisation de récepteurs du CRF et comme agents de référence dans des analyses pour la liaison aux récepteurs de CRF. Des méthodes d'utilisation des composés dans des études de localisation de récepteurs sont présentées.

公开(公告)号：CA2496197A1

公开(公告)日：2004-03-04

申请号：CA2496197

申请日：2003-08-20

Applicant: NEUROGEN CORP ,  AVENTIS PHARMA INC

Inventor： YOON TAEYOUNG ,  GE PING ,  DELOMBAERT STEPHANE ,  HORVATH RAYMOND F ,  JOHN STANLY ,  SHUTSKE GREG ,  KAISER BERND ,  DARROW JIM ,  YAMAGUCHI YASUCHIKA ,  ZHANG CUNYU ,  MOORCROFT NEIL ,  HODGETTS KEVIN ,  ZHANG XUECHUM ,  DOLLER DARIO ,  LU JINQI ,  ZHANG LU YAN

IPC: A61P25/22 ,  A61P25/24 ,  C07D241/12 ,  C07D241/18 ,  C07D241/20 ,  C07D241/26 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  A61K31/497

Abstract: Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds ca n act as selective modulators of CRF receptors. The 5-substituted-2-arylpyrazi ne compounds provided herein are useful in the treatment of a number of CNS and peripheral disorders, particularly stress, anxiety, depression, cardiovascul ar disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

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：ECSP066408A

公开(公告)日：2006-09-18

申请号：ECSP066408

申请日：2006-03-03

Applicant: NEUROGEN CORP ,  AVENTIS PHARMA INC

Inventor： GE PING ,  HORVATH RAYMOND F ,  ZHANG YAN LU ,  YAMAGUCHI YASUCHIKA ,  KAISER BERND ,  ZHANG XUECHUN ,  ZHANG SUOMING ,  ZHAO HE ,  JOHN STANLY ,  MOORCROFT NEIL ,  SHUTSKE GREG

IPC: A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  C07D471/00 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: Compuestos heteroarilo fusionados con piridinas, pirazinas y pirimidinas de fórmulas I-a, I-b, XX, I-a I-b XXdonde Z1, Z2, Z3, Z4, Z5, E, Ar y R son como se define en la memoria descriptiva, útiles en el tratamiento de diveros desórdenes periféricos del sistema nervioso central, particularmente estrés, ansiedad, depresió, desórdenes cardiovasculares y desordenes alimentarios; composiciones farmacéuticas que los contienen; y métodos para ensayar la localización de CRF en muestras biológicas.

公开(公告)号：NO20061180A

公开(公告)日：2006-03-31

申请号：NO20061180

申请日：2006-03-14

Applicant: AVENTIS PHARMA INC

Inventor： GE PING ,  HORVATH RAYMOND F ,  KAISER BERND ,  ZHANG YAN LU ,  YAMAGUCHI YASUCHIKA ,  ZHANG XUECHUN ,  ZHANG SUOMING ,  ZHAO HE ,  JOHN STANLY ,  MOORCROFT NEIL ,  SHUTSKE GREG

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  C07D487/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D487/04

公开(公告)号：CA2537829A1

公开(公告)日：2005-03-17

申请号：CA2537829

申请日：2004-09-03

Applicant: NEUROGEN CORP ,  AVENTIS PHARMA INC

Inventor： GE PING ,  HORVATH RAYMOND F ,  ZHANG LU YAN ,  ZHAO HE ,  MOORCROFT NEIL ,  JOHN STANLY ,  SHUTSKE GREG ,  ZHANG XUECHUN ,  ZHANG SUOMING ,  KAISER BERND ,  YAMAGUCHI YASUCHIKA

IPC: C07D487/04 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61P9/00 ,  A61P25/24 ,  C07D471/04 ,  C07D519/00

Abstract: Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds th at act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eati ng disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention ar e also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in recept or localization studies are given.