公开(公告)号：EP1322309B1

公开(公告)日：2008-08-13

申请号：EP00965522.6

申请日：2000-09-29

申请人： NEUROGEN CORPORATION

发明人： THURKAUF, Andrew ,  ZHANG, Xiaoyan ,  HE, Xia-shu ,  ZHAO, He ,  PETERSON, John ,  MAYNARD, George ,  OHLIGER, Robert

IPC分类号： C07D405/12 ,  C07D233/54 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D401/12 ,  A61K31/38 ,  A61K31/40 ,  A61K31/44 ,  A61K31/415 ,  A61K31/47

CPC分类号： C07D207/327 ,  A61K31/38 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  A61K31/47 ,  C07D217/04 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D333/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D471/04

摘要： The invention includes low molecular weight, non-peptidic, non-peptidommetic, organic molecules that can act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also such ligands that can act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure; 2) heteroaryl in structure; 3) a pharmaceutically acceptable oral dose can provide a detectable in vivo effect; 4) comprise fewer than four or preferably no amide bonds, and 5) capable of habiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. The invention also includes pharmaceutical composition comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders.

公开(公告)号：EP1322309A2

公开(公告)日：2003-07-02

申请号：EP00965522.6

申请日：2000-09-29

申请人： Neurogen Corporation

发明人： THURKAUF, Andrew ,  ZHANG, Xiaoyan ,  HE, Xia-shu ,  ZHAO, He ,  PETERSON, John ,  MAYNARD, George ,  OHLIGER, Robert

IPC分类号： A61K31/38 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  A61K31/47 ,  C07D215/00 ,  C07D233/02 ,  C07D235/02 ,  C07D317/44 ,  C07D405/00 ,  C07D419/00 ,  C07D471/02

CPC分类号： C07D207/327 ,  A61K31/38 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  A61K31/47 ,  C07D217/04 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D333/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D471/04

摘要： The invention includes low molecular weight, non-peptidic, non-peptidommetic, organic molecules that can act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also such ligands that can act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure; 2) heteroaryl in structure; 3) a pharmaceutically acceptable oral dose can provide a detectable in vivo effect; 4) comprise fewer than four or preferably no amide bonds, and 5) capable of habiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. The invention also includes pharmaceutical composition comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders.

公开(公告)号：EP1909797A2

公开(公告)日：2008-04-16

申请号：EP06788999.8

申请日：2006-07-28

申请人： NEUROGEN CORPORATION

发明人： XIE, Linghong ,  OCHTERSKI, Joseph W. ,  GAO, Yang ,  HAN, Bingsong ,  CALDWELL, Timothy M. ,  XU, Yuelian ,  PETERSON, John M. ,  GE, Ping ,  OHLIGER, Robert

IPC分类号： A61K31/551 ,  A61K31/55 ,  A61K31/497 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/454 ,  C07D403/02

CPC分类号： C07D403/06 ,  C07D207/09 ,  C07D207/14 ,  C07D211/14 ,  C07D211/34 ,  C07D211/52 ,  C07D211/58 ,  C07D211/64 ,  C07D211/72 ,  C07D213/74 ,  C07D213/82 ,  C07D215/48 ,  C07D217/02 ,  C07D237/20 ,  C07D237/22 ,  C07D237/24 ,  C07D239/47 ,  C07D241/08 ,  C07D241/20 ,  C07D243/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/56 ,  C07D277/82 ,  C07D295/033 ,  C07D295/185 ,  C07D295/192 ,  C07D295/215 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/10 ,  C07D491/107

摘要： Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

公开(公告)号：EP1651636A1

公开(公告)日：2006-05-03

申请号：EP04778036.6

申请日：2004-07-09

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  HODGETTS, Kevin, J. ,  HUTCHISON, Alan, J. ,  OHLIGER, Robert ,  YOON, Taeyoung ,  ZHENG, Xiaozhang

IPC分类号： C07D401/12 ,  C07D251/52 ,  C07D251/54 ,  C07D401/14 ,  A61K31/506 ,  A61K31/53 ,  A61P17/02 ,  A61P11/06 ,  A61P19/00 ,  A61P13/02 ,  A61P11/14 ,  A61P3/04

CPC分类号： C07D401/12 ,  A61K31/506 ,  A61K31/53 ,  C07D251/52 ,  C07D251/54 ,  C07D401/14 ,  G01N33/566

摘要： Substituted heterocyclic diarylamine analogues of Formula I are provided: wherein X, Y and Z are independently N or optionally substituted C, and other variables are as described in the specification. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

公开(公告)号：EP1487798A1

公开(公告)日：2004-12-22

申请号：EP03714371.6

申请日：2003-03-25

申请人： Neurogen Corporation

发明人： MITCHELL, Scott ,  OHLIGER, Robert ,  ZHANG, LuYan ,  ZHAO, He ,  CURRIE, Kevin ,  LEE, Kyungae

IPC分类号： C07D217/04 ,  A61K31/47

CPC分类号： C07D221/20 ,  A61K31/47 ,  C07D211/14 ,  C07D211/70 ,  C07D217/04 ,  C07D217/14 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D417/12 ,  C07D495/04

摘要： Substituted tetrahydroisoquinolines of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.