公开(公告)号：EP0640075A1

公开(公告)日：1995-03-01

申请号：EP92903112.0

申请日：1991-12-23

申请人： NEUROGEN CORPORATION

发明人： THURKAUF, Andrew, Y. ,  HUTCHISON, Alan, J.

IPC分类号： A61K31 ,  A61P25 ,  C07D233 ,  C07D401 ,  C07D403

CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： This invention encompasses compounds of formulas (I), where R1, R3, R4, R6, X, Y, and Z and T are variables; and M is α or β, where R2 is a variable; or R1 and R2 together may represent -(CH2)n1 where n1 is 1, 2, or 3. These compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extraparamidyl side effects associated with the use of conventional neuroleptic agents.

公开(公告)号：EP1809626A2

公开(公告)日：2007-07-25

申请号：EP05812516.2

申请日：2005-10-04

申请人： NEUROGEN CORPORATION

发明人： CHENARD, Bertrand, L ,  GHOSH, Manuka ,  DOLLER, Dario ,  HUTCHISON, Alan, J. ,  LI, Guiying

IPC分类号： C07D451/06 ,  C07D451/02 ,  C07D451/04 ,  A61K31/46 ,  A61P3/04

CPC分类号： C07D451/02 ,  C07D451/04 ,  C07D451/06

摘要： Aryl substituted 8-azabicyclo[3.2.1]octane compounds and analogues thereof, are provided. Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding, neuropsychiatric, reproductive and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

公开(公告)号：EP1807390A2

公开(公告)日：2007-07-18

申请号：EP05826325.2

申请日：2005-11-01

申请人： NEUROGEN CORPORATION

发明人： HUTCHISON, Alan, J. ,  YUAN, Jun

IPC分类号： C07C273/00 ,  C07C275/00

CPC分类号： A61K31/17 ,  Y10T436/171538

摘要： CB1 antagonists are provided. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 receptor modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.

公开(公告)号：EP1756107A2

公开(公告)日：2007-02-28

申请号：EP05760258.3

申请日：2005-06-16

申请人： NEUROGEN CORPORATION

发明人： HUTCHISON, Alan, J. ,  CHENARD, Bertrand, L. ,  LI, Guiying ,  GHOSH, Manuka ,  TARRANT, James, G. ,  YOON, Taeyoung ,  LUKE, George, P. ,  LEE, Kyungae ,  O'DONNELL, Mary-Margaret, E. ,  PRINGLE, Wallace, C. ,  PETERSON, John, M. ,  HODGETTS, Kevin, J. ,  STEENSTRA, Cheryl, K. ,  DOLLER, Dario

IPC分类号： C07D471/04 ,  C07D487/08 ,  C07D487/04 ,  C07D211/74 ,  C07D207/26 ,  C07D207/08 ,  C07D307/79 ,  C07D295/08 ,  C07D295/06 ,  C07D211/34 ,  A61P3/00

CPC分类号： C07D295/073 ,  C07D207/08 ,  C07D207/12 ,  C07D207/26 ,  C07D207/38 ,  C07D211/18 ,  C07D211/34 ,  C07D211/38 ,  C07D211/42 ,  C07D211/46 ,  C07D211/52 ,  C07D211/74 ,  C07D213/64 ,  C07D213/74 ,  C07D213/82 ,  C07D231/12 ,  C07D233/54 ,  C07D233/56 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D275/02 ,  C07D295/088 ,  C07D295/096 ,  C07D295/192 ,  C07D307/20 ,  C07D307/79 ,  C07D307/82 ,  C07D309/06 ,  C07D309/12 ,  C07D311/14 ,  C07D401/12 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08

摘要： Aryl-substituted piperazine derivatives are provided. Such compounds may be used to modulate MCH receptor activity in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH 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：EP1165555B1

公开(公告)日：2003-07-16

申请号：EP00919382.2

申请日：2000-03-10

申请人： NEUROGEN CORPORATION

发明人： YUAN, Jun ,  MAYNARD, George, D. ,  HUTCHISON, Alan, J.

IPC分类号： C07D471/00

CPC分类号： C07D471/04 ,  C07D495/04 ,  G01N2333/705

摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.

公开(公告)号：EP1165555A2

公开(公告)日：2002-01-02

申请号：EP00919382.2

申请日：2000-03-10

申请人： NEUROGEN CORPORATION

发明人： YUAN, Jun ,  MAYNARD, George, D. ,  HUTCHISON, Alan, J.

IPC分类号： C07D471/00

CPC分类号： C07D471/04 ,  C07D495/04 ,  G01N2333/705

摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.