公开(公告)号：EP1347982B1

公开(公告)日：2005-11-16

申请号：EP01270536.4

申请日：2001-12-11

申请人： NEUROGEN CORPORATION ,  PFIZER INC.

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry, L. ,  DARROW, James, William ,  DE LOMBAERT, Stephane ,  HUTCHISON, Alan ,  TRAN, Jennifer ,  ZHENG, Xiaozhang ,  ELLIOTT, Richard, Louis ,  HAMMOND, Marlys

IPC分类号： C07D491/10 ,  A61K31/517 ,  A61K31/438

CPC分类号： C07D487/04 ,  C07D491/10

摘要： Substituted spiro [isobenzofuran-1,4'-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4'-piperidines capable of modulating NPY5 receptor activity are provided (1) . Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders(e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and method for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

公开(公告)号：EP1347982A2

公开(公告)日：2003-10-01

申请号：EP01270536.4

申请日：2001-12-11

申请人： Neurogen Corporation ,  PFIZER INC.

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry, L. ,  DARROW, James, William ,  DE LOMBAERT, Stephane ,  HUTCHISON, Alan ,  TRAN, Jennifer ,  ZHENG, Xiaozhang ,  ELLIOTT, Richard, Louis ,  HAMMOND, Marlys

IPC分类号： C07D491/10

CPC分类号： C07D487/04 ,  C07D491/10

摘要： Substituted spiro [isobenzofuran-1,4'-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4'-piperidines capable of modulating NPY5 receptor activity are provided (1) . Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders(e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and method for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

公开(公告)号：EP1165518A2

公开(公告)日：2002-01-02

申请号：EP00919946.4

申请日：2000-03-31

申请人： NEUROGEN CORPORATION

发明人： DESIMONE, Robert, W. ,  HUTCHISON, Alan ,  SHAW, Kenneth ,  MAYNARD, George, D. ,  PETERSON, John, M. ,  LEW, Richard ,  BRIELMANN, Harry, L.

IPC分类号： C07D235/14 ,  C07D471/04 ,  C07D403/10 ,  C07D401/06 ,  A61K31/415 ,  A61K31/495 ,  A61K31/535 ,  A61K31/44

CPC分类号： C07D471/04

摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable salts thereof wherein: R1 is not 3-fluorobenzyl and represents (C2-C6) alkenyl, aryl (C1-C6)alkyl or heteroaryl (C1-C6)alkyl, OR7, O(CH2)nC(O)R7, O(CH2)nNR7R8, O(CH2)nCO2R7, NR7COR8, COR7, CONR7R8 or CO2R7; R2 represents hydrogen, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, amino (C1-C6)alkyl, mono- or di(C1-C6)alkylamino (C1-C6), or mono- or di(C1-C6)alkylamino(C1-C6)alkoxy; or OR7, O(CH2)nC(O)R7, O(CH2)nNR7R8, O(CH2)nCO2R7, NR7COR8, COR7, CONR7R8 or CO2R7; R3 represents (C1-C6)alkyl; R4 represents halogen or trifluoromethyl; R5 and R6 represent hydrogen, trifluoromethyl, triluoromethoxy, cyano, (C1-C6)alkyl, halogen, (C1-C6)alkylamino(C1-C6)alkyl, mono or di(C1-C6)alkylamino(C1-C6), or mono- or di(C1-C6)alkylamino(C1-C6)alkoxy; or together form a 5 or 6 membered aromatic ring which is optionally substituted. X represents a bond or CH2 which is optionally mono- or disubstituted with a (C1-C6)alkyl or (C1-C6)alkoxy; and A, B, C and D are the same or different and represent CRp or N with the proviso that not more than two of A,B, C and D represent N; which compounds are selective modulators of Bradykinin B2 receptors.

公开(公告)号：EP1471910A2

公开(公告)日：2004-11-03

申请号：EP03703887.4

申请日：2003-01-17

申请人： NEUROGEN CORPORATION

发明人： BAKTHAVATCHALAM, Rajagopal ,  BLUM, Charles, A. ,  BRIELMANN, Harry, L. ,  CALDWELL, Timothy, M. ,  DE LOMBAERT, Stéphane ,  HODGETTS, Kevin, J. ,  YOON, Taeyoung ,  ZHENG, Xiaozhang

IPC分类号： A61K31/4706

CPC分类号： C07D401/04 ,  C07D215/42 ,  C07D215/44 ,  C07D237/34 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D471/04

摘要： This invention relates generally to substituted quinazolin-4-ylamine analogues that are modulators of capsaicin receptors, and to the use of such compounds for treating conditions related to capsaicin receptor activation. The invention further relates to the use such compounds as probes for the detection and localization of capsaicin receptors.

摘要翻译： 本发明一般涉及作为辣椒素受体调节剂的取代的喹唑啉-4-基胺类似物，并涉及这类化合物用于治疗与辣椒素受体活化有关的病症的用途。 本发明进一步涉及使用这些化合物作为用于辣椒素受体的检测和定位的探针。