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1. 发明申请

WO2006102645A1 BIARYL DERIVED AMIDE MODULATORS OF VANILLOID VR1 RECEPTOR 审中-公开
标题翻译： VANILLOID VR1受体的BIARYL衍生的AMEM调节剂
公开(公告)号：WO2006102645A1
公开(公告)日：2006-09-28
申请号：PCT/US2006/010994
申请日：2006-03-23
申请人： JANSSEN PHARMACEUTICA, N.V. , CODD, Ellen , DAX, Scott , FLORES, Christopher , JETTER, Michelle , YOUNGMAN, Mark
发明人： CODD, Ellen , DAX, Scott , FLORES, Christopher , JETTER, Michelle , YOUNGMAN, Mark
IPC分类号： C07C233/29 , C07C233/55 , C07C237/42 , C07D213/53 , C07D213/75 , A61K31/167 , A61K31/44 , A61K31/4164 , A61K31/4245 , A61K31/431 , A61K31/381 , A61P29/00 , C07D333/24 , C07D401/12 , C07D271/06 , C07D291/04
CPC分类号： C07D291/04 , C07C233/29 , C07C233/55 , C07C237/42 , C07D213/53 , C07D213/75 , C07D233/64 , C07D233/68 , C07D235/06 , C07D271/06 , C07D333/24 , C07D401/04 , C07D401/12
摘要： The invention is directed to novel vanilloid receptor type 1 (VR1) ligands. More specifically, the invention relates to novel biaryl-derived amides that are potent antagonists or agonists of VR1. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
摘要翻译：本发明涉及新型香草素受体1型（VR1）配体。更具体地，本发明涉及作为VR1的有效拮抗剂或激动剂的新型联芳基衍生的酰胺。还描述了使用本发明的化合物治疗轻度至重度疼痛和各种疾病的药物和兽医组合物和方法。

2. 发明申请

WO2004007459A3 NAPHTHOL, QUINOLINE AND ISOQUINOLINE-DERIVATIVES AS MODULATORS OF VANILLOID VR1 RECEPTOR 审中-公开
标题翻译：作为VANILLOID VR1受体的调节剂的萘酚，喹啉和异喹啉衍生物
公开(公告)号：WO2004007459A3
公开(公告)日：2004-03-18
申请号：PCT/US0321518
申请日：2003-07-10
申请人： JANSSEN PHARMACEUTICA NV , CODD ELLEN , DAX SCOTT L , JETTER MICHELE , MCDONNELL MARK , MCNALLY JAMES J , YOUNGMAN MARK
发明人： CODD ELLEN , DAX SCOTT L , JETTER MICHELE , MCDONNELL MARK , MCNALLY JAMES J , YOUNGMAN MARK
IPC分类号： C07C275/28 , C07C275/30 , C07C275/32 , C07D213/40 , C07D215/38 , C07D217/02 , C07D217/22 , C07D217/24 , C07D235/10 , C07D235/14 , C07D307/52 , C07D333/20 , C07D333/58 , C07D401/12 , C07D409/04 , A61K31/34 , A61K31/472 , C07D307/38
CPC分类号： C07C275/28 , C07C275/30 , C07C275/32 , C07D213/40 , C07D215/38 , C07D217/02 , C07D217/22 , C07D217/24 , C07D235/14 , C07D307/52 , C07D333/20 , C07D333/58 , C07D401/12 , C07D409/04
摘要： This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to naphthol, quinoline and isoquinoline-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
摘要翻译：本发明涉及香草素受体VR1配体。更具体地说，本发明涉及作为VR1的有效拮抗剂或激动剂的萘酚，喹啉和异喹啉衍生的脲，其可用于治疗和预防哺乳动物的炎性和其它疼痛状况。

3. 发明申请

WO2004007459A2 NAPHTHOL, QUINOLINE AND ISOQUINOLINE-DERIVED UREA MODULATORS OF VANILLOID VR1 RECEPTOR 审中-公开
标题翻译：香兰素VR1受体NAPHTHOL，QUINOLINE和异喹啉衍生的尿素调节剂
公开(公告)号：WO2004007459A2
公开(公告)日：2004-01-22
申请号：PCT/US2003/021518
申请日：2003-07-10
申请人： JANSSEN PHARMACEUTICA N.V. , CODD, Ellen , DAX, Scott, L. , JETTER, Michele , MCDONNELL, Mark , MCNALLY, James, J. , YOUNGMAN, Mark
发明人： CODD, Ellen , DAX, Scott, L. , JETTER, Michele , MCDONNELL, Mark , MCNALLY, James, J. , YOUNGMAN, Mark
IPC分类号： C07D215/00
CPC分类号： C07C275/28 , C07C275/30 , C07C275/32 , C07D213/40 , C07D215/38 , C07D217/02 , C07D217/22 , C07D217/24 , C07D235/14 , C07D307/52 , C07D333/20 , C07D333/58 , C07D401/12 , C07D409/04
摘要： This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to naphthol, quinoline and isoquinoline-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
摘要翻译：本发明涉及香草素受体VR1配体。更具体地说，本发明涉及萘酚，喹啉和异喹啉衍生的脲，它们是有效的VR1拮抗剂或激动剂，它们可用于治疗和预防哺乳动物的炎症和其它疼痛病症。

4. 发明申请

WO2006020225A1 ASSAY SYSTEMS AND METHODS FOR DETECTING MOLECULES THAT INTERACT WITH MEMBRANE CHANNELS 审中-公开
标题翻译：用于检测与膜通道相互作用的分子的测定系统和方法
公开(公告)号：WO2006020225A1
公开(公告)日：2006-02-23
申请号：PCT/US2005/025428
申请日：2005-07-19
申请人： JANSSEN PHARMACEUTICA N.V. , ZHANG, Sui-Po , CODD, Ellen E.
发明人： ZHANG, Sui-Po , CODD, Ellen E.
IPC分类号： G01N33/542
CPC分类号： G01N33/542 , G01N33/6872 , G01N2500/10
摘要： The invention provides an assay system for detecting a molecule that interacts with a membrane channel, the assay system including cell membranes including one or more membrane channels; support bodies including scintillant and a coupling agent that associates with the cell membrane; a ligand that is selected to bind the membrane channel, the ligand including a scintillant-activating label. According to the invention, association of the support bodies with the cell membrane and binding of the ligand to the membrane channel results in emission from the scintillant of the support bodies, and, in the presence of a test molecule that interacts with the membrane channel, the emission from the scintillant of the support bodies changes. Methods of identifying a molecule that interacts with a cell membrane channel are also described.
摘要翻译：本发明提供了一种用于检测与膜通道相互作用的分子的测定系统，该测定系统包括包含一个或多个膜通道的细胞膜; 支持体，包括闪烁体和与细胞膜缔合的偶联剂; 被选择以结合膜通道的配体，该配体包括闪烁体激活标记。根据本发明，支持体与细胞膜的结合以及配体与膜通道的结合导致来自支持体的闪烁体的发射，并且在与膜通道相互作用的测试分子的存在下，来自支撑体的闪烁体的发射变化。还描述了鉴定与细胞膜通道相互作用的分子的方法。

5. 发明申请

WO2005003131A1 TRICYCLIC DELTA OPIOID MODULATORS 审中-公开
标题翻译： TRICYCLIC DELTA OPIOID调制器
公开(公告)号：WO2005003131A1
公开(公告)日：2005-01-13
申请号：PCT/US2004/019911
申请日：2004-06-22
申请人： JANSSEN PHARMACEUTICA N.V. , CARSON, John, R. , CODD, Ellen , RAZLER, Christine, M. , WORKS, Andrea
发明人： CARSON, John, R. , CODD, Ellen , RAZLER, Christine, M. , WORKS, Andrea
IPC分类号： C07D471/08
CPC分类号： C07D405/04 , C07D405/14 , C07D409/14 , C07D471/08
摘要： The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
摘要翻译：本发明涉及Δ阿片样物质受体调节剂。更具体地，本发明涉及三环类阿片样物质调节剂。还描述了使用本发明的化合物治疗轻度至重度疼痛和各种疾病的药物和兽医组合物和方法。

6. 发明申请

WO2003097586A1 AMINOTETRALIN-DERIVED UREA MODULATORS OF VANILLOID VR1 RECEPTOR 审中-公开
标题翻译： VANILLOID VR1受体的氨基酸衍生的尿素调节剂
公开(公告)号：WO2003097586A1
公开(公告)日：2003-11-27
申请号：PCT/US2003/015254
申请日：2003-05-15
申请人： JANSSEN PHARMACEUTICA N.V. , CODD, Ellen , DAX, Scott, L. , JETTER, Michele , MCDONELL, Mark , MCNALLY, James, J. , YOUNGMAN, Mark
发明人： CODD, Ellen , DAX, Scott, L. , JETTER, Michele , MCDONELL, Mark , MCNALLY, James, J. , YOUNGMAN, Mark
IPC分类号： C07C275/26
CPC分类号： C07D213/40 , C07C275/26 , C07C275/28 , C07C275/32 , C07C335/14 , C07C2601/02 , C07C2602/10 , C07D215/38 , C07D217/02 , C07D217/08 , C07D217/22 , C07D217/24 , C07D233/64 , C07D237/28 , C07D239/74 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/32 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04
摘要： This invention is directed to vanilloid receptor VR1 ligands of formula (1). More particularly, this invention relates to β-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
摘要翻译：本发明涉及式（1）的香草素受体VR1配体。更具体地说，本发明涉及作为VR1的有效拮抗剂或激动剂的β-氨基四氢萘衍生的脲，其可用于治疗和预防哺乳动物的炎症和其它疼痛病症。

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