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公开(公告)号：EP1444224A2
公开(公告)日：2004-08-11
申请号：EP02748081.3
申请日：2002-08-06
发明人： BASTIAN, Jolie, Anne , FINLEY, Don, Richard , HE, John, Xiaoqiang , JESUDASON, Cynthia, Darshini , RATZ, Andrew, Michael , ROCCO, Vincent, Patrick , RUEHTER, Gerd,Lilly Research Laboratories Hamburg , SALL, Daniel, Jon , SCHOTTEN, Theo,Lilly Research Labs. Hamburg , SPINAZZE, Patrick, Gianpietro , STEVENS, Freddie, Craig , TRANKLE, William, George , WERNER, John, Arnold
IPC分类号： C07D403/12 , A61K31/404 , A61P3/04 , C07D409/14 , C07D401/14 , C07D409/12 , C07D405/12 , C07D209/34 , C07D403/14 , C07D417/14
CPC分类号： C07D231/12 , C07D209/34 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/14
摘要： The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.
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公开(公告)号：EP1204659B1
公开(公告)日：2003-11-26
申请号：EP00955245.6
申请日：2000-07-21
发明人： BRINER, Karin , BURKHART, Joseph, Paul , BURKHOLDER, Timothy, Paul , CUNNINGHAM, Brian, Eugene , FISHER, Matthew, Joseph , GRITTON, William, Harlan , JESUDASON, Cynthia, Darshini , MILLER, Shawn, Christopher , MULLANEY, Jeffrey, Thomas , REINHARD, Matthew, Robert , ROTHHAAR, Roger, Ryan , STEVENS, Freddie, Craig , WINNEROSKI, Leonard, Larry, Jr. , XU, Yanping , XU, Yao-Chang
IPC分类号： C07D405/04 , A61K31/4525 , A61P3/04 , A61P25/24
CPC分类号： C07D405/04
摘要： The present invention provides serotonergic benzofurans of Formula (I): where A, R, R?1, R2, R3, and R4¿ are as described in the specification.
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13.发明公开OXAZOLE DERIVATIVES AS HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES 有权恶唑，组胺H3受体具有活性，其制备方法和治疗用途
公开(公告)号：EP1786790A1
公开(公告)日：2007-05-23
申请号：EP05773290.1
申请日：2005-07-14
发明人： BEAVERS, Lisa, Selsam , BOULET, Serge, Louis , FINN, Terry, Patrick,Addex Pharmaceuticals SA , GADSKI, Robert, Alan , HORNBACK, William, Joseph , JESUDASON, Cynthia, Darshini , PICKARD, Richard, Todd , STEVENS, Freddie, Craig , VAUGHT, Grant, Matthews
IPC分类号： C07D263/32 , C07D333/38 , C07D277/22 , A61K31/422 , A61P25/00
CPC分类号： C07D413/14 , C07D263/32 , C07D413/06 , C07D417/14
摘要： The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently -(C1-C7) alkyl(optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence -H, -halogen, or -CH3.
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公开(公告)号：EP1756051A1
公开(公告)日：2007-02-28
申请号：EP05754884.4
申请日：2005-05-24
发明人： BEAVERS, Lisa, Selsam , GADSKI, Robert, Alan , JESUDASON, Cynthia, Darshini , PICKARD, Richard, Todd , STEVENS, Freddie, Craig
IPC分类号： C07D207/09 , C07D401/12 , C07D403/12 , A61K31/4025 , A61P3/04 , A61P25/00
CPC分类号： C07D207/09 , C07D401/12 , C07D403/12 , Y02E60/36
摘要： The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
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公开(公告)号：EP1421078A1
公开(公告)日：2004-05-26
申请号：EP02752178.0
申请日：2002-08-06
发明人： BASTIAN, Jolie, Anne , EVERS, BrittaLilly Research Laboratories Hamburg , FINLEY, Don, Richard , HE, John, Xiaoqiang , JESUDASON, Cynthia, Darshini , KARANJAWALA, Rushad, E. , RATZ, Andrew, Michael , ROCCO, Vincent, Patrick , RUEHTER, GerdLilly Research Laboratories Hamburg , SALL, Daniel, Jon , SCHOTTEN, TheoLilly Research Laboratories Hamburg , SPINAZZE, Patrick, Gianpietro , STEVENS, Freddie, Craig , TRANKLE, William, George , WERNER, John, Arnold
IPC分类号： C07D403/12 , C07D409/12 , C07D413/12 , C07D409/14 , C07D417/12 , A61P3/04 , A61P3/10 , A61K31/41 , A61K31/38
CPC分类号： C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g., for treating Type 2 diabetes and/or obesity.
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公开(公告)号：EP1341759A2
公开(公告)日：2003-09-10
申请号：EP01985160.9
申请日：2001-10-26
发明人： JESUDASON, Cynthia, Darshini , SALL, Daniel, Jon , STEVENS, Freddie, Craig , WERNER, John, Arnold
IPC分类号： C07D209/34
CPC分类号： C07D401/12 , C07D209/34 , C07D209/96 , C07D403/12 , C07D405/04 , C07D405/12
摘要： The present invention relates to a β;3 adrenergic receptor agonist of formula I: (I);or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.
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公开(公告)号：EP1204659A2
公开(公告)日：2002-05-15
申请号：EP00955245.6
申请日：2000-07-21
发明人： BRINER, Karin , BURKHART, Joseph, Paul , BURKHOLDER, Timothy, Paul , CUNNINGHAM, Brian, Eugene , FISHER, Matthew, Joseph , GRITTON, William, Harlan , JESUDASON, Cynthia, Darshini , MILLER, Shawn, Christopher , MULLANEY, Jeffrey, Thomas , REINHARD, Matthew, Robert , ROTHHAAR, Roger, Ryan , STEVENS, Freddie, Craig , WINNEROSKI, Leonard, Larry, Jr. , XU, Yanping , XU, Yao-Chang
IPC分类号： C07D405/04 , A61K31/4525 , A61P3/04 , A61P25/24
CPC分类号： C07D405/04
摘要： The present invention provides serotonergic benzofurans of Formula (I): where A, R, R?1, R2, R3, and R4¿ are as described in the specification.
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