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公开(公告)号：EP1861360A1
公开(公告)日：2007-12-05
申请号：EP06738050.1
申请日：2006-03-13
发明人： BEAVERS, Lisa, Selsam , FINLEY, Don, Richard , STEVENS, Freddie, Craig , PICKARD, Richard, Todd , JESUDASON, Cynthia, Darshini , HIPSKIND, Philip, Arthur , GADSKI, Robert, Alan , TAKAKUWA, Takako
IPC分类号： C07D207/09 , C07D401/14 , A61K31/40 , A61K31/435 , A61P25/00
CPC分类号： C07D207/09 , C07D401/14
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 and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
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公开(公告)号：EP1444224B1
公开(公告)日：2006-05-03
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：EP1756051B1
公开(公告)日：2012-09-12
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
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4.发明授权
公开(公告)号：EP1805169B1
公开(公告)日：2008-12-24
申请号：EP05804419.9
申请日：2005-10-11
IPC分类号： C07D409/12 , C07D417/12 , C07D405/12 , C07D413/12 , A61K31/4025 , A61P25/00
CPC分类号： C07D417/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention provides novel compounds with histamine-H3 receptor antagonist or inverse agonist activity. In particular, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and intermediates and methods for making these compounds. The invention provides methods of using compounds and pharmaceutical compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
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公开(公告)号：EP1585731A2
公开(公告)日：2005-10-19
申请号：EP03749068.7
申请日：2003-09-12
发明人： BEAVERS, Lisa, Selsam , FINLEY, Don, Richard , GADSKI, Robert, Alan , HIPSKIND, Philip, Arthur , JESUDASON, Cynthia, Darshini , PICKARD, Richard, Todd , STEVENS, Freddie, Craig , SEIDAM ,Christopher ,Stephen
IPC分类号： C07D215/08 , C07D215/20 , C07D215/06 , C07D215/58 , C07D215/227 , C07D209/26 , C07D209/04 , C07D209/24 , C07D209/22 , A61K31/404 , A61K31/47 , A61P37/00
CPC分类号： C07D215/227 , C07D209/04 , C07D209/22 , C07D209/24 , C07D209/26 , C07D209/32 , C07D215/06 , C07D215/08 , C07D215/20 , C07D215/26 , C07D215/58 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06
摘要： The present invention discloses novel compounds of Formula ( I ) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist 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 them to treat obesity and other histamine H3 receptor-related diseases.
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公开(公告)号：EP1861360B1
公开(公告)日：2009-12-02
申请号：EP06738050.1
申请日：2006-03-13
发明人： BEAVERS, Lisa, Selsam , FINLEY, Don, Richard , GADSKI, Robert, Alan , HIPSKIND, Philip, Arthur , JESUDASON, Cynthia, Darshini , PICKARD, Richard, Todd , STEVENS, Freddie, Craig , TAKAKUWA, Takako
IPC分类号： C07D207/09 , C07D401/14 , A61K31/40 , A61K31/435 , A61P25/00
CPC分类号： C07D207/09 , C07D401/14
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 and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
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7.发明授权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：EP1786790B1
公开(公告)日：2009-06-03
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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8.发明授权INDOLE DERIVATIVES AS BETA-3 ADRENERGIC AGONISTS FOR THE TREATMENT OF TYPE 2 DIABETES 有权吲哚衍生物ASβ-3肾上腺素能激动剂用于治疗2型糖尿病
公开(公告)号：EP1421078B1
公开(公告)日：2006-09-27
申请号：EP02752178.0
申请日：2002-08-06
发明人： BASTIAN, Jolie, Anne , EVERS, Britta Lilly Research Laboratories Hamburg , FINLEY, Don, Richard , HE, John, Xiaoqiang , JESUDASON, Cynthia, Darshini , KARANJAWALA, Rushad, E. , RATZ, Andrew, Michael , ROCCO, Vincent, Patrick , RUEHTER, Gerd Lilly Research Laboratories Hamburg , SALL, Daniel, Jon , SCHOTTEN, Theo Lilly 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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9.发明公开
公开(公告)号：EP1805169A1
公开(公告)日：2007-07-11
申请号：EP05804419.9
申请日：2005-10-11
IPC分类号： C07D409/12 , C07D417/12 , C07D405/12 , C07D413/12 , A61K31/4025 , A61P25/00
CPC分类号： C07D417/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention provides novel compounds with histamine-H3 receptor antagonist or inverse agonist activity. In particular, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and intermediates and methods for making these compounds. The invention provides methods of using compounds and pharmaceutical compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
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公开(公告)号：EP1341759B1
公开(公告)日：2006-06-14
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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