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1. 发明申请

US20050080110A1 Beta 3 adrenergic agonists 失效
标题翻译： β3肾上腺素能激动剂
公开(公告)号：US20050080110A1
公开(公告)日：2005-04-14
申请号：US10486867
申请日：2002-08-06
申请人： Daniel Sall , Jolie Bastian , Rushad Karanjawala , Cynthia Jesudason , Theo Schotten , Britta Evers , Gerd Reuhter , Don Finley , Freddie Stevens , Vincent Rocco , Patrick Spinazze , John He , John Werner , William Trankle , Andrew Ratz
发明人： Daniel Sall , Jolie Bastian , Rushad Karanjawala , Cynthia Jesudason , Theo Schotten , Britta Evers , Gerd Reuhter , Don Finley , Freddie Stevens , Vincent Rocco , Patrick Spinazze , John He , John Werner , William Trankle , Andrew Ratz
IPC分类号： A61K31/381 , A61K31/4045 , A61K31/41 , A61K31/4178 , A61K31/4196 , A61K31/42 , A61K31/422 , A61K31/425 , A61K31/427 , A61K31/433 , A61K31/4436 , A61K31/4439 , A61K31/506 , A61P3/04 , A61P3/10 , A61P43/00 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D49/02 , C07D41/02 , C07D43/02
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.
摘要翻译：本发明涉及式（I）的β3肾上腺素能受体激动剂; 或其药学盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于例如治疗2型糖尿病和/或肥胖症。

2. 发明申请

US20050159473A1 3-Substituted oxindole beta3 agonists 失效
标题翻译： 3-取代的羟吲哚β3激动剂
公开(公告)号：US20050159473A1
公开(公告)日：2005-07-21
申请号：US11082106
申请日：2005-03-16
申请人： Daniel Sall , Jolie Bastian , Cynthia Jesudason , Don Finley , Freddie Stevens , Vincent Rocco , Patrick Spinazze , John He , John Werner , William Trankle , Andrew Ratz , Theo Schotten , Gerd Reuhter
发明人： Daniel Sall , Jolie Bastian , Cynthia Jesudason , Don Finley , Freddie Stevens , Vincent Rocco , Patrick Spinazze , John He , John Werner , William Trankle , Andrew Ratz , Theo Schotten , Gerd Reuhter
IPC分类号： A01N41/12 , A61K31/4045 , A61K31/4178 , A61K31/4196 , A61K31/427 , A61K31/4439 , A61K31/497 , A61P3/04 , A61P3/10 , C07D209/34 , C07D209/96 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/14 , C07D521/00 , A61K31/404 , C07D43/02
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.
摘要翻译：本发明涉及式I的β3肾上腺素能受体激动剂：或其药用盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于治疗2型糖尿病和/或肥胖症。

3. 发明申请

US20060167046A1 Histamine h3 receptor antagonists, preparation and therapeutic uses 审中-公开
标题翻译：组胺h3受体拮抗剂，制剂和治疗用途
公开(公告)号：US20060167046A1
公开(公告)日：2006-07-27
申请号：US10525315
申请日：2003-09-12
申请人： Lisa Beavers , Don Finley , Robert Gadski , Philip Hipskind , Cynthia Jesudason , Richard Pickard , Freddie Stevens
发明人： Lisa Beavers , Don Finley , Robert Gadski , Philip Hipskind , Cynthia Jesudason , Richard Pickard , Freddie Stevens
IPC分类号： A61K31/4709 , A61K31/454 , A61K31/405 , C07D401/02 , C07D403/02
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-II3 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 or using them to treat obesity and other histamine II3 receptor-related diseases.
摘要翻译：本发明公开了具有组胺-II3受体拮抗剂活性的式（I）的新化合物或其药学上可接受的盐以及其制备方法。在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物，以及用于治疗肥胖症和其他组胺II3受体相关疾病的方法或用它们。

4. 发明申请

US20060014963A1 2-Oxo-benzimidazolyl substituted ethanolamine derivatives and their use as beta3 agonists 失效
标题翻译： 2-氧代苯并咪唑基取代的乙醇胺衍生物及其作为β3激动剂的用途
公开(公告)号：US20060014963A1
公开(公告)日：2006-01-19
申请号：US11228620
申请日：2005-09-16
申请人： Cynthia Jesudason , Don Finley
发明人： Cynthia Jesudason , Don Finley
IPC分类号： A61K31/4184 , C07C235/12
CPC分类号： C07D213/82 , C07C235/46 , C07C2601/02 , C07C2601/08 , C07D235/26 , C07D401/12
摘要： The present invention relates to a β3 adrenergic receptor agonist of formula (I), wherein R is C3-C8 alkyl or (C3-C7 cycloalkyl)C1-C5 alk-di-yl: R1 is H, CN, halo; C1-C6 alkyl, C1-C4 haloalkyl, C02 R6, CONR6R6, NR6COR7, NR6R6, OR6, SR6, SOR7. S02R7 or S02NR6R6; R1a is H, halo or C1-C6 aLkyl; R2 is Hi or C1-C6 alkyl; R3 and R4 are independently H or C1-C6 alkyl R5 is hydrogen, optionally substituted phenyl or optionally substituted heterocycle; X is absent or is OCH2 or SCH2; X1 is absent or C1-C5 alk-di-yl; and X2 is absent or is O, S, NH, NHS02, S02NH or CH2; or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 deabetes and/or obesity
摘要翻译：本发明涉及式（I）的β3 N 3肾上腺素能受体激动剂，其中R是C 3 -C 8烷基或（C C 3 -C 3 - 环烷基）C 1 -C 5烷基 - 二基：R 1 H，CN，卤素; C 1 -C 6烷基，C 1 -C 4卤代烷基，C 0 2 或者S0＆lt; 2＆lt; 6＆lt; 6＆gt; 6＆lt; 6＆gt; R 1a是H，卤素或C 1 -C 6 -C 1-4烷基; R 2是H 1或C 1 -C 6烷基; R 3和R 4独立地为H或C 1 -C 6烷基R 5， SUP>是氢，任选取代的苯基或任选取代的杂环; X不存在或是OCH 2或SCH 2; X 1不存在或C 1 -C 5烷基 - 二基; 和X 2不存在，或者是O，S，NH，NHSO 2，SO 2 NH或CH 2， ; 或其药学盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于治疗2型糖尿病和/或肥胖

5. 发明申请

US20070208024A1 HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES 有权
标题翻译：组胺H3受体代谢物，制剂和治疗用途
公开(公告)号：US20070208024A1
公开(公告)日：2007-09-06
申请号：US10599488
申请日：2005-03-25
申请人： Lisa Beavers , Don Finley , Terry Finn , Robert Gadski , Philip Hipskind , William Hornback , Cynthia Jesudason , Richard Pickard , Takako Takakuwa , Grant Vaught
发明人： Lisa Beavers , Don Finley , Terry Finn , Robert Gadski , Philip Hipskind , William Hornback , Cynthia Jesudason , Richard Pickard , Takako Takakuwa , Grant Vaught
IPC分类号： A61K31/495 , A61K31/4025 , C07D207/04 , C07D401/08 , C07D247/00 , A61K31/44
CPC分类号： C07D207/09 , C07D401/10 , C07D403/10 , C07D405/10 , C07D413/10 , C07D471/04
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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
摘要翻译：本发明公开了具有组胺H3受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法

6. 发明申请

US20050014741A1 2-oxo-benzimidazolyl substituted ethanolamine derivatives and their use as beta3 agonists 失效
标题翻译： 2-氧代 - 苯并咪唑基取代的乙醇胺衍生物及其作为β3激动剂的用途
公开(公告)号：US20050014741A1
公开(公告)日：2005-01-20
申请号：US10498261
申请日：2002-12-24
申请人： Cynthia Darshini , Don Finley
发明人： Cynthia Darshini , Don Finley
IPC分类号： A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/55 , A61P1/04 , A61P1/12 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/14 , A61P13/08 , A61P13/10 , A61P15/00 , A61P25/24 , A61P27/02 , A61P27/06 , A61P29/00 , A61P43/00 , C07C235/46 , C07D213/82 , C07D235/26 , C07D401/12 , C07
CPC分类号： C07D213/82 , C07C235/46 , C07C2601/02 , C07C2601/08 , C07D235/26 , C07D401/12
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 for treating Type 2 diabetes and/or obesity.
摘要翻译：本发明涉及式I的β3肾上腺素能受体激动剂：或其药用盐; 其能够增加细胞中的脂肪分解和能量消耗，因此可用于治疗2型糖尿病和/或肥胖症。

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