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1. 发明申请

US20070155754A1 Histamine h3 receptor antagonists, preparation and therapeutic uses 失效
标题翻译：组胺h3受体拮抗剂，制剂和治疗用途
公开(公告)号：US20070155754A1
公开(公告)日：2007-07-05
申请号：US10598262
申请日：2005-02-22
申请人： Lisa Beavers , Robert Gadski , Philip Hipskind , Cynthia Jesudason , Karen Lobb , Richard Pickard , Craig Lindsley
发明人： Lisa Beavers , Robert Gadski , Philip Hipskind , Cynthia Jesudason , Karen Lobb , Richard Pickard , Craig Lindsley
IPC分类号： A61K31/496 , A61K31/454 , A61K31/4025 , C07D403/14
CPC分类号： C07D295/125 , C07D207/09 , C07D295/02 , C07D295/096 , C07D295/155 , C07D295/192 , C07D487/04
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.
摘要翻译：本发明公开了具有组胺H3受体拮抗剂活性的式I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使用它们治疗肥胖症和其他组胺H3受体相关疾病的方法。

2. 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。

3. 发明申请

US20080015235A1 Histamine H3 Receptor Inhibitors, Preparation and Therapeutic Uses 有权
标题翻译：组胺H3受体抑制剂，制备和治疗用途
公开(公告)号：US20080015235A1
公开(公告)日：2008-01-17
申请号：US11577388
申请日：2005-10-11
申请人： Cynthia Jesudason , Freddie Stevens
发明人： Cynthia Jesudason , Freddie Stevens
IPC分类号： C07D403/12 , A61K31/4025 , A61K31/422 , A61K31/4245 , C07D409/12 , C07D417/12 , C07D405/12 , A61K31/426 , A61P25/00
CPC分类号： C07D417/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof, 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：本发明公开了新颖的式I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，本发明公开了药物。包含式I化合物的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。

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

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。

6. 发明申请

US20070197604A1 Oxazole derivatives as histamine h3 receptor agents,preparation and therapeutic uses 有权
标题翻译：恶唑衍生物作为组胺h3受体剂，制备和治疗用途
公开(公告)号：US20070197604A1
公开(公告)日：2007-08-23
申请号：US11572283
申请日：2005-07-14
申请人： Lisa Beavers , Serge Boulet , Terry Finn , Robert Gadski , Willaim Hornback , Cynthia Jesudason , Richard Pickard , Freddie Stevens , Grant Vaught
发明人： Lisa Beavers , Serge Boulet , Terry Finn , Robert Gadski , Willaim Hornback , Cynthia Jesudason , Richard Pickard , Freddie Stevens , Grant Vaught
IPC分类号： A61K31/421 , A61K31/44 , C07D413/10
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.
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（I）的新型芳基恶唑化合物或其药学上可接受的盐，以及制备和使用这些化合物的方法。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这些组合物治疗肥胖症，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。式I（I）或其药学上可接受的盐，其中：m在每次出现时独立地为1,2或3，Z独立地表示碳（被氢或本文所示的任选取代基）或氮，条件是当Z为氮，然后R6不连接到Z; R 1和R 2独立地为 - （C 1 -C 7 -C 7）烷基（任选被一至三个卤素取代），或R 1和R 2以及与它们相连的氮形成氮杂环丁烷基环，吡咯烷基环或哌啶基环，其中如此形成的氮杂环丁烷基，吡咯烷基或哌啶基环可以任选地被R 5取代一至三次; R 6在每次出现时独立地为-H， - 卤素或-CH 3。

7. 发明申请

US20050054713A1 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：US20050054713A1
公开(公告)日：2005-03-10
申请号：US10970194
申请日：2004-10-21
申请人： Cynthia Jesudason , Daniel Sall , Freddie Stevens , John Werner
发明人： Cynthia Jesudason , Daniel Sall , Freddie Stevens , John Werner
IPC分类号： A61K31/403 , A61K31/404 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61P3/04 , A61P3/10 , A61P43/00 , C07B53/00 , C07D209/34 , C07D209/96 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D209/36
CPC分类号： C07D401/12 , C07D209/34 , C07D209/96 , C07D403/12 , C07D405/04 , C07D405/12
摘要： The present invention relates to a β3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is useful for treating Type II 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; 其可用于治疗II型糖尿病和/或肥胖症。

8. 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

9. 发明申请

US20060089347A1 Substituted azepines as histamine h3 receptor antagonists, preparation and therapeutic uses 审中-公开
标题翻译：取代的吖庚因作为组胺h3受体拮抗剂，制剂和治疗用途
公开(公告)号：US20060089347A1
公开(公告)日：2006-04-27
申请号：US10523071
申请日：2003-08-15
申请人： Robert Gadski , Phillip Hipskind , Cynthia Jesudason , Richard Pickard , Lisa Beavers , Christopher Sledem , Alay Singh
发明人： Robert Gadski , Phillip Hipskind , Cynthia Jesudason , Richard Pickard , Lisa Beavers , Christopher Sledem , Alay Singh
IPC分类号： A61K31/55 , C07D223/16
CPC分类号： C07D403/06 , C07D223/16
摘要： The present invention discloses novel substituted azepine compounds of Formula (I) or pharmaceutically acceptable salts thereof which have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such azepines as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases.
摘要翻译：本发明公开了具有选择性组胺-H 3受体拮抗剂活性的新颖的式（I）取代的吖庚因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，本发明公开了包含这种吖庚因的药物组合物以及使用它们治疗肥胖症和其他组胺H3受体相关疾病的方法。

10. 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。

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