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21. 发明授权

US6075040A Selective .beta..sub.3 adrenergic agonists 失效
标题翻译：选择性β3肾上腺素能激动剂
公开(公告)号：US6075040A
公开(公告)日：2000-06-13
申请号：US850562
申请日：1997-05-02
申请人： Michael Gregory Bell , Thomas Alan Crowell , Cynthia Darshini Jesudason , Donald Paul Matthews , John Hampton McDonald, III , David Andrew Neel , Christopher John Rito , Anthony John Shuker , Mark Alan Winter
发明人： Michael Gregory Bell , Thomas Alan Crowell , Cynthia Darshini Jesudason , Donald Paul Matthews , John Hampton McDonald, III , David Andrew Neel , Christopher John Rito , Anthony John Shuker , Mark Alan Winter
IPC分类号： A61K31/404 , A61K31/4192 , A61K31/4439 , C07D209/04 , C07D209/08 , C07D235/06 , C07D235/26 , C07D249/18 , C07D263/58 , C07D285/14 , C07D401/00 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/41 , A61K31/415 , C07D235/04 , C07D271/12
CPC分类号： C07D235/06 , A61K31/404 , A61K31/4192 , A61K31/4439 , C07D209/08 , C07D235/26 , C07D249/18 , C07D263/58 , C07D285/14 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formulas I and II: ##STR1##
摘要翻译：本发明在医药领域，特别是治疗II型糖尿病和肥胖症。更具体地，本发明涉及可用于治疗II型糖尿病和肥胖症的选择性β3肾上腺素能受体激动剂。本发明提供了治疗II型糖尿病的化合物和方法，包括向有需要的哺乳动物施用式I和II的化合物：

22. 发明授权

US07846950B2 Histamine H3 receptor inhibitors, preparation and therapeutic uses 有权
标题翻译：组胺H3受体抑制剂，制剂和治疗用途
公开(公告)号：US07846950B2
公开(公告)日：2010-12-07
申请号：US11577388
申请日：2005-10-11
申请人： Cynthia Darshini Jesudason , Freddie Craig Stevens
发明人： Cynthia Darshini Jesudason , Freddie Craig Stevens
IPC分类号： A61K31/422 , A61K31/4025 , A61K31/4245 , C07D417/12 , C07D405/12 , 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 deficiences, narcolepsy, and other histamine H3 receptor-related diseases.
摘要翻译：本发明提供具有组胺H3受体拮抗剂或反向激动剂活性的新型化合物。特别地，本发明提供式I化合物或其药学上可接受的盐，包含该化合物的药物组合物，使用这些化合物和组合物的治疗方法，以及制备这些化合物的中间体和方法。本发明提供了使用化合物和药物组合物治疗肥胖，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。

23. 发明授权

US07122680B2 3-Substituted oxindole β3 agonsists 失效
标题翻译： 3-取代的羟吲哚β3治疗师
公开(公告)号：US07122680B2
公开(公告)日：2006-10-17
申请号：US10970194
申请日：2004-10-21
申请人： Cynthia Darshini Jesudason , Daniel Jon Sall , Freddie Craig Stevens , John Arnold Werner
发明人： Cynthia Darshini Jesudason , Daniel Jon Sall , Freddie Craig Stevens , John Arnold Werner
IPC分类号： C07D209/04 , C07D209/32 , C07D401/12 , C07D237/02 , A61K31/44
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 N 3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。

24. 发明授权

US06265581B1 Selective &bgr;3 adrenergic agonists 失效
标题翻译：选择性β3肾上腺素激动剂
公开(公告)号：US06265581B1
公开(公告)日：2001-07-24
申请号：US09551184
申请日：2000-04-17
申请人： Michael Gregory Bell , Thomas Alan Crowell , Christine Ann Droste , Cynthia Darshini Jesudason , Donald Paul Matthews , John Hampton McDonald, III , David Andrew Neel , Christopher John Rito , Anthony John Shuker , Mark Alan Winter
发明人： Michael Gregory Bell , Thomas Alan Crowell , Christine Ann Droste , Cynthia Darshini Jesudason , Donald Paul Matthews , John Hampton McDonald, III , David Andrew Neel , Christopher John Rito , Anthony John Shuker , Mark Alan Winter
IPC分类号： C07D40100
CPC分类号： C07D235/06 , A61K31/404 , A61K31/4192 , A61K31/4439 , C07D209/08 , C07D235/26 , C07D249/18 , C07D263/58 , C07D285/14 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective &bgr;3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formulas I and II:
摘要翻译：本发明在医药领域，特别是治疗II型糖尿病和肥胖症。更具体地，本发明涉及可用于治疗II型糖尿病和肥胖症的选择性β3肾上腺素能受体激动剂。本发明提供了治疗II型糖尿病的化合物和方法，包括向有需要的哺乳动物施用式I和II的化合物：

25. 发明授权

US5977154A Selective .beta.3 adrenergic agonist 失效
标题翻译：选择性β3肾上腺素能激动剂
公开(公告)号：US5977154A
公开(公告)日：1999-11-02
申请号：US882931
申请日：1997-06-26
申请人： Michael Gregory Bell , Christine Ann Droste , Cynthia Darshini Jesudason , Christopher John Rito , Anthony John Shuker , Mark Alan Winter
发明人： Michael Gregory Bell , Christine Ann Droste , Cynthia Darshini Jesudason , Christopher John Rito , Anthony John Shuker , Mark Alan Winter
IPC分类号： A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/4192 , A61K31/42 , A61K31/423 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61K31/496 , A61K31/50 , A61K31/501 , A61K31/53 , A61K31/535 , A61K31/5355 , A61K31/537 , A61K31/5375 , A61K31/5377 , A61P3/00 , A61P3/10 , A61P43/00 , C07C235/46 , C07C255/54 , C07D209/08 , C07D213/63 , C07D235/06 , C07D235/08 , C07D235/26 , C07D249/18 , C07D257/04 , C07D263/56 , C07D263/58 , C07D285/14 , C07D295/18 , C07D333/34 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D413/10
CPC分类号： C07D209/08 , A61K31/404 , A61K31/4192 , C07D235/06 , C07D235/26 , C07D249/18 , C07D263/58 , C07D285/14 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formulas I and II: ##STR1##
摘要翻译：本发明在医药领域，特别是治疗II型糖尿病和肥胖症。更具体地，本发明涉及可用于治疗II型糖尿病和肥胖症的选择性β3肾上腺素能受体激动剂。本发明提供了治疗II型糖尿病的化合物和方法，包括向有需要的哺乳动物施用式I和II的化合物：

26. 发明授权

US5840738A Selective .beta.-3 adrenergic agonists 失效
标题翻译：选择性β-3肾上腺素能激动剂
公开(公告)号：US5840738A
公开(公告)日：1998-11-24
申请号：US882623
申请日：1997-06-25
申请人： Michael Gregory Bell , Thomas Alan Crowell , Christine Ann Droste , Cynthia Darshini Jesudason , Donald Paul Matthews , John Hampton McDonald, III , David Andrew Neel , Christopher John Rito , Anthony John Shuker , Mark Alan Winter
发明人： Michael Gregory Bell , Thomas Alan Crowell , Christine Ann Droste , Cynthia Darshini Jesudason , Donald Paul Matthews , John Hampton McDonald, III , David Andrew Neel , Christopher John Rito , Anthony John Shuker , Mark Alan Winter
IPC分类号： A61K31/404 , A61K31/4192 , A61K31/4439 , C07D209/04 , C07D209/08 , C07D235/06 , C07D235/26 , C07D249/18 , C07D263/58 , C07D285/14 , C07D401/00 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/415
CPC分类号： C07D235/06 , A61K31/404 , A61K31/4192 , A61K31/4439 , C07D209/08 , C07D235/26 , C07D249/18 , C07D263/58 , C07D285/14 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formulas I and II: ##STR1##
摘要翻译：本发明在医药领域，特别是治疗II型糖尿病和肥胖症。更具体地，本发明涉及可用于治疗II型糖尿病和肥胖症的选择性β3肾上腺素能受体激动剂。本发明提供了治疗II型糖尿病的化合物和方法，包括向有需要的哺乳动物施用式I和II的化合物：

27. 发明授权

US07214697B2 2-Oxo-benzimidazolyl substituted ethanolamine derivatives and their use as β3 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：US07214697B2
公开(公告)日：2007-05-08
申请号：US11228620
申请日：2005-09-16
申请人： Cynthia Darshini Jesudason , Don Richard Finley
发明人： Cynthia Darshini Jesudason , Don Richard Finley
IPC分类号： A61K31/4184 , C07D213/82
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, CO2 R6, CONR6R6, NR6COR7, NR6R6, OR6, SR6, SOR7, S02R7 or SO2NR6R6; R1a is H, halo or C1–C6 alkyl; R2 is H 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, NHSO2, SO2NH 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 diabetes 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，CO 2 C 1 -C 6烷基，C 1 -C 4烷基，C 1 -C 4烷基， R 6，C 6，C 6，R 6，R 6，R 6，R 6， 6，6，6或6，SR 6，SOR 7，S 0，或者是SO 2，NR 6，S 6，S 6， R 1a是H，卤素或C 1 -C 6烷基; R 2是H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/或肥胖症

28. 发明授权

US07087635B2 3-substituted oxindole β3 agonists 失效
标题翻译： 3-取代羟吲哚β3激动剂
公开(公告)号：US07087635B2
公开(公告)日：2006-08-08
申请号：US11082106
申请日：2005-03-16
申请人： Daniel Jon Sall , Jolie Anne Bastian , Cynthia Darshini Jesudason , Don Richard Finley , Freddie Craig Stevens , Vincent Patrick Rocco , Patrick Gianpietro Spinazze , John Xiaoqiang He , John Arnold Werner , William George Trankle , Andrew Michael Ratz , Theo Schotten , Gerd Reuhter
发明人： Daniel Jon Sall , Jolie Anne Bastian , Cynthia Darshini Jesudason , Don Richard Finley , Freddie Craig Stevens , Vincent Patrick Rocco , Patrick Gianpietro Spinazze , John Xiaoqiang He , John Arnold Werner , William George Trankle , Andrew Michael Ratz , Theo Schotten , Gerd Reuhter
IPC分类号： A61K31/40 , A61K31/38 , C07D209/54 , C07D317/08 , C07D409/00
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。

29. 发明授权

US06911463B2 3-substituted oxindole β-3 agonists 失效
标题翻译： 3-取代羟吲哚β-3激动剂
公开(公告)号：US06911463B2
公开(公告)日：2005-06-28
申请号：US10486508
申请日：2002-08-06
申请人： Daniel Jon Sall , Jolie Anne Bastian , Cynthia Darshini Jesudason , Theo Schotten , Gerd Reuhter , Don Richard Finley , Freddie Craig Stevens , Vincent Patrick Rocco , Patrick Gianpietro Spinazze , John Xiaoqiang He , John Arnold Werner , William George Trankle , Andrew Michael Ratz
发明人： Daniel Jon Sall , Jolie Anne Bastian , Cynthia Darshini Jesudason , Theo Schotten , Gerd Reuhter , Don Richard Finley , Freddie Craig Stevens , Vincent Patrick Rocco , Patrick Gianpietro Spinazze , John Xiaoqiang He , John Arnold Werner , William George Trankle , Andrew Michael Ratz
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 , A61K31/4035 , A61K31/425 , C07D209/44 , C07D209/54
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/或肥胖症。

30. 发明授权

US06730792B2 &bgr;3 adrenergic agonists 有权
标题翻译： β3肾上腺素能激动剂
公开(公告)号：US06730792B2
公开(公告)日：2004-05-04
申请号：US10311112
申请日：2002-12-13
申请人： Britta Evers , Cynthia Darshini Jesudason , Rushad Eruch Karanjawala , David Michael Remick , Daniel Jon Sall , Miles Goodman Siegel , Wolfgang Stenzel , Russell Dean Stucky , John Arnold Werner
发明人： Britta Evers , Cynthia Darshini Jesudason , Rushad Eruch Karanjawala , David Michael Remick , Daniel Jon Sall , Miles Goodman Siegel , Wolfgang Stenzel , Russell Dean Stucky , John Arnold Werner
IPC分类号： C07D40104
CPC分类号： C07D207/333 , A61K9/0014 , A61K9/0019 , A61K9/0031 , A61K9/0043 , A61K9/0056 , A61K9/0073 , A61K9/0095 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/107 , A61K9/12 , A61K9/2054 , C07D213/30 , C07D213/82 , C07D213/84 , C07D261/08 , C07D277/24 , C07D333/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to a &bgr;3 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 II diabetes and/or obesity. The compound can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compound can be used to reduced neurogenic inflammation or as an antidepressant agent. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.
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II型糖尿病和/或肥胖症。该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠蠕动。此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。还公开了使用该化合物治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠蠕动的组合物和方法。

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