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1. 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。

2. 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。

3. 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

4. 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。

5. 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。

6. 发明授权

US5861573A Dividing bullet with weakened longitudnal seam for separating into halves upon impact with target 失效
标题翻译：分割子弹与削弱的纵向缝在目标撞击时分为两半
公开(公告)号：US5861573A
公开(公告)日：1999-01-19
申请号：US829206
申请日：1997-03-31
申请人： Richard Pickard
发明人： Richard Pickard
IPC分类号： F42B12/34
CPC分类号： F42B12/34
摘要： A dividing bullet includes a projectile body having a longitudinal mid-plane and a pair of projectile halves. The halves are disposed on opposite sides of the longitudinal mid-plane and substantially symmetrical in relation to one another and to a longitudinal central axis of the projectile body. The dividing bullet also includes a seam extending through the projectile body formed between the halves along the longitudinal mid-plane of the projectile body. The halves are joined to one another along the seam by a joint that is weaker in strength than the material making up the pair of halves of the projectile body such that the projectile body will separate at the seam along the longitudinal mid-plane into the halves upon impact with a target.
摘要翻译：分割子弹包括具有纵向中间平面和一对抛射体半部的射弹体。半部设置在纵向中间平面的相对侧上，并且相对于彼此和射弹体的纵向中心轴线基本对称。分割子弹还包括沿着射弹体的纵向中间平面在两半之间形成的射弹体延伸的接缝。一半的接缝通过一个接合部彼此接合，该接头的强度弱于构成射弹体的一对半部分的材料，使得射弹体将沿着纵向中间平面的接缝分离成两半与目标的冲击。

7. 发明授权

US5801324A Dividing bullet having longitudinally joined jacketed projectile segments that separate upon target impact 失效
标题翻译：具有纵向连接的夹套弹丸的分割子弹，其在目标冲击时分离
公开(公告)号：US5801324A
公开(公告)日：1998-09-01
申请号：US831458
申请日：1997-03-31
申请人： Richard Pickard
发明人： Richard Pickard
IPC分类号： F42B12/34
CPC分类号： F42B12/34
摘要： A dividing bullet includes a projectile body and a seam through the projectile body. The projectile body has a longitudinal central axis and a plurality of individually jacketed longitudinally extending segments. Each segment has an inner core of a first material and outer jacket of a second material substantially encasing the inner core of the first material. The plurality of jacketed segments are symmetrically disposed about the longitudinal central axis. The seam extends through the projectile body between the individually jacketed segments thereof. The individually jacketed segments are joined together at the seam by a joint that is weaker in strength than the second material making up the outer jacket of each of the jacketed segments such that the projectile body will separate at the seam into the jacketed segments upon impact with a target. The second material of the outer jacket of each of the jacketed segments is greater in strength than the first material of the inner core thereof. The plurality of jacketed segments can be two, three or four in number.
摘要翻译：分裂的子弹包括射弹体和通过射弹体的接缝。射弹体具有纵向中心轴线和多个单独夹套的纵向延伸段。每个段具有第一材料的内芯和基本上包围第一材料的内芯的第二材料的外护套。多个夹套段围绕纵向中心轴对称设置。接缝在其单独夹套的段之间延伸穿过射弹体。单个夹套的节段在接缝处通过一个接头弱于与构成每个夹套段的外护套的第二材料相比较弱的接头，使得射弹体在撞击时将在接缝处分离成夹套段，一个目标。每个夹套段的外护套的第二材料的强度比其内芯的第一材料强。多个夹套的段可以是两个，三个或四个。

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