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1. 发明授权

US09260391B2 Hypoglycemic dihydropyridones 有权
标题翻译：低血糖二氢吡啶酮
公开(公告)号：US09260391B2
公开(公告)日：2016-02-16
申请号：US13058142
申请日：2009-08-07
申请人： Yuli Xie , Shixian Deng , Donald W. Landry , Paul Harris , Antonella Maffei
发明人： Yuli Xie , Shixian Deng , Donald W. Landry , Paul Harris , Antonella Maffei
IPC分类号： A61K31/45 , A61K31/351 , C07D211/74 , C07D309/30 , C07D211/94 , C07D211/76 , C07D211/88 , C07D309/32 , C07D471/04
CPC分类号： C07D211/94 , C07D211/76 , C07D211/88 , C07D309/32 , C07D471/04
摘要： The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.
摘要翻译：本发明尤其提供式I化合物：其中取代基名称在说明书中指出。本发明还提供了包含式I化合物的药物组合物，以及通过施用有效量的式I化合物来治疗或预防患者中的糖尿病或高血糖并使受试者血糖水平正常化的方法。

2. 发明申请

US20110294800A1 HYPOGLYCEMIC DIHYDROPYRIDONES 有权
标题翻译：高分子二氢吡啶
公开(公告)号：US20110294800A1
公开(公告)日：2011-12-01
申请号：US13058142
申请日：2009-08-07
申请人： Yuli Xie , Shixian Deng , Donald W. Landry , Paul Harris , Antonella Maffei
发明人： Yuli Xie , Shixian Deng , Donald W. Landry , Paul Harris , Antonella Maffei
IPC分类号： A61K31/4418 , C07D211/46 , C07D455/06 , C07D413/14 , C07D309/32 , A61P3/08 , A61K31/451 , A61K31/473 , A61K31/5377 , A61K31/366 , A61P3/10 , C07D211/86 , C07D211/76
CPC分类号： C07D211/94 , C07D211/76 , C07D211/88 , C07D309/32 , C07D471/04
摘要： The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.
摘要翻译：本发明尤其提供式I化合物：其中取代基名称在说明书中指出。本发明还提供了包含式I化合物的药物组合物，以及通过施用有效量的式I化合物来治疗或预防患者中的糖尿病或高血糖并使受试者血糖水平正常化的方法。

3. 发明授权

US09012471B2 Glucose metabolism modulating compounds 有权
标题翻译：葡萄糖代谢调节化合物
公开(公告)号：US09012471B2
公开(公告)日：2015-04-21
申请号：US12937177
申请日：2009-04-10
申请人： Paul Harris , Antonella Maffei , Yuli Xie , Donald Landry
发明人： Paul Harris , Antonella Maffei , Yuli Xie , Donald Landry
IPC分类号： A61K31/4375 , C07D455/06 , C07D211/86
CPC分类号： C07D211/88 , C07D211/46 , C07D211/86 , C07D471/04
摘要： The present invention provides, inter alia, dihydropyridone compounds and compositions, including analogs of a vesicular monoamine transporter type 2 (VMAT2) antagonist. The present invention also provides methods of using such compounds/analogs for modulating glucose levels, and/or preventing, treating, or ameliorating the effects of diabetes and hyper-glycemia.
摘要翻译：本发明尤其提供二氢吡啶酮化合物和组合物，包括囊泡单胺转运蛋白2型（VMAT2）拮抗剂的类似物。本发明还提供了使用这些化合物/类似物来调节葡萄糖水平和/或预防，治疗或改善糖尿病和高血糖症的作用的方法。

4. 发明申请

US20110118300A1 GLUCOSE METABOLISM MODULATING COMPOUNDS 有权
标题翻译：葡萄糖代谢调节化合物
公开(公告)号：US20110118300A1
公开(公告)日：2011-05-19
申请号：US12937177
申请日：2009-04-10
申请人： Paul Harris , Antonella Maffei , Yuli Xie , Donald Landry
发明人： Paul Harris , Antonella Maffei , Yuli Xie , Donald Landry
IPC分类号： A61K31/4375 , C07D455/06 , C07D213/69 , C07D211/74 , A61K31/4412 , A61K31/44 , A61P3/10
CPC分类号： C07D211/88 , C07D211/46 , C07D211/86 , C07D471/04
摘要： The present invention provides, inter alia, dihydropyridone compounds and compositions, including analogs of a vesicular monoamine transporter type 2 (VMAT2) antagonist. The present invention also provides methods of using such compounds/analogs for modulating glucose levels, and/or preventing, treating, or ameliorating the effects of diabetes and hyper-glycemia.
摘要翻译：本发明尤其提供二氢吡啶酮化合物和组合物，包括囊泡单胺转运蛋白2型（VMAT2）拮抗剂的类似物。本发明还提供了使用这些化合物/类似物来调节葡萄糖水平和/或预防，治疗或改善糖尿病和高血糖症的作用的方法。

5. 发明申请

US20100204258A1 METHODS AND COMPOSITIONS FOR MODULATING INSULIN SECRETION AND GLUCOSE METABOLISM 审中-公开
标题翻译：用于调节胰岛素分泌和葡萄糖代谢的方法和组合物
公开(公告)号：US20100204258A1
公开(公告)日：2010-08-12
申请号：US12450100
申请日：2008-03-12
申请人： Paul Harris , Yuli Xie , Donald Landry , Shi-Xian Deng , Antonella Maffei
发明人： Paul Harris , Yuli Xie , Donald Landry , Shi-Xian Deng , Antonella Maffei
IPC分类号： A61K31/4375 , A61K31/137 , A61P5/48 , A61P3/10
CPC分类号： A61K31/473 , A61K31/00 , A61K31/05 , A61K31/4741 , A61K31/4745 , A61K31/475
摘要： The present invention relates to methods and compositions for treating or ameliorating the effects of diabetes. In addition, the present invention relates to methods and compositions for treating or preventing hyperglycemia, as well as modulating monoamine levels, islet β-cell insulin secretion, insulin and/or glucagon levels in a patient. In certain preferred embodiments, such methods include administering to a patient an effective amount of a vesicular monoamine transporter type 2 (VMAT2) antagonist, such as tetrabenazine (TBZ), dihydrotetrabenazine (DTBZ), tetrahydroberberine (THB), reserpine, emetine, Compound 6, or enantiomers, optical isomers, diastereomers, N-oxides, crystalline forms, hydrates, metabolites or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及用于治疗或改善糖尿病的作用的方法和组合物。此外，本发明涉及用于治疗或预防高血糖的方法和组合物，以及调节患者体内单胺水平，胰岛素和细胞胰岛素分泌，胰岛素和/或胰高血糖素水平。在某些优选的实施方案中，这些方法包括向患者施用有效量的2型（VMAT2）囊泡单胺转运蛋白拮抗剂，如丁苯那嗪（TBZ），二氢丁苯那嗪（DTBZ），四氢小檗碱（THB），利血平，，或对映体，旋光异构体，非对映异构体，N-氧化物，结晶形式，水合物，代谢物或药学上可接受的盐。

6. 发明申请

US20090202428A1 Use of Dtbz for Imaging Endocrine Pancreas and Beta Cell Mass In Type 1 Diabetes 审中-公开
标题翻译：在1型糖尿病中使用Dtbz成像内分泌胰腺和β细胞
公开(公告)号：US20090202428A1
公开(公告)日：2009-08-13
申请号：US11988040
申请日：2006-06-21
申请人： Paul Harris , Antonella Maffei , Ronald Van Heertum
发明人： Paul Harris , Antonella Maffei , Ronald Van Heertum
IPC分类号： A61K51/00
CPC分类号： A61K51/0455
摘要： The present invention provides non-invasive methods for determining the beta cell mass in the pancreas of a subject by administering to the subject an effective amount of a vesicular monoamine transporter type 2 (VMAT2)-specific radioligand; obtaining at least one computerized image of at least a portion of the pancreas of the subject; and quantitatively analyzing the computerized image in order to determine the beta cell mass in the pancreas of the subject. The present invention additionally provides methods for diagnosing a metabolic neuroendocrine disorder in a subject including insulinoma, diabetes and preclinical diabetes, as well as methods for determining the efficacy of treatment for a metabolic disorder. The present invention further provides methods for assessing the prognosis of a subject at risk for developing diabetes, and methods for managing the treatment or prevention of diabetes. The present invention also provides kits for use in determining the beta cell mass in the pancreas of a subject, as well as diagnosing metabolic or neuroendocrine disorders in a subject.
摘要翻译：本发明提供了通过向受试者施用有效量的2型（VMAT2）特异性囊泡单体转运蛋白来确定受试者胰腺中的β细胞团的非侵入性方法; 获得所述受试者的胰脏的至少一部分的至少一个计算机化图像; 并定量分析计算机化图像，以确定受试者胰腺中的β细胞量。本发明另外提供了用于诊断包括胰岛素瘤，糖尿病和临床前糖尿病的受试者中的代谢神经内分泌障碍的方法以及用于确定治疗代谢紊乱的功效的方法。本发明还提供了评估患有糖尿病风险的受试者的预后的方法，以及用于治疗或预防糖尿病的方法。本发明还提供了用于确定受试者胰腺中的β细胞群以及诊断受试者中代谢或神经内分泌障碍的试剂盒。

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