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1. 发明授权

US08278442B2 Bicyclic aryl and heteroaryl compounds for the treatment of metabolic disorders 失效
标题翻译：用于治疗代谢紊乱的双环芳基和杂芳基化合物
公开(公告)号：US08278442B2
公开(公告)日：2012-10-02
申请号：US12601100
申请日：2008-05-22
申请人： Jason Bloxham , Stuart Edward Bradley , Tom Banksia Dupree , Peter Timothy Fry , Patrick Eric Hanrahan , Thomas Martin Krulle , Martin James Procter , Colin Peter Sambrook-Smith , Karen Lesley Schofield , Donald Smyth , Alan John Stewart
发明人： Jason Bloxham , Stuart Edward Bradley , Tom Banksia Dupree , Peter Timothy Fry , Patrick Eric Hanrahan , Thomas Martin Krulle , Martin James Procter , Colin Peter Sambrook-Smith , Karen Lesley Schofield , Donald Smyth , Alan John Stewart
IPC分类号： C07D213/84 , C07D217/22 , C07D403/12 , C07D413/12
CPC分类号： C07D213/62 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.
摘要翻译：式（I）化合物或其药学上可接受的盐是阿片样物质受体调节剂，例如 μ-阿片受体拮抗剂，中性拮抗剂或反向激动剂，并且可用于治疗包括肥胖症在内的代谢紊乱。

2. 发明申请

US20120059014A1 Compounds for the Treatment of Metabolic Disorders 审中-公开
标题翻译：化合物治疗代谢紊乱
公开(公告)号：US20120059014A1
公开(公告)日：2012-03-08
申请号：US13255531
申请日：2010-03-12
申请人： Oscar Barba , Tom Banksia Dupree , Peter Timothy Fry , Matthew Colin Thor Fyfe , Revathy Perpetua Jeevaratnam , Thomas Martin Krulle , Karen Lesley Schofield , Donald Smyth , Thomas Staroske , Alan John William Stewart , David French Stonehouse , Simon Andrew Swain , David Matthew Withall
发明人： Oscar Barba , Tom Banksia Dupree , Peter Timothy Fry , Matthew Colin Thor Fyfe , Revathy Perpetua Jeevaratnam , Thomas Martin Krulle , Karen Lesley Schofield , Donald Smyth , Thomas Staroske , Alan John William Stewart , David French Stonehouse , Simon Andrew Swain , David Matthew Withall
IPC分类号： A61K31/506 , C07D413/14 , A61K31/4545 , A61K31/501 , A61P9/12 , A61P3/04 , A61P3/00 , A61P3/08 , A61P3/06 , A61P7/00 , C07D401/14 , A61P3/10
CPC分类号： C07D403/12
摘要： The present invention is directed to therapeutic compounds of the following formula (I) which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.
摘要翻译：本发明涉及具有作为GPR119激动剂的活性的下式（I）的治疗性化合物，并且可用于治疗包括II型糖尿病的代谢紊乱。

3. 发明申请

US20080188472A1 Indole-2-Carboxylic Acid Hydrazides 审中-公开
标题翻译：吲哚-2-羧酸酰肼
公开(公告)号：US20080188472A1
公开(公告)日：2008-08-07
申请号：US10592011
申请日：2005-03-08
申请人： Stuart Edward Bradley , Revathy Perpetua Jeevaratnam , Thomas Martin Krulle , Martin James Procter , Robert John Rowley , Gerard Hugh Thomas , Ana Valdes
发明人： Stuart Edward Bradley , Revathy Perpetua Jeevaratnam , Thomas Martin Krulle , Martin James Procter , Robert John Rowley , Gerard Hugh Thomas , Ana Valdes
IPC分类号： A61K31/5377 , C07D209/42 , C07D409/12 , A61K31/404 , A61K31/427 , A61K31/422 , A61K31/4178 , C07D417/12 , C07D413/12 , A61P9/10 , A61P3/10 , C07D403/12 , C07D401/12 , C07D471/04 , C07D413/14 , A61K31/4725 , A61K31/4439 , A61K31/437
CPC分类号： C07D471/04 , C07D209/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D495/04
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia, e.g. myocardial ischemia, or as cardioprotectants or inhibitors of abnormal cell growth.
摘要翻译：式（I）化合物或其药学上可接受的盐是糖原磷酸化酶的抑制剂，可用于预防或治疗糖尿病，高血糖症，高胆固醇血症，高胰岛素血症，高脂血症，高血压，动脉粥样硬化或组织缺血。心肌缺血或作为心脏保护剂或异常细胞生长的抑制剂。

4. 发明授权

US07214681B2 Tri(cyclo) substituted amide compounds 失效
标题翻译：三（环）取代的酰胺化合物
公开(公告)号：US07214681B2
公开(公告)日：2007-05-08
申请号：US10776584
申请日：2004-02-10
申请人： Matthew Colin Thor Fyfe , Lisa Sarah Gardner , Maseo Nawano , Martin James Procter , Chrystelle Marie Rasamison , Karen Lesley Schofield , Vilasben Kanji Shah , Kosuke Yasuda
发明人： Matthew Colin Thor Fyfe , Lisa Sarah Gardner , Maseo Nawano , Martin James Procter , Chrystelle Marie Rasamison , Karen Lesley Schofield , Vilasben Kanji Shah , Kosuke Yasuda
IPC分类号： A61K31/502 , C07D43/02
CPC分类号： C07D231/12 , C07D211/34 , C07D213/55 , C07D233/56 , C07D249/08 , C07D277/30 , C07D277/40 , C07D277/46 , C07D307/54 , C07D309/04 , C07D309/08 , C07D333/24 , C07D333/28 , C07D335/02 , C07D405/10 , C07D405/12 , C07D407/12 , C07D409/10 , C07D413/12 , C07D417/12 , C07D417/14 , C07D491/08
摘要： Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
摘要翻译：式（I）化合物或其药学上可接受的盐可用于预防和治疗高血糖症和糖尿病。

5. 发明授权

US07083933B1 Methods for identification of modulators of OSGPR116 activity 失效
标题翻译：用于鉴定OSGPR116活性调节剂的方法
公开(公告)号：US07083933B1
公开(公告)日：2006-08-01
申请号：US10841183
申请日：2004-05-06
申请人： Graeme Griffin
发明人： Graeme Griffin
IPC分类号： G01N33/566 , G01N33/567 , G01N33/569 , G01N33/574 , C07K14/705
CPC分类号： C07K14/705 , G01N33/76 , G01N2333/726
摘要： This invention relates to the identification of fatty acid or lipid amides that decrease food intake in mammals, including fatty acid ethanolamides, as ligands for the G-protein coupled receptor OSGPR116, and describes the first demonstration of a specific G-protein coupled receptor that is activated by fatty acid ethanolamides that inhibit feeding. The invention is directed to new methods for screening candidate drugs for their ability to modulate the activity of OSGPR116, and new pharmaceutical agents identified by these methods. It is also directed to the use of such agents in the manufacture of medicaments for the treatment of OSGPR116 mediated diseases, and methods of treating diseases such as obesity and diabetes by administering to an individual a therapeutic amount of a modulator of OSGPR116 identified by these methods.
摘要翻译：本发明涉及在哺乳动物（包括脂肪酸乙醇酰胺）中降低食物摄取量的脂肪酸或脂质酰胺作为G蛋白偶联受体OSGPR116的配体，并且描述了特异性G蛋白偶联受体的第一次证明由脂肪酸乙醇酰胺激活，抑制喂养。本发明涉及用于筛选候选药物以调节OSGPR116的活性的能力的新方法，以及通过这些方法鉴定的新药物。还涉及这样的药剂在制备用于治疗OSGPR116介导的疾病的药物中的用途，以及通过向个体施用治疗量的通过这些方法鉴定的OSGPR116调节剂的治疗疾病如肥胖症和糖尿病的方法。

6. 发明授权

US08193359B2 G-protein coupled receptor agonists 失效
标题翻译： G蛋白偶联受体激动剂
公开(公告)号：US08193359B2
公开(公告)日：2012-06-05
申请号：US11794220
申请日：2005-12-23
申请人： Matthew Colin Thor Fyfe , Gerard Hugh Thomas , Lisa Sarah Bertram , Stuart Edward Bradley , William Gattrell , Chrystelle Marie Rasamison , Vilasben Kanji Shah
发明人： Matthew Colin Thor Fyfe , Gerard Hugh Thomas , Lisa Sarah Bertram , Stuart Edward Bradley , William Gattrell , Chrystelle Marie Rasamison , Vilasben Kanji Shah
IPC分类号： C07D491/048 , A61K31/4355
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.
摘要翻译：式（I）化合物或其药学上可接受的盐或N-氧化物是GPR116的激动剂，可用于治疗肥胖症和治疗糖尿病。

7. 发明申请

US20110230507A1 Piperidine GPCR Agonists 审中-公开
标题翻译：哌啶GPCR激动剂
公开(公告)号：US20110230507A1
公开(公告)日：2011-09-22
申请号：US13003567
申请日：2009-07-10
申请人： Lisa Sarah Bertram , Matthew Colin Thor Fyfe , Revathy Perpetua Jeevaratnam , John Keily
发明人： Lisa Sarah Bertram , Matthew Colin Thor Fyfe , Revathy Perpetua Jeevaratnam , John Keily
IPC分类号： A61K31/506 , C07D413/14 , A61K31/454 , C07D405/14 , A61K31/4545 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00
CPC分类号： C07D413/14
摘要： Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.
摘要翻译：式（I）化合物或其药学上可接受的盐是GPCR激动剂，可用于治疗糖尿病和肥胖症。

8. 发明授权

US07166579B2 Prodrugs of DP IV-inhibitors 有权
标题翻译： DP IV抑制剂的前药
公开(公告)号：US07166579B2
公开(公告)日：2007-01-23
申请号：US10735582
申请日：2003-12-11
申请人： Hans-Ulrich Demuth , Dagmar Schlenzig , Torsten Hoffmann , Susanne Manhart
发明人： Hans-Ulrich Demuth , Dagmar Schlenzig , Torsten Hoffmann , Susanne Manhart
IPC分类号： A61K38/05 , A61K38/04
CPC分类号： C07K5/06165 , A61K38/00 , C07K5/06173 , C07K5/0806 , C07K5/0808 , C07K5/0823
摘要： Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.
摘要翻译：丝氨酸肽酶二肽基肽酶IV的不稳定抑制剂的前药化合物用于治疗各种疾病，特别是代谢紊乱。前药化合物可用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸痛，糖尿病，糖尿病性神经病变和肾病。

9. 发明授权

US07060719B2 Glutaminyl based DPIV inhibitors 有权
标题翻译：基于谷氨酰胺基的DPIV抑制剂
公开(公告)号：US07060719B2
公开(公告)日：2006-06-13
申请号：US10779158
申请日：2004-02-13
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
IPC分类号： A61K31/425 , A61K31/40 , C07D277/04 , C07D207/00
CPC分类号： C07D277/04 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D295/185 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K7/06
摘要： The present invention provides compounds of the formula: wherein X=CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.
摘要翻译：本发明提供下式的化合物：其中X = CH 2或S或其药学上可接受的盐可用于治疗由DPIV或DPIV样酶如关节炎，肥胖，免疫和自身免疫介导的病症疾病，同种异体移植，癌症，神经元疾病和皮肤疾病。

10. 发明授权

US06890905B2 Methods for improving islet signaling in diabetes mellitus and for its prevention 失效
标题翻译：改善糖尿病胰岛信号的方法及其预防
公开(公告)号：US06890905B2
公开(公告)日：2005-05-10
申请号：US10216349
申请日：2002-08-09
申请人： Hans-Ulrich Demuth , Konrad Glund , Andrew J. Pospisilik , Kerstin Kuehn-Wache
发明人： Hans-Ulrich Demuth , Konrad Glund , Andrew J. Pospisilik , Kerstin Kuehn-Wache
IPC分类号： A61K31/40 , A61K31/426 , A61K38/00 , A61K31/425 , A61K31/70
CPC分类号： A61K31/40 , A61K31/426
摘要： The present invention discloses methods for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic β-cells, to cause differentiation of pancreatic epithelial cells into insulin producing β-cells, to improve muscle sensitivity to insulin and other weight control efforts by the chronic oral administration of a DP IV-inhibitor. The administration causes the active form of GLP-1 and other non-nutrient stimulated growth hormones to remain biologically active longer under physiological conditions. The extended presence of such hormones, in particular in the pancreatic tissue can also facilitate differentiation and regeneration of the β-cells already present that are in need of repair.
摘要翻译：本发明公开了用于治疗性治疗哺乳动物（包括但不限于人）的方法，以增加内源性胰腺β-细胞的相对胰岛素产生性能，使胰腺上皮细胞分化为产生胰岛素的β细胞，以改善肌肉对胰岛素和其他体重控制努力通过慢性口服给予DP IV抑制剂。在生理条件下，给药导致GLP-1和其他非营养刺激生长激素的活性形式在生物活性更长的时间内保持生物活性。这种激素，特别是胰腺组织的延长存在也可促进已经存在的需要修复的β细胞的分化和再生。

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