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1. 发明申请

WO2003099279A1 COMBINATION OF A DPP IV INHIBITOR AND A CARDIOVASCULAR COMPOUND 审中-公开
标题翻译： DPP IV抑制剂和心血管化合物的组合
公开(公告)号：WO2003099279A1
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005639
申请日：2003-05-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HOLMES, David, Grenville , SHETTY, Suraj, Shivappa , HUGHES, Thomas, Edward
发明人： HOLMES, David, Grenville , SHETTY, Suraj, Shivappa , HUGHES, Thomas, Edward
IPC分类号： A61K31/454
CPC分类号： A61K31/454 , A61K31/16 , A61K31/40 , A61K31/41
摘要： The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and a cardiovascular compound (being different from a statin) or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention, delay of progression or treatment of diseases and disorders selected from the group consisting of hypertension, congestive heart failure, left ventricular hypertrophy, peripheral arterial disease, diabetes, especially type 2 diabetes mellitus, diabetic retinophathy, macular degeneration, cataract, diabetic nephropathy, glomerulosclerosis, chronic renal failure, diabetic neuropathy, syndrome X, premenstrual syndrome, coronary heart disease, angina pectoris, thrombosis, atherosclerosis, myocardial infarction, transient ischemic attacks, stroke, vascular restenosis, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertryglyceridemia, insulin resistance, impaired glucose metabolism, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, obesity, erectile dysfunction, skin and connective tissue disorders, foot ulcerations and ulcerative colitis, endothelial dysfunction and impaired vascular compliance.
摘要翻译：本发明涉及分别包含DPP IV抑制剂或其药学上可接受的盐和心血管化合物（不同于他汀类）或其药学上可接受的盐的组合制剂或药物组合物的组合。本发明还涉及这种组合用于预防，延缓进展或治疗选自高血压，充血性心力衰竭，左心室肥大，外周动脉疾病，糖尿病，特别是2型糖尿病，糖尿病性视网膜病变，黄斑变性，白内障，糖尿病肾病，肾小球硬化，慢性肾功能衰竭，糖尿病性神经病，X综合征，经前期综合征，冠心病，心绞痛，血栓形成，动脉粥样硬化，心肌梗死，短暂性脑缺血发作，中风，血管再狭窄，高血糖症，高胰岛素血症，高脂血症，高甘油三酯血症，胰岛素抵抗，糖代谢障碍，葡萄糖耐量降低的病症，空腹血浆葡萄糖受损的病症，肥胖症，勃起功能障碍，皮肤和结缔组织疾病，足部溃疡和溃疡性结肠炎，内皮功能障碍功能受损和血管依从性受损。

2. 发明申请

WO2007035665A1 USE OF A DPP-IV INHIBITOR TO REDUCE HYPOGLYCEMIC EVENTS 审中-公开
标题翻译：使用DPP-IV抑制剂减少高血压事件
公开(公告)号：WO2007035665A1
公开(公告)日：2007-03-29
申请号：PCT/US2006/036338
申请日：2006-09-18
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , BALKAN, Börk , HOLMES, David, Grenville , HUGHES, Thomas, Edward , VILLHAUER, Edwin, Bernard
发明人： BALKAN, Börk , HOLMES, David, Grenville , HUGHES, Thomas, Edward , VILLHAUER, Edwin, Bernard
IPC分类号： A61K45/06
CPC分类号： A61K45/06 , A61K31/155 , A61K31/64 , A61K38/28 , A61K2300/00
摘要： The invention relates to a method to reduce the hypoglycemic events, especially sever hypoglycemic events resulting from insulin treatment, wherein the patient is treated with a Dipeptidyl peptidase IV inhibitor (DPP-IV inhibitor) or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及一种减少低血糖事件的方法，特别是由胰岛素治疗引起的切断的低血糖事件，其中患者用二肽基肽酶IV抑制剂（DPP-IV抑制剂）或其药学上可接受的盐治疗。

3. 发明申请

WO2003101448A1 THE USE OF SUBSTITUTED CYANOPYRROLIDINES AND COMBINATION PREPARATIONS CONTAINING THEM FOR TREATING HYPERLIPIDEMIA AND ASSOCIATED DISEASES 审中-公开
标题翻译：使用替代的CYANOPRROLIDINES和组合制剂，用于治疗高脂血症和相关疾病
公开(公告)号：WO2003101448A1
公开(公告)日：2003-12-11
申请号：PCT/EP2003/005762
申请日：2003-06-02
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HOLMES, David, Grenville , HUGHES, Thomas, Edward
发明人： HOLMES, David, Grenville , HUGHES, Thomas, Edward
IPC分类号： A61K31/40
CPC分类号： A61K31/401 , A61K31/40 , A61K45/06 , A61K2300/00
摘要： Disclosed are methods and compositions for the treatment of hyperlipidemia and conditions associated therewith, such as CHD, ischemic stroke, restenosis after angioplasty, peripheral vascular disease, intermittent claudication, myocardial infarction (e.g. necrosis and apoptosis), dyslipidemia and post-prandial lipemia. The methods include administration of a therapeutically effective amount of a compound of formula (I), wherein R is substituted adamantyl; and N is 0 to 3; in free form or in acid addition salt form, and a pharmaceutically acceptable carrier.
摘要翻译：公开了用于治疗高脂血症和与之相关的病症的方法和组合物，例如CHD，缺血性卒中，血管成形术后的再狭窄，外周血管疾病，间歇性跛行，心肌梗死（例如坏死和凋亡），血脂异常和餐后脂肪血症。所述方法包括施用治疗有效量的式（I）化合物，其中R是取代的金刚烷基; N为0〜3; 游离形式或酸加成盐形式，和药学上可接受的载体。

4. 发明申请

WO2008057337A3 USE OF DIPEPTIDYL PEPTIDASE IV INHIBITORS FOR PREVENTING, DELAYING OR REDUCING THE OCCURANCE OF EDEMA 审中-公开
公开(公告)号：WO2008057337A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/022902
申请日：2007-10-30
申请人： NOVARTIS AG , BALKAN, Börk , HOLMES, David, Grenville , HUGHES, Thomas, Edward , VILLHAUER, Edwin, Bernard
发明人： BALKAN, Börk , HOLMES, David, Grenville , HUGHES, Thomas, Edward , VILLHAUER, Edwin, Bernard
IPC分类号： A61K31/4422 , A61K31/4439 , A61K45/00 , A61K31/40 , A61K31/425 , A61K31/44 , A61K31/47 , A61P43/00
摘要： A method to prevent, delay the progression or reduce, the occurrence of edema, comprising administering a therapeutically effective amount of a DPP-IV inhibitor, or pharmaceutically acceptable salt thereof, to a patient in need thereof.

5. 发明申请

WO2005049088A2 COMBINATION OF ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物的组合
公开(公告)号：WO2005049088A2
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012989
申请日：2004-11-16
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HOLMES, David, Grenville
发明人： HOLMES, David, Grenville
IPC分类号： A61K45/06
CPC分类号： A61K45/06 , A61K31/137 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4439 , A61K31/47 , A61K31/4704 , A61K2300/00
摘要： The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and an antiobesity agent, or an appetite regulating agent, or a pharmaceutically acceptable salt thereof.. The present invention furthermore relates to the use of such a combination for the prevention, delay of progression or treatment of diseases and disorders selected from the group consisting of hypertension, congestive heart failure, left ventricular hypertrophy, peripheral arterial disease, diabetes, especially type 2 diabetes mellitus, diabetic retinopathy, macular degeneration, cataract, diabetic nephropathy, glomerulosclerosis, chronic renal failure, diabetic neuropathy, syndrome X, premenstrual syndrome, coronary heart disease, angina pectoris, thrombosis, atherosclerosis, myocardial infarction, transient ischemic attacks, stroke, vascular restenosis, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertryglyceridemia, insulin resistance, impaired glucose metabolism, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, obesity, erectile dysfunction, skin and connective tissue disorders, foot ulcerations and ulcerative colitis, endothelial dysfunction and impaired vascular compliance.
摘要翻译：本发明涉及分别包含DPP IV抑制剂或其药学上可接受的盐和抗肥胖剂或食欲调节剂或其药学上可接受的盐的组合制剂或药物组合物的组合。本发明还涉及这种组合用于预防，延缓进展或治疗选自高血压，充血性心力衰竭，左心室肥大，外周动脉疾病，糖尿病，特别是2型糖尿病糖尿病，糖尿病性视网膜病变，黄斑变性，白内障，糖尿病肾病，肾小球硬化，慢性肾功能衰竭，糖尿病性神经病变，X综合征，经前期综合征，冠心病，心绞痛，血栓形成，动脉粥样硬化，心肌梗死，短暂性脑缺血发作，中风，血管再狭窄，高血糖，高血糖血糖异常，高脂血症，高甘油三酯血症，胰岛素抵抗，糖代谢障碍，葡萄糖耐量降低的病症，空腹血浆葡萄糖受损的病症，肥胖症，勃起功能障碍，皮肤和结缔组织疾病，足部溃疡和溃疡性结肠炎，血管内皮功能障碍和血管依从性受损。

6. 发明公开

EP1511484A1 COMBINATION OF A DPP IV INHIBITOR AND A CARDIOVASCULAR COMPOUND 审中-公开
标题翻译：组合的DPP-IV抑制剂和心血管CONNECTION作者
公开(公告)号：EP1511484A1
公开(公告)日：2005-03-09
申请号：EP03755149.6
申请日：2003-05-28
申请人： Novartis AG , Novartis Pharma GmbH
发明人： HOLMES, David, Grenville , SHETTY, Suraj, Shivappa , HUGHES, Thomas, Edward
IPC分类号： A61K31/454 , A61K31/40 , A61K31/16 , A61P3/10 , A61K31/41
CPC分类号： A61K31/454 , A61K31/16 , A61K31/40 , A61K31/41
摘要： The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and a cardiovascular compound (being different from a statin) or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention, delay of progression or treatment of diseases and disorders selected from the group consisting of hypertension, congestive heart failure, left ventricular hypertrophy, peripheral arterial disease, diabetes, especially type 2 diabetes mellitus, diabetic retinophathy, macular degeneration, cataract, diabetic nephropathy, glomerulosclerosis, chronic renal failure, diabetic neuropathy, syndrome X, premenstrual syndrome, coronary heart disease, angina pectoris, thrombosis, atherosclerosis, myocardial infarction, transient ischemic attacks, stroke, vascular restenosis, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertryglyceridemia, insulin resistance, impaired glucose metabolism, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, obesity, erectile dysfunction, skin and connective tissue disorders, foot ulcerations and ulcerative colitis, endothelial dysfunction and impaired vascular compliance.

7. 发明授权

EP1248604B2 COMBINATIONS COMPRISING DIPEPTIDYLPEPTIDASE-IV INHIBITORS AND ANTIDIABETIC AGENTS 有权
标题翻译：组合物，包含二肽基肽酶IV抑制剂和抗糖尿病药物
公开(公告)号：EP1248604B2
公开(公告)日：2012-02-29
申请号：EP01909661.9
申请日：2001-01-19
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BALKAN, Börk , HUGHES, Thomas, Edward , HOLMES, David, Grenville , VILLHAUER, Edwin, Bernard
IPC分类号： A61K45/06 , A61P3/10 , A61K31/00 , A61K31/4025 , A61K31/44 , A61K31/505
CPC分类号： A61K45/06 , A61K31/00 , A61K31/4025 , A61K31/44 , A61K31/505 , A61K2300/00
摘要： The invention relates to a combination which comprises a DPP-IV inhibitor and at least one further antidiabetic compound, preferably selected from the group consisting of insulin signalling pathway modulators, like inhibitors of protein tyrosine phosphatases (PTPases), non-small molecule mimetic compounds and inhibitors of glutamine-fructose-6-phosphate amidotransferase (GFAT), compounds influencing a dysregulated hepatic glucose production, like inhibitors of glucose-6-phosphatase (G6Pase), inhibitors of fructose-1,6-bisphosphatase (F-1,6-BPase), inhibitors of glycogen phosphorylase (GP), glucagon receptor antagonists and inhibitors of phosphoenolpyruvate carboxykinase (PEPCK), pyruvate dehydrogenase kinase (PDHK) inhibitors, insulin sensitivity enhancers, insulin secretion enhancers, α-glucosidase inhibitors, inhibitors of gastric emptying, insulin, and α2-adrenergic antagonists, for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of conditions mediated by dipeptidylpeptidase - IV (DPP-IV), in particular diabetes, more especially type 2 diabetes mellitus, conditions of impaired glucose tolerance (IGT), conditions of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, obesity and osteoporosis; and the use of such combination for the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight.

8. 发明公开

EP1513519A1 THE USE OF SUBSTITUTED CYANOPYRROLIDINES AND COMBINATION PREPARATIONS CONTAINING THEM FOR TREATING HYPERLIPIDEMIA AND ASSOCIATED DISEASES 有权
标题翻译：取代CYANOPYRROLIDINEN用于治疗高脂血症USE
公开(公告)号：EP1513519A1
公开(公告)日：2005-03-16
申请号：EP03737984.9
申请日：2003-06-02
申请人： Novartis AG , Novartis Pharma GmbH
发明人： HOLMES, David, Grenville , HUGHES, Thomas, Edward
IPC分类号： A61K31/40 , A61K45/06 , A61P9/10
CPC分类号： A61K31/401 , A61K31/40 , A61K45/06 , A61K2300/00
摘要： Disclosed are methods and compositions for the treatment of hyperlipidemia and conditions associated therewith, such as CHD, ischemic stroke, restenosis after angioplasty, peripheral vascular disease, intermittent claudication, myocardial infarction (e.g. necrosis and apoptosis), dyslipidemia and post-prandial lipemia. The methods include administration of a therapeutically effective amount of a compound of formula (I), wherein R is substituted adamantyl; and N is 0 to 3; in free form or in acid addition salt form, and a pharmaceutically acceptable carrier.

9. 发明授权

EP1513519B1 THE USE OF SUBSTITUTED CYANOPYRROLIDINES FOR TREATING HYPERLIPIDEMIA 有权
标题翻译：取代CYANOPYRROLIDINEN用于治疗高脂血症USE
公开(公告)号：EP1513519B1
公开(公告)日：2009-02-18
申请号：EP03737984.9
申请日：2003-06-02
申请人： NOVARTIS AG , Novartis Pharma GmbH
发明人： HOLMES, David, Grenville , HUGHES, Thomas, Edward
IPC分类号： A61K31/40 , A61P9/10
CPC分类号： A61K31/401 , A61K31/40 , A61K45/06 , A61K2300/00
摘要： Disclosed are methods and compositions for the treatment of hyperlipidemia and conditions associated therewith, such as CHD, ischemic stroke, restenosis after angioplasty, peripheral vascular disease, intermittent claudication, myocardial infarction (e.g. necrosis and apoptosis), dyslipidemia and post-prandial lipemia. The methods include administration of a therapeutically effective amount of a compound of formula (I), wherein R is substituted adamantyl; and N is 0 to 3; in free form or in acid addition salt form, and a pharmaceutically acceptable carrier.

10. 发明公开

EP1928499A1 USE OF A DPP-IV INHIBITOR TO REDUCE HYPOGLYCEMIC EVENTS 有权
标题翻译： DPP-IV抑制剂的使用，减少低血糖事件
公开(公告)号：EP1928499A1
公开(公告)日：2008-06-11
申请号：EP06803805.8
申请日：2006-09-18
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： BALKAN, Börk , HOLMES, David, Grenville , HUGHES, Thomas, Edward , VILLHAUER, Edwin, Bernard
IPC分类号： A61K45/06
CPC分类号： A61K45/06 , A61K31/155 , A61K31/64 , A61K38/28 , A61K2300/00
摘要： The invention relates to a method to reduce the hypoglycemic events, especially sever hypoglycemic events resulting from insulin treatment, wherein the patient is treated with a Dipeptidyl peptidase IV inhibitor (DPP-IV inhibitor) or a pharmaceutically acceptable salt thereof.

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