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11. 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.

12. 发明公开

EP1768664A1 COMBINATION OF DPP-IV INHIBITORS AND COMPOUNDS MODULATING 5-HT3 AND/OR 5-HT4 RECEPTORS 审中-公开
标题翻译： DPP-IV抑制剂和化合物的调制的5-HT3和/或5-HT 4受体组合
公开(公告)号：EP1768664A1
公开(公告)日：2007-04-04
申请号：EP05761596.5
申请日：2005-07-13
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： VILLHAUER, Edwin, Bernard
IPC分类号： A61K31/40 , A61K31/404 , A61P1/00 , A61P3/10
CPC分类号： A61K31/40 , A61K31/404 , 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 comprising at least one therapeutic agent selected from an agent interacting with a 5-HT3 receptor and/or an agent interacting with 5HT4 receptor, 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 selected from insulin resistance, impaired glucose metabolism, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, diabetes particularly type 2 diabetes mellitus, obesity, diabetic retinopathy, macular degeneration, cataracts, diabetic nephropathy, glomerulosclerosis, diabetic neuropathy, erectile dysfunction, premenstrual syndrome, coronary heart disease, hypertension, angina pectoris, myocardial infarction, stroke, vascular restenosis, skin and connective tissue disorders, foot ulceration’s and ulcerative colitis, endothelial dysfunction and impaired vascular compliance, altered gastrointestinal motility, sensitivity and/or secretion disorder(s) which include, but are not limited to, heartburn, bloating, postoperative ileus, abdominal pain and discomfort, early satiety, epigastric pain, nausea, vomiting, burbulence, regurgitation, intestinal pseudoobstruction, anal incontinence, GERD, IBS, dyspepsia, chronic constipation or diarrhea, diabetic gastropathy, gastroparesis, e.g. diabetic gastroparesis, ulcerative colitis, Crohn's disease, ulcers and the visceral pain associated therewith.

13. 发明授权

EP0937040B1 N-SUBSTITUTED 2-CYANOPYRROLIDINES 失效
标题翻译： N-取代的2-氰基吡咯烷类
公开(公告)号：EP0937040B1
公开(公告)日：2004-07-21
申请号：EP97950112.9
申请日：1997-11-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： VILLHAUER, Edwin, Bernard
IPC分类号： C07D207/00 , C07D401/00 , C07K5/00
CPC分类号： C07D401/12 , C07D207/16 , C07D403/12

14. 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.

15. 发明公开

EP1912938A2 SALTS OF VILDAGLIPTIN 审中-公开
标题翻译：维格列汀盐
公开(公告)号：EP1912938A2
公开(公告)日：2008-04-23
申请号：EP06789345.3
申请日：2006-08-02
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： REBER, Jean-Louis , VILLHAUER, Edwin, Bernard
IPC分类号： C07D207/16 , A61K31/401 , A61P3/10
CPC分类号： C07D207/16
摘要： The present invention relates to novel salt forms of vildagliptin (LAF237), i.e. salt forms of (S)-1-[(3-hydroxy-1-adamantyl)amino]acetyl-2-cyano-pyrrolidine.

16. 发明公开

EP1791842A1 PROCESS FOR THE PREPARATION OF 6, 8-SUBSTITUTED `1, 7 NAPHTHPYRIDIN DERIVATIVES BY REACTING THE 8-HALO-`1, 7 NAPHTHPYRIDIN-DERIVATE WITH AN ORGANIC BORONIC ACID DERIVATIVES AND INTERMADIATES OF THIS PROCESS 审中-公开
标题翻译：用于生产6,8-取代的1,7- NAPHTHPYRIDINDERIVATEN通过实施8 - 卤-1,7- NAPHTHPYRIDINDERIVATS WITH有机硼酸衍生物，和中间产品这一程序
公开(公告)号：EP1791842A1
公开(公告)日：2007-06-06
申请号：EP05805619.3
申请日：2005-09-12
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： JIANG, Xinglong , KAPA, Prasad, Koteswara , LEE, George, Tien-San , VILLHAUER, Edwin, Bernard
IPC分类号： C07D471/04
CPC分类号： C07D213/81 , C07D471/04
摘要： A process for the preparation of compounds of formula (I) wherein R1 is C1-C20-alkyl optionally substituted by one or two of hydroxy, C3-C12cycloalkyl, C6-C12-aryl, C1-C7-alkoxy, thiol, C1-C7-alkylthio or carboxy, or R1 is C3-C12-cycloalkyl optionally substituted by one or two of C1-C7-alkyl, hydroxy, C1C7-alkoxy, CI-C7-alkylthio or carboxy, or R1 is C6-C12-aryl optionally substituted by one, two, three or four substituents selected from C1-C7-alkyl, halo; hydroxy, C1-C7-alkoxy, C1-C7-alkylthio and nitro, or R1 is heteroaryl optionally substituted by C1-C7- alkyl, Cl-C7-alkoxy or halo; R2 and R3 are independently hydrogen or C1-C20-alkoxy; R4 is C6-C12-aryl optionally substituted by one, two, three or four substituents selected from C1-C7-alkyl, halo, hydroxy, C1-C7-alkoxy, C1-C7-alkylthio and nitro, or R4 is heteroaryl optionally substituted by C1-C7,- alkyl, C1-C7-alkoxy or halo; and X is N or CH; or a salt thereof; which process comprises coupling compounds of formula (VI) and Y is chloro or bromo in the presence of a catalyst and a base with a compound of the formula (VII) and R6 and R7 are hydrogen or, C1-C7-alkyl, or R6 and R7 combined are C2-C3 alkylene optionally substituted by one or two of C1-C4-alkyl that together with the boron and the oxygen atoms form a 5- or 6-membered ring.

17. 发明公开

EP1385549A2 COMBINATION OF NATEGLINIDE OR REPAGLINIDE WITH AT LEAST ONE FURTHER ANTIDIABETIC COMPOUND 审中-公开
标题翻译：或那格列奈瑞格列奈组合中的至少一种其他抗糖尿病化合物
公开(公告)号：EP1385549A2
公开(公告)日：2004-02-04
申请号：EP02724221.3
申请日：2002-03-11
申请人： Novartis AG , Novartis Pharma GmbH
发明人： VILLHAUER, Edwin, Bernard
IPC分类号： A61K45/06 , A61K31/445 , A61K31/195 , A61P3/10
CPC分类号： A61K45/06 , A61K31/195 , A61K31/445 , A61K38/2278 , A61K38/26 , A61K2300/00
摘要： The present invention relates to a combination of organic compounds which comprises at least two antidiabetic agents, preferably with different modes of action, in which the active ingredients are in each case present in free form or in the form of a pharmaceutically acceptable salt and, optionally, at least on pharmaceutically acceptable carrier, for simultaneous, separate or sequential use.

18. 发明授权

EP1928499B1 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：EP1928499B1
公开(公告)日：2011-06-29
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.

19. 发明授权

EP1248604B1 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：EP1248604B1
公开(公告)日：2006-11-29
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： A61K45/00 , A61K31/401 , A61P3/10
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.

20. 发明公开

EP1296974A2 2-CYANOPYRROLIDINE DERIVATIVES AND THEIR USE AS MEDICAMENTS 有权
标题翻译： 2-氰基衍生物及其AS DRUGS
公开(公告)号：EP1296974A2
公开(公告)日：2003-04-02
申请号：EP01984014.9
申请日：2001-06-11
申请人： Novartis AG , Novartis Pharma GmbH
发明人： VILLHAUER, Edwin, Bernard
IPC分类号： C07D401/12 , C07D207/16 , C07D403/12 , C07D417/12 , C07D409/12 , A61K31/40 , A61K31/4439 , A61K31/506 , A61K31/428 , A61K31/427 , A61P3/10
CPC分类号： C07D401/12 , C07D207/16 , C07D403/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to certain N-(substituted glycyl)-2-cyanopyrrolidines of formula (I) wherein Y is as defined herein, in free form or in acid addition salt form. Compounds of formula (I) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.

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