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1. 发明申请

WO0152825A2 COMBINATIONS COMPRISING DIPEPTIDYLPEPTIDASE - IV INHIBITOR 审中-公开
标题翻译：包含DIPEPTIDYPEPTIDASE-IV抑制剂的组合
公开(公告)号：WO0152825A2
公开(公告)日：2001-07-26
申请号：PCT/EP0100590
申请日：2001-01-19
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , BALKAN BOERK , HUGHES THOMAS EDWARD , HOLMES DAVID GRENVILLE , VILLHAUER EDWIN BERNARD
发明人： BALKAN BOERK , HUGHES THOMAS EDWARD , HOLMES DAVID GRENVILLE , VILLHAUER EDWIN BERNARD
IPC分类号： A61K31/00 , A61K31/155 , A61K31/198 , A61K31/40 , A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/4453 , A61K31/505 , A61K31/7036 , A61K45/06 , A61P3/00 , A61P3/04 , A61P3/10 , A61P19/02 , A61P19/10 , A61P29/00 , A61P43/00
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, alpha -glucosidase inhibitors, inhibitors of gastric emptying, insulin, and alpha 2-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.
摘要翻译：本发明涉及包含DPP-IV抑制剂和至少一种另外的抗糖尿病化合物的组合，其优选选自胰岛素信号通路调节剂，如蛋白酪氨酸磷酸酶（PTPases）的抑制剂，非小分子模拟化合物和谷氨酰胺 - 果糖-6-磷酸酰胺转移酶（GFAT）的抑制剂，影响失调的肝脏葡萄糖产生的化合物，如葡萄糖-6-磷酸酶（G6Pase）的抑制剂，果糖-1,6-二磷酸酶抑制剂（F-1,6- BPA），糖原磷酸化酶（GP）的抑制剂，胰高血糖素受体拮抗剂和磷酸烯醇丙酮酸羧激酶（PEPCK），丙酮酸脱氢酶激酶（PDHK）抑制剂，胰岛素敏感性增强剂，胰岛素分泌增强剂，α-葡糖苷酶抑制剂，胃排空抑制剂，胰岛素和α2-肾上腺素能拮抗剂，用于同时，分开或顺序用于预防，延缓进展或治疗由二肽基肽酶IV（DPP-IV）介导的病症，特别是糖尿病，尤其是2型糖尿病，葡萄糖耐量降低的病症（IGT），空腹血浆葡萄糖受损的病症，代谢性酸中毒，酮症，关节炎，肥胖症和骨质疏松症; 以及使用这种组合来进行哺乳动物的美容治疗，以实现美容上有益的体重减轻。

2. 发明申请

WO2008057337A2 USE OF ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物的使用
公开(公告)号：WO2008057337A2
公开(公告)日：2008-05-15
申请号：PCT/US2007022902
申请日：2007-10-30
申请人： NOVARTIS AG , BALKAN BOERK , HOLMES DAVID GRENVILLE , HUGHES THOMAS EDWARD , VILLHAUER EDWIN BERNARD
发明人： BALKAN BOERK , HOLMES DAVID GRENVILLE , HUGHES THOMAS EDWARD , VILLHAUER EDWIN BERNARD
CPC分类号： A61K31/425 , A61K31/40 , A61K31/44 , A61K31/4422 , A61K31/4439 , A61K31/47 , A61K45/06 , A61K2300/00
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.
摘要翻译：一种预防，延缓进展或降低水肿发生的方法，包括向有需要的患者施用治疗有效量的DPP-IV抑制剂或其药学上可接受的盐。

3. 发明申请

WO2007149797A2 USE OF ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物的使用
公开(公告)号：WO2007149797A2
公开(公告)日：2007-12-27
申请号：PCT/US2007071420
申请日：2007-06-18
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HOLMES DAVID GRENVILLE , HUGHES THOMAS EDWARD , VILLHAUER EDWIN BERNARD , BALKAN BOERK
发明人： HOLMES DAVID GRENVILLE , HUGHES THOMAS EDWARD , VILLHAUER EDWIN BERNARD , BALKAN BOERK
IPC分类号： A61K31/155 , A61K31/401 , A61P1/00 , A61P3/00 , A61P43/00
CPC分类号： A61K31/155 , A61K31/401
摘要： A method to prevent, delay the progression or reduce, the Gastrointestinal disorders or Gastrointestinal side effects induced by metformin, comprising administering a therapeutically effective amount of metformin or a pharmaceutically acceptable salt thereof, in combination with a therapeutically effective amount of a DPP-IV inhibitor, preferably vildagliptin, or a pharmaceutically acceptable salt thereof, to a patient in need thereof.
摘要翻译：一种预防，延缓进展或减少由二甲双胍诱导的胃肠道疾病或胃肠道副作用的方法，包括给予治疗有效量的二甲双胍或其药学上可接受的盐与治疗有效量的DPP-IV抑制剂，优选维格列汀，或其药学上可接受的盐给有此需要的患者。

4. 发明申请

WO0196295A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO0196295A2
公开(公告)日：2001-12-20
申请号：PCT/EP0106595
申请日：2001-06-11
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , VILLHAUER EDWIN BERNARD
发明人： VILLHAUER EDWIN BERNARD
IPC分类号： A61K31/40 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/506 , A61P3/04 , A61P3/08 , A61P3/10 , A61P19/02 , A61P19/10 , A61P43/00 , C07D207/16 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12 , C07D417/14 , C07D207/00
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.
摘要翻译：本发明涉及游离形式或酸加成盐形式的某些其中Y如本文所定义的式（I）的N-（取代甘氨酰基）-2-氰基吡咯烷。式（I）化合物抑制DPP-IV（二肽基肽酶-IV）活性。因此，它们被指示用作抑制DPP-IV的药物和用于治疗由DPP-IV介导的病症，例如非胰岛素依赖性糖尿病，关节炎，肥胖症，骨质疏松症和葡萄糖耐量降低的其它病症。

5. 发明申请

WO2007019255A3 SALTS OF VILDAGLIPTIN 审中-公开
标题翻译：维拉胶的盐
公开(公告)号：WO2007019255A3
公开(公告)日：2007-05-31
申请号：PCT/US2006030335
申请日：2006-08-02
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , REBER JEAN-LOUIS , VILLHAUER EDWIN BERNARD
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.
摘要翻译：本发明涉及维格列汀（LAF237）的新型盐形式，即（S）-1 - [（3-羟基-1-金刚烷基）氨基]乙酰基-2-氰基 - 吡咯烷的盐形式。

6. 发明申请

WO9819998A3 N-substituted 2-cyanopyrrolidines 审中-公开
标题翻译： N-取代的2-氰基吡咯烷
公开(公告)号：WO9819998A3
公开(公告)日：1998-07-16
申请号：PCT/EP9706125
申请日：1997-11-05
申请人： NOVARTIS AG , VILLHAUER EDWIN BERNARD
发明人： VILLHAUER EDWIN BERNARD
IPC分类号： A61K31/40 , A61K31/401 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/505 , A61K31/506 , A61P3/00 , A61P3/10 , A61P43/00 , C07D207/16 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D207/16 , C07D403/12
摘要： N-(N'-substituted glycyl)-2-cyanopyrrolidines, e.g. the compounds of formula (I) wherein R has various significances, are novel. They 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.

7. 发明专利

JP2014088435A Combination comprising dipeptidyl peptidase-iv inhibitor and antidiabetic agent 有权
标题翻译：包含DIPEPTIDYL PEPTIDASE-IV抑制剂和抗生素的组合
公开(公告)号：JP2014088435A
公开(公告)日：2014-05-15
申请号：JP2014020963
申请日：2014-02-06
申请人： Novartis Ag , ノバルティスアーゲー
发明人： BALKAN BOERK , HUGHES THOMAS EDWARD , HOLMES DAVID GRENVILLE , VILLHAUER EDWIN BERNARD
IPC分类号： A61K45/06 , A61K31/00 , A61K31/155 , A61K31/198 , A61K31/40 , A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/4453 , A61K31/505 , A61K31/7036 , A61P3/00 , A61P3/04 , A61P3/10 , A61P19/02 , A61P19/10 , A61P29/00 , A61P43/00
CPC分类号： A61K45/06 , A61K31/00 , A61K31/4025 , A61K31/44 , A61K31/505 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a combination useful in prevention, progress retardation or treatment of dipeptidyl peptidase-IV inhibitor (DPP-IV) mediate condition, particularly diabetes, more particularly type 2 diabetes, impaired glucose tolerance (IGT), fasting blood sugar level abnormal condition, metabolic acidosis, ketosis, arthritis, obesity and osteoporosis.SOLUTION: A combination comprises a DPP-IV inhibitor and further at least one antidiabetic compound.
摘要翻译：要解决的问题：提供可用于预防，进展延迟或二肽基肽酶-IV抑制剂（DPP-IV）治疗的组合介导病症，特别是糖尿病，特别是2型糖尿病，葡萄糖耐量降低（IGT），空腹血糖水平异常情况，代谢性酸中毒，酮症，关节炎，肥胖症和骨质疏松症。解决方案：组合包含DPP-IV抑制剂和至少一种抗糖尿病化合物。

8. 发明专利

JP2011162550A Combination comprising dipeptidylpeptidase-iv inhibitor and antidiabetic agent 有权
标题翻译：包含DIPEPTIDYPEPTIDASE-IV抑制剂和抗生素的组合
公开(公告)号：JP2011162550A
公开(公告)日：2011-08-25
申请号：JP2011076253
申请日：2011-03-30
申请人： Novartis Ag , ノバルティスアーゲー
发明人： BALKAN BOERK , HUGHES THOMAS EDWARD , HOLMES DAVID GRENVILLE , VILLHAUER EDWIN BERNARD
IPC分类号： A61K45/06 , A61K31/00 , A61K31/155 , A61K31/198 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/4453 , A61K31/505 , A61K31/7036 , A61P3/00 , A61P3/04 , A61P3/10 , A61P19/02 , A61P19/10 , A61P29/00 , A61P43/00
CPC分类号： A61K45/06 , A61K31/00 , A61K31/4025 , A61K31/44 , A61K31/505 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a combination useful for the prevention, delay of progression or treatment of conditions mediated by dipeptidylpeptidase-IV inhibitor (DPP-IV), particularly diabetes, further particularly type 2 diabetes, impairment of glucose tolerance (IGT), conditions of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, obesity and osteoporosis.
SOLUTION: The combination includes a DPP-IV inhibitor and at least one further antidiabetic combination.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供可用于预防，延缓或治疗由二肽基肽酶-IV抑制剂（DPP-IV）介导的病症，特别是糖尿病，进一步特别是2型糖尿病，葡萄糖耐量降低（ IGT），空腹血浆葡萄糖受损的病症，代谢性酸中毒，酮症，关节炎，肥胖症和骨质疏松症。解决方案：该组合包括DPP-IV抑制剂和至少一种另外的抗糖尿病组合。版权所有（C）2011，JPO＆INPIT

9. 发明专利

JP2005112864A N-substituted 2-cyanopyrrolidine 审中-公开
标题翻译： N-取代的2-氰基吡咯烷酮
公开(公告)号：JP2005112864A
公开(公告)日：2005-04-28
申请号：JP2005008992
申请日：2005-01-17
申请人： Novartis Ag , ノバルティスアクチエンゲゼルシャフト
发明人： VILLHAUER EDWIN BERNARD
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4015 , A61P3/04 , A61P3/10 , A61P43/00 , C07D207/16
CPC分类号： C07D207/16
摘要： PROBLEM TO BE SOLVED: To provide a dipeptidyl-peptidase-IV (DPP-IV) inhibitor.
SOLUTION: A compound of formula (I) (wherein R is a substituted adamantyl; and (n) is 0 to 3) in free form or in acid addition salt form has DPP-IV (dipeptidyl-peptidase-IV) inhibitory activity. The compound is useful as a medicine for inhibiting DPP-IV and for 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.
COPYRIGHT: (C)2005,JPO&NCIPI

10. 发明专利

JP2017081994A ジペプチジルペプチダーゼ−ＩＶ阻害剤および抗糖尿病薬剤を含む組合せ物审中-公开
公开(公告)号：JP2017081994A
公开(公告)日：2017-05-18
申请号：JP2017007638
申请日：2017-01-19
申请人：ノバルティスアーゲー , Novartis Ag , ノバルティスアーゲー
发明人： BALKAN BOERK , HUGHES THOMAS EDWARD , HOLMES DAVID GRENVILLE , VILLHAUER EDWIN BERNARD
IPC分类号： A61K45/06 , A61K31/00 , A61K31/155 , A61K31/198 , A61K31/40 , A61K31/4025 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/4453 , A61K31/505 , A61K31/7036 , A61P3/00 , A61P3/04 , A61P3/10 , A61P19/02 , A61P19/10 , A61P29/00 , A61P43/00
CPC分类号： A61K45/06 , A61K31/00 , A61K31/4025 , A61K31/44 , A61K31/505 , A61K2300/00
摘要：【課題】ジペプチジルペプチダーゼ−IV阻害剤(DPP−IV)仲介状態、特に糖尿病、さらに特に2型糖尿病、耐糖能障害(IGT)、空腹時血糖値異常状態、代謝性アシドーシス、ケトーシス、関節炎、肥満および骨粗しょう症の予防、進行遅延または処置において有用な組合せ物を提供することが、本発明の課題である。【解決手段】上記課題は、DPP−IV阻害剤および少なくとも1つのさらなる抗糖尿病性化合物を含む組合せ物により解決される。【選択図】なし

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