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1. 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

2. 发明专利

JP2010090173A Combination of dpp iv inhibitor and 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：JP2010090173A
公开(公告)日：2010-04-22
申请号：JP2010010967
申请日：2010-01-21
申请人： Novartis Ag , ノバルティスアーゲー
发明人： HOLMES DAVID GRENVILLE , SHETTY SURAJ SHIVAPPA , HUGHES THOMAS EDWARD
IPC分类号： A61K45/06 , A61K31/16 , A61K31/40 , A61K31/401 , A61K31/41 , A61K31/4439 , A61K31/454 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/14 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/10 , A61P17/00 , A61P19/04 , A61P27/02 , A61P27/06 , A61P27/12 , A61P43/00
CPC分类号： A61K31/454 , A61K31/16 , A61K31/40 , A61K31/41
摘要： PROBLEM TO BE SOLVED: To provide a combined medicine which is effective for the prevention, delay of progress or treatment of malady and disease.
SOLUTION: A combination contains a DPP IV inhibitor and a cardiovascular compound effective for the prevention, delay of progress or treatment of malady and disease selected from the group consisting of hyperpiesia, congested heart failure, left ventricular hypertrophy, peripheral arterial disease, diabetes, especially type 2 diabetes, diabetic retinopathy, macular degeneration, cataract, diabetic nephropathy, glomerulosclerosis, chronic kidney failure, diabetic neuropathy, syndrome X, premenstrual syndrome, coronary heart disease, angina cordis, thrombosis, arterial sclerosis, myocardial infarction, transient ischemic attack, apoplexy, vascular restenosis, hyperglycaemia, hyperinsulinemia, hyperlipidemia, hypertriglyceridemia, insulin resistance, impaired glucose metabolism, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, obesity, erectile dysfunction, disease of skin and connective tissue, podalic tumor formation and chronic ulcerative colitis, endothelium dysfunction and impaired vascular compliance.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供一种有效预防，延缓进展或治疗疾病和疾病的联合药物。解决方案：组合包含DPP IV抑制剂和心血管化合物，其有效预防，延迟进展或治疗疾病和疾病，其选自高血压，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，糖尿病性肾病，肾小球硬化，慢性肾功能衰竭，糖尿病性神经病变，X综合征，经前综合征，冠心病，心绞痛，血栓形成，动脉硬化，心肌梗死，攻击，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，葡萄糖代谢受损，葡萄糖耐量降低的病症，空腹血糖异常，肥胖症，勃起功能障碍，皮肤病和结缔组织疾病，扁桃体肿瘤形成和慢性溃疡性大肠杆菌 Tis，内皮功能障碍和血管依从性受损。版权所有（C）2010，JPO＆INPIT

3. 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。

4. 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

5. 发明专利

JP2010155866A Use of substituted cyanopyrrolidine and combination preparation containing them for treating hyperlipidemia and associated disease 审中-公开
标题翻译：使用取代的氰基吡咯烷和组合制剂，用于治疗高脂血症和相关疾病
公开(公告)号：JP2010155866A
公开(公告)日：2010-07-15
申请号：JP2010087181
申请日：2010-04-05
申请人： Novartis Ag , ノバルティスアーゲー
发明人： HOLMES DAVID GRENVILLE , HUGHES THOMAS EDWARD
IPC分类号： A61K31/40 , C07D207/16 , A61K31/015 , A61K31/05 , A61K31/20 , A61K31/22 , A61K31/355 , A61K31/366 , A61K31/375 , A61K31/401 , A61K31/405 , A61K31/4415 , A61K31/455 , A61K31/616 , A61K31/714 , A61K45/00 , A61K45/06 , A61P3/06 , A61P9/10
CPC分类号： A61K31/401 , A61K31/40 , A61K45/06 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a method and a composition 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.
SOLUTION: A composition including a compound of formula (I) wherein R is substituted adamantyl; and n is 0 to 3, and the use thereof are provided.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供用于治疗高脂血症的方法和组合物及其相关的病症，例如CHD，缺血性中风，血管成形术后的再狭窄，外周血管疾病，间歇性跛行，心肌梗塞（例如坏死和凋亡）），血脂异常和餐后脂肪血症。解决方案：包含其中R是取代金刚烷基的式（I）化合物的组合物; n为0〜3，提供使用。版权所有（C）2010，JPO＆INPIT

6. 发明专利

JP2014159436A Use of dipeptidyl peptidase iv inhibitors 有权
标题翻译：西酞菁肽抑制剂的使用
公开(公告)号：JP2014159436A
公开(公告)日：2014-09-04
申请号：JP2014075331
申请日：2014-04-01
申请人： Novartis Ag , ノバルティスアーゲー
发明人： PRATLEY RICHARD , FOLEY JAMES E , HUGHES THOMAS EDWARD
IPC分类号： A61K45/00 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/403 , A61K31/426 , A61K31/4427 , A61K31/4439 , A61K31/472 , A61K31/4985 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12
CPC分类号： A61K31/403 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/426 , A61K31/4439 , A61K31/472 , A61K31/4985
摘要： PROBLEM TO BE SOLVED: To provide pharmaceuticals for the treatment of cardiovascular diseases or damage, renal diseases or damage, heart failure, or heart failure associated diseases, without causing side effects.SOLUTION: The invention provides use of a dipeptidyl peptidase IV inhibitor (DPP-IV inhibitor), preferably, 1-{2-[(5-cyanopyridin-2-yl)amino]ethylamino}acetyl-2(S)-cyano-pyrrolidine dihydrochloride, (S)-1-[(3-hydroxy-1-adamantyl)amino]acetyl-2-cyano-pyrrolidine, L-threo-isoleucyl thiazolidine (P32/98), MK-0431, GSK23A, BMS-477118, etc.
摘要翻译：要解决的问题：提供用于治疗心血管疾病或损伤，肾脏疾病或损伤，心力衰竭或心力衰竭相关疾病的药物，而不引起副作用。解决方案：本发明提供了二肽基肽酶IV抑制剂（DPP -IV抑制剂），优选1- {2 - [（5-氰基吡啶-2-基）氨基]乙基氨基}乙酰基-2（S） - 氰基 - 吡咯烷二盐酸盐，（S）-1 - [（3-羟基 - 1-金刚烷基）氨基]乙酰基-2-氰基 - 吡咯烷，L-苏式 - 异亮氨酰基噻唑烷（P32 / 98），MK-0431，GSK23A，BMS-477118等

7. 发明专利

JP2012211146A Use of dipeptidyl peptidase iv inhibitor 审中-公开
标题翻译：西酞菁肽抑制剂的使用
公开(公告)号：JP2012211146A
公开(公告)日：2012-11-01
申请号：JP2012123284
申请日：2012-05-30
申请人： Novartis Ag , ノバルティスアーゲー
发明人： PRATLEY RICHARD , FOLEY JAMES E , HUGHES THOMAS EDWARD
IPC分类号： A61K45/00 , A61K31/00 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/426 , A61K31/4439 , A61K31/472 , A61K31/4985 , A61K38/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , C07D207/16 , C07D217/24 , C07D277/04 , C07D401/12 , C07D487/04
CPC分类号： A61K31/403 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/426 , A61K31/4439 , A61K31/472 , A61K31/4985
摘要： PROBLEM TO BE SOLVED: To provide a method for the prevention, the delay in progression or the treatment of cardiovascular diseases or damages, renal diseases or damages, heart failure, or heart failure associated diseases.SOLUTION: There is provided the use of a Dipeptidyl peptidase IV inhibitor (DPP-IV inhibitor), preferably (S)-1-[(3-hydroxy-1-adamantyl)amino] acetyl-2-cyano-pyrrolidine, L-threo-isoleucyl thiazolidine (P32/98), MK-0431, GSK23A, BMS-477118, 3-(aminomethyl)-2-isobuthyl-1-oxo-4- phenyl-1,2-dihydro-6-isoquinolinecarboxamide and 2-{[3-(aminomethyl)-2-isobutyl-4-phenyl-1-oxo-1,2-dihydro-6-isoquinolyl]oxy}acetamide or a pharmaceutically acceptable salt thereof.
摘要翻译：要解决的问题：提供预防，延迟进展或治疗心血管疾病或损伤，肾脏疾病或损伤，心力衰竭或心力衰竭相关疾病的方法。提供了二肽基肽酶IV抑制剂（DPP-IV抑制剂），优选（S）-1 - [（3-羟基-1-金刚烷基）氨基]乙酰基-2-氰基 - 吡咯烷的用途， L-苏氨基异亮氨酰基噻唑烷（P32 / 98），MK-0431，GSK23A，BMS-477118,3-（氨基甲基）-2-异丁基-1-氧代-4-苯基-1,2-二氢-6-异喹啉甲酰胺和 2- [3-（氨基甲基）-2-异丁基-4-苯基-1-氧代-1,2-二氢-6-异喹啉基]氧基}乙酰胺或其药学上可接受的盐。版权所有（C）2013，JPO＆INPIT

8. 发明专利

JP2011116772A 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：JP2011116772A
公开(公告)日：2011-06-16
申请号：JP2011045331
申请日：2011-03-02
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： A61K45/00 , A61K31/00 , A61K31/155 , A61K31/192 , A61K31/194 , A61K31/198 , A61K31/216 , A61K31/225 , A61K31/28 , A61K31/365 , A61K31/40 , A61K31/4025 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/4453 , A61K31/505 , A61K31/64 , 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： PROBLEM TO BE SOLVED: To provide a combination useful 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. SOLUTION: The combination is provided which comprises a DPP-IV inhibitor and at least one further antidiabetic compound. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供可用于预防，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，更特别是2型糖尿病的病症的组合，受损的病症葡萄糖耐量（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：提供了包含DPP-IV抑制剂和至少一种其它抗糖尿病化合物的组合。版权所有（C）2011，JPO＆INPIT

9. 发明专利

JP2006273873A Combinations comprising dipeptidyl peptidase-iv inhibitor and antidiabetic agents 审中-公开
标题翻译：包含DIPEPTIDYL PEPTIDASE-IV抑制剂和抗生素的组合
公开(公告)号：JP2006273873A
公开(公告)日：2006-10-12
申请号：JP2006189416
申请日：2006-07-10
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： 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 that is useful for the prevention, progress delay and treatment of the mediating state of the dipeptidyl-peptidase IV inhibitor (DPP-IV), particularly diabetes, further particularly diabetes type 2, trouble or disorder of glucose tolerance (IGT), fasting blood sugar damage, metabolic acidosis, ketosis, adiposis, osteoporosis. SOLUTION: These problems can be dissolved by combining the DPP-IV inhibitor with at least one of the antidiabetic compounds. COPYRIGHT: (C)2007,JPO&INPIT

10. 发明申请

WO2007041368A3 DPP IV INHIBITOR FOR USE IN THE TREATMENT OF AUTOIMMUNE DISEASES AND GRAFT REJECTION 审中-公开
标题翻译： DPP IV抑制剂用于治疗自身免疫性疾病和死亡抑制
公开(公告)号：WO2007041368A3
公开(公告)日：2007-10-25
申请号：PCT/US2006038203
申请日：2006-09-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ALLISON MALCOLM , BURKEY BRYAN , HUGHES THOMAS EDWARD , KEMP DANIEL MATTHEW
发明人： ALLISON MALCOLM , BURKEY BRYAN , HUGHES THOMAS EDWARD , KEMP DANIEL MATTHEW
IPC分类号： A61K31/40 , A61P3/10 , A61P17/06 , A61P37/06
CPC分类号： A61K45/06 , A61K31/40 , 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 immunosuppressive or immunomodulator 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 that may be inhibited by DPP IV inhibition, for the prevention, delay of progression or treatment of autoimmune diseases, and the disorders associated therewith, or for the prevention, delay of progression or treatment of graft rejection.
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并且包含至少一种免疫抑制剂或免疫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DPP IV抑制可能被抑制的疾病和病症，用于预防，延缓进展或治疗自身免疫性疾病以及所述疾病或用于预防，延缓进展或治疗移植排斥反应。

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