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1. 发明申请

WO2007019255A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2007019255A2
公开(公告)日：2007-02-15
申请号：PCT/US2006/030335
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。

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

WO2006031959A1 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：通过用有机硼酸衍生物和本方法的异构体反应8-羟基-1,7-萘啶衍生物制备6,8取代的1,7-萘啶衍生物的方法
公开(公告)号：WO2006031959A1
公开(公告)日：2006-03-23
申请号：PCT/US2005/032909
申请日：2005-09-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , JIANG, Xinglong , KAPA, Prasad, Koteswara , LEE, George, Tien-San , VILLHAUER, Edwin, Bernard
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 R 1 is C 1 -C 20 -alkyl optionally substituted by one or two of hydroxy, C 3 -C 12 cycloalkyl, C 6 -C 12 -aryl, C 1 -C 7 -alkoxy, thiol, C 1 -C 7 -alkylthio or carboxy, or R 1 is C 3 -C 12 -cycloalkyl optionally substituted by one or two of C 1 -C 7 -alkyl, hydroxy, C 1 C 7 -alkoxy, C I -C 7 -alkylthio or carboxy, or R 1 is C 6 -C 12 -aryl optionally substituted by one, two, three or four substituents selected from C 1 -C 7 -alkyl, halo; hydroxy, C 1 -C 7 -alkoxy, C 1 -C 7 -alkylthio and nitro, or R 1 is heteroaryl optionally substituted by C 1 -C 7 - alkyl, C l -C 7 -alkoxy or halo; R 2 and R 3 are independently hydrogen or C 1 -C 20 -alkoxy; R 4 is C 6 -C 12 -aryl optionally substituted by one, two, three or four substituents selected from C 1 -C 7 -alkyl, halo, hydroxy, C 1 -C 7 -alkoxy, C 1 -C 7 -alkylthio and nitro, or R 4 is heteroaryl optionally substituted by C 1 -C 7 ,- alkyl, C 1 -C 7 -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 R 6 and R 7 are hydrogen or, C 1 -C 7 -alkyl, or R 6 and R 7 combined are C 2 -C 3 alkylene optionally substituted by one or two of C 1 -C 4 -alkyl that together with the boron and the oxygen atoms form a 5- or 6-membered ring.
摘要翻译：制备式（I）化合物的方法，其中R 1是任选被一个或两个取代的C 1 -C 20 -C 20 - 烷基的羟基，C 3 -C 12环烷基，C 6 -C 12 - 芳基，C 1 -C 12 - C 1 -C 7 - 烷氧基，硫醇，C 1 -C 7 - 烷硫基或羧基，或R 1 任选被C 1 -C 7烷基中的一个或两个取代的C 3 -C 12 - 环烷基，烷基，羟基，C 1 -C 7 - 烷氧基，C 1 -C 7 - 烷硫基或C 1 -C 6 - 羧基或R 1是任选被一个，两个，三个或四个选自C

4. 发明申请

WO2006005613A1 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抑制剂和调节5-HT3和/或5-HT4受体的化合物的组合
公开(公告)号：WO2006005613A1
公开(公告)日：2006-01-19
申请号：PCT/EP2005/007636
申请日：2005-07-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , VILLHAUER, Edwin, Bernard
发明人： VILLHAUER, Edwin, Bernard
IPC分类号： A61K31/40
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-HT 3 receptor and/or an agent interacting with 5HT 4 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.
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的组合制剂或药物组合物，并且包含至少一种治疗剂，所述治疗剂选自与5-HT _{3受体和/或与5HT 4受体相互作用的试剂或其药学上可接受的盐。本发明还涉及这种组合用于预防，延缓进展或治疗选自胰岛素抵抗，葡萄糖代谢异常，葡萄糖耐量降低的病症，空腹血糖降低的病症，糖尿病特别是2型糖尿病，肥胖症，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，糖尿病性神经病，勃起功能障碍，经前期综合征，冠心病，高血压，心绞痛，心肌梗塞，中风，血管再狭窄，皮肤和结缔组织障碍，足部溃疡和溃疡性结肠炎，内皮功能障碍和受损的血管依从性，改变的胃肠蠕动，敏感性和/或分泌障碍，其包括但不限于胃灼热，腹胀，术后肠梗阻，腹痛和不适，早期饱腹感，上腹部疼痛，恶心，呕吐，浑浊，反胃，肠假手术，肛门失禁，GERD，IBS，消化不良，慢性便秘或腹泻，糖尿病性胃病，胃轻瘫等。糖尿病胃轻瘫，溃疡性结肠炎，克罗恩病，溃疡和与其相关的内脏疼痛。}

5. 发明申请

WO2002072146A3 COMBINATION OF NATEGLINIDE OR REPAGLINIDE WITH AT LEAST ONE FURTHER ANTIDIABETIC COMPOUND 审中-公开
公开(公告)号：WO2002072146A3
公开(公告)日：2002-09-19
申请号：PCT/EP2002/002665
申请日：2002-03-11
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , VILLHAUER, Edwin, Bernard
发明人： VILLHAUER, Edwin, Bernard
IPC分类号： A61K45/06
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.

6. 发明申请

WO2012047948A1 NEW CRYSTALLINE FORMS OF THE SODIUM SALT OF (4- {4- [5- ( 6 - TRIFLUOROMETHYL - PYRIDIN- 3 - YLAMINO ) - PYRIDIN- 2 -YL] -PHENYL} - CYCLOHEXYL) -ACETIC ACID 审中-公开
标题翻译：（4- {4- [5-（6-三氟甲基 - 吡啶-3-基）氨基] - 吡啶-2-基] - 苯基} - 环己基） - 酸的钠盐的新晶体形式
公开(公告)号：WO2012047948A1
公开(公告)日：2012-04-12
申请号：PCT/US2011/054841
申请日：2011-10-05
申请人： NOVARTIS AG , SUTTON, Paul, Allen , GIRGIS, Michael, J. , LIANG, Jessica , PRASHAD, Mahavir , VILLHAUER, Edwin, Bernard
发明人： SUTTON, Paul, Allen , GIRGIS, Michael, J. , LIANG, Jessica , PRASHAD, Mahavir , VILLHAUER, Edwin, Bernard
IPC分类号： C07D401/12 , A61K31/415 , A61P3/04
CPC分类号： C07D401/12 , A61K31/444 , A61K45/06 , C07D213/72
摘要： The present invention relates to novel crystalline forms of (4-{4-[5-(6-Trifluoromethyl-pyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid, sodium and their use in the treatment or prevention of a condition or a disorder associated with DGAT1 activity in animals, particularly humans. It also relates processes for making such novel crystalline forms.
摘要翻译：本发明涉及（4- {4- [5-（6-三氟甲基 - 吡啶-3-基氨基） - 吡啶-2-基] - 苯基} - 环己基） - 乙酸的新型结晶形式及其用途在治疗或预防与动物，特别是人类中DGAT1活性相关的疾病或病症。它还涉及制备这种新型结晶形式的方法。

7. 发明申请

WO2002072146A2 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：WO2002072146A2
公开(公告)日：2002-09-19
申请号：PCT/EP2002/002665
申请日：2002-03-11
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , VILLHAUER, Edwin, Bernard
发明人： VILLHAUER, Edwin, Bernard
IPC分类号： A61K45/06
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.
摘要翻译：本发明涉及有机化合物的组合，其包含至少两种抗糖尿病药物，优选具有不同的作用模式，其中活性成分在每种情况下以游离形式或以药学上可接受的盐形式存在，并且任选地，至少在药学上可接受的载体上，用于同时，分开或顺序使用。

8. 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.

9. 发明授权

EP1296974B1 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：EP1296974B1
公开(公告)日：2009-08-05
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.

10. 发明授权

EP1137635B1 N-SUBSTITUTED 2-CYANOPYRROLIDINES 有权转让
标题翻译： N-取代的2-氰基吡咯烷类
公开(公告)号：EP1137635B1
公开(公告)日：2005-10-19
申请号：EP99959396.5
申请日：1999-12-09
申请人： Novartis AG , Novartis Pharma GmbH
发明人： VILLHAUER, Edwin, Bernard
IPC分类号： C07D207/16 , A61K31/401 , A61P3/10
CPC分类号： C07D207/16

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