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1. 发明申请

WO2007006761A1 DICYCLOALKYLCARBAMOYL UREAS AS GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：WO2007006761A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/064028
申请日：2006-07-07
申请人： NOVO NORDISK A/S , MURRAY, Anthony , LAU, Jesper , VEDSØ, Per , JEPPESEN, Lone , KRISTIANSEN, Marit
发明人： MURRAY, Anthony , LAU, Jesper , VEDSØ, Per , JEPPESEN, Lone , KRISTIANSEN, Marit
IPC分类号： C07C275/14 , C07C275/52 , C07C275/62 , A61K31/33
CPC分类号： C07C275/62 , C07C2601/02 , C07C2601/14
摘要： This invention relates to dicycloalkylcarbamoyl ureas of formula (I), which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
摘要翻译：本发明涉及式（I）的二环烷基氨基甲酰基脲，其为葡糖激酶的活化剂，因此可用于治疗，治疗，控制或辅助治疗疾病，其中葡萄糖激酶活性增加是有益的。

2. 发明申请

WO2007006760A1 DICYCLOALKYL UREA GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：WO2007006760A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/064026
申请日：2006-07-07
申请人： NOVO NORDISK A/S , MURRAY, Anthony , LAU, Jesper , VEDSØ, Per , KRISTIANSEN, Marit , JEPPESEN, Lone
发明人： MURRAY, Anthony , LAU, Jesper , VEDSØ, Per , KRISTIANSEN, Marit , JEPPESEN, Lone
IPC分类号： C07D277/48 , C07D417/12 , C07D417/04 , C07D417/14 , C07D277/54 , A61K31/426 , A61K31/427 , A61P3/10
CPC分类号： C07D277/54 , C07D277/48 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes. (I)
摘要翻译：二环烷基脲葡糖激酶活化剂化合物是可用于治疗糖尿病的葡糖激酶抑制剂。（一世）

3. 发明申请

WO2005066145A1 HETEROARYL-UREAS AND THEIR USE AS GLUCOKINASE ACTIVATORS 审中-公开
标题翻译： HETEROARYL-UREAS及其作为GLUCOKINASE激活剂的用途
公开(公告)号：WO2005066145A1
公开(公告)日：2005-07-21
申请号：PCT/DK2005/000002
申请日：2005-01-06
申请人： NOVO NORDISK A/S , MURRAY, Anthony , LAU, Jesper , JEPPESEN, Lone , VEDSØ, Per , ANKERSEN, Michael , LUNDBECK, Jane, Marie , KRISTIANSEN, Marit , VALCARCE-LOPEZ, Maria Carmen , POLISETTI, Dharma, Rao , SUBRAMANIAN, Govindan , ANDREWS, Robert, Carl , CHRISTEN, Daniel, P. , COOPER, Jeremy, T. , SANTHOSH, Kalpathy, Chidambareswaran
发明人： MURRAY, Anthony , LAU, Jesper , JEPPESEN, Lone , VEDSØ, Per , ANKERSEN, Michael , LUNDBECK, Jane, Marie , KRISTIANSEN, Marit , VALCARCE-LOPEZ, Maria Carmen , POLISETTI, Dharma, Rao , SUBRAMANIAN, Govindan , ANDREWS, Robert, Carl , CHRISTEN, Daniel, P. , COOPER, Jeremy, T. , SANTHOSH, Kalpathy, Chidambareswaran
IPC分类号： C07D277/48
CPC分类号： C07D417/12 , A61K31/4168 , A61K31/427 , A61K31/433 , C07D213/75 , C07D233/88 , C07D241/20 , C07D261/14 , C07D271/08 , C07D277/48 , C07D277/56 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/135 , C07D417/04 , C07D417/06 , C07D417/14 , C07D513/04
摘要： This invention relates to compounds that are of formula (I) wherein A is heteroaryl and R 1 and R 2 are both cyclic residues, that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial .
摘要翻译：本发明涉及式（I）化合物，其中A是杂芳基，R 1和R 2都是环状残基，其是葡糖激酶的活化剂，因此可用于治疗，治疗，对照或疾病的辅助治疗，其中增加葡萄糖激酶活性是有益的。

4. 发明申请

WO2007006814A1 UREA GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：WO2007006814A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/064289
申请日：2006-07-14
申请人： NOVO NORDISK A/S , LAU, Jesper , MURRAY, Anthony , VEDSØ, Per , KRISTIANSEN, Marit , JEPPESEN, Lone
发明人： LAU, Jesper , MURRAY, Anthony , VEDSØ, Per , KRISTIANSEN, Marit , JEPPESEN, Lone
IPC分类号： C07D277/48 , C07D285/08 , C07D285/12 , A61K31/426
CPC分类号： C07D277/48
摘要： The invention provides a compound of general formula (I) wherein the substituents are defined futher in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.
摘要翻译：本发明提供了一种通式（I）的化合物，其中取代基在本申请中进一步定义，以及在所附实施方案中描述的其它实施方案。本发明还提供本发明化合物用于制备用于治疗各种疾病的药物的用途，例如，用于治疗2型糖尿病。

5. 发明申请

WO2006058923A1 HETEROAROMATIC GLUCOKINASE ACTIVATORS 审中-公开
标题翻译：异氟烷激酶
公开(公告)号：WO2006058923A1
公开(公告)日：2006-06-08
申请号：PCT/EP2005/056473
申请日：2005-12-05
申请人： NOVO NORDISK A/S , JEPPESEN, Lone , KRISTIANSEN, Marit
发明人： JEPPESEN, Lone , KRISTIANSEN, Marit
IPC分类号： C07D277/46 , C07D277/54 , A61K31/426 , A61P3/10
CPC分类号： C07D277/46 , C07D277/54
摘要： The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, of Formula (I) wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators for the treatment of type II diabetes.
摘要翻译：本发明描述了式（I）的2,3-二取代的N-杂芳族丙酰胺，其中3位的取代是任选取代的苯环，并且2-位的取代是烷基或环烷基; 包含它们的药物组合物; 及其使用方法。丙酰胺是用于治疗II型糖尿病的葡萄糖激酶激活剂。

6. 发明申请

WO2004089362A1 2-CYANOPYRROLES AND THEIR ANALOGUES AS DDP-IV INHIBITORS 审中-公开
标题翻译：作为DDP-IV抑制剂的2-氰基吡咯及其类似物
公开(公告)号：WO2004089362A1
公开(公告)日：2004-10-21
申请号：PCT/DK2004/000232
申请日：2004-04-02
申请人： NOVO NORDISK A/S , KANSTRUP, Anders, Bendtz , LUNDBECK, Jane, Marie , CHRISTIANSEN, Lise, Brown , KRISTIANSEN, Marit , CHRISTENSEN, Leif , CHRISTENSEN, Inge, Thøger , BOWLER, Andrew, Neil
发明人： KANSTRUP, Anders, Bendtz , LUNDBECK, Jane, Marie , CHRISTIANSEN, Lise, Brown , KRISTIANSEN, Marit , CHRISTENSEN, Leif , CHRISTENSEN, Inge, Thøger , BOWLER, Andrew, Neil
IPC分类号： A61K31/4025
CPC分类号： C07D401/06 , C07D207/16 , C07D403/06 , C07D405/06 , C07D409/06
摘要： The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV having the formula I: (I) The invention furthermore relates to pharmaceutical compositions comprising the compounds and the use of such compounds for the manufacture of medicaments for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.
摘要翻译：本发明涉及具有式I的DPP-IV酶的治疗活性和选择性抑制剂：（I）本发明还涉及包含该化合物的药物组合物和该化合物在制备用于治疗疾病的药物中的用途与通过DPP-IV失活的蛋白质相关，例如2型糖尿病和肥胖症。

7. 发明申请

WO2004037233A2 USE OF GLYCOGEN PHOSPHORYLASE INHIBITORS FOR TREATMENT OF CARDIOVASCULAR DISEASES 审中-公开
标题翻译：糖原磷酸化酶抑制剂在心血管疾病治疗中的应用
公开(公告)号：WO2004037233A2
公开(公告)日：2004-05-06
申请号：PCT/DK2003/000695
申请日：2003-10-14
申请人： NOVO NORDISK A/S
发明人： RYTVED, Klaus, Asger , DRAGSTED, Nils , NYBORG, Niels, Chresten, Berg, , IVERSEN, Lars , KRISTIANSEN, Marit
IPC分类号： A61K31/00
CPC分类号： A61K45/06 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K2300/00
摘要： Methods and uses for the treatment of cardiac and cardiovascular diseases comprising administration of a glycogen phosphorylase inhibitor to a patient in need thereof.
摘要翻译：用于治疗心脏和心血管疾病的方法和用途，包括向有此需要的患者施用糖原磷酸化酶抑制剂。

8. 发明申请

WO1992003426A1 PIPERAZINYL DERIVATIVES 审中-公开
标题翻译：哌嗪衍生物
公开(公告)号：WO1992003426A1
公开(公告)日：1992-03-05
申请号：PCT/DK1991000244
申请日：1991-08-23
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , JEPPESEN, Lone , KRISTIANSEN, Marit , HANSEN, John, Bondo
IPC分类号： C07D295/084
CPC分类号： C07D277/62 , C07D295/088 , C07D295/13 , C07D317/66 , C07D319/18
摘要： Piperazinyl derivatives of general formula (I) wherein R1 represents substituted phenyl, 1- or 2-naphthyl, azanaphtyl or diazanaphtyl groups; n is 1, 2, 3 or 4; X is -O- or (1) wherein R2 is hydrogen, C¿1-6?-alkyl or C3-8-cycloalkyl; Y is =O or =S or =NZ wherein Z is hydrogen, C1-6-alkyl or -CN and R?3¿ is selected from a group consisting of various structures have been found to exhibit high affinity for various receptor subtypes including the 5-HT¿2? receptor, the 5-HT1A receptor, the alpha1 receptor, the dopamine receptor or a combination of these and may therefore be useful for treating CNS system, cardiovascular system and gastrointestinal disorders.

9. 发明申请

WO2003004496A1 DPP-IV-INHIBITING PURINE DERIVATIVES FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：用于治疗糖尿病的DPP-IV抑制嘌呤衍生物
公开(公告)号：WO2003004496A1
公开(公告)日：2003-01-16
申请号：PCT/DK2002/000439
申请日：2002-06-27
申请人： NOVO NORDISK A/S
发明人： KANSTRUP, Anders, Bendtz , SAMS, Christian, Klarner , LUNDBECK, Jane, Marie , CHRISTIANSEN, Lise, Brown , KRISTIANSEN, Marit
IPC分类号： C07D473/08
CPC分类号： C07D473/00 , C07D473/02
摘要： The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. (I)
摘要翻译：本发明涉及式I的DPP-IV酶的治疗活性和选择性抑制剂，包含该化合物的药物组合物和这些化合物在制备用于治疗与被灭活的蛋白质相关的疾病的药物中的用途通过DPP-IV，如2型糖尿病和肥胖。（一世）

10. 发明申请

WO1993013103A1 IMIDAZOQUINAZOLINE COMPOUNDS AND THEIR PREPARATION AND USE 审中-公开
标题翻译：咪唑烷腈化合物及其制备和使用
公开(公告)号：WO1993013103A1
公开(公告)日：1993-07-08
申请号：PCT/DK1992000385
申请日：1992-12-18
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , HANSEN, Holger, Claus , KRISTIANSEN, Marit
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/505 , A61K31/535
摘要： Imidazoquinazoline compounds having formula (I), wherein Q is (a), (b), (c), or (d) -COOR or -CN; wherein R is H, alkyl, unsubstituted or substituted cycloalkyl, alkoxy, alkoxyalkyl or CF3; R is alkyl; R and R independently are H, alkyl optionally substituted, cycloalkyl, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonylalkyl, formylalkyl, or an acetal thereof, or R and R together with the N-atom form a 4-6 membered cyclic amino group in which ring system one or more of the carbon atoms may be exchanged with N,O or S, sulphinyl, sulphonyl or carbonyl or an acetal thereof, each of these ring systems optionally being substituted; R , R , R and R independently are H, OH, halogen, CF3 NO2, NH2, CN, alkyl, alkenyl, alkynyl, alkoxy, alkoxyalkyl or alkoxycarbonyl. The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, antipsychotics, antiemetics, in improving the cognitive function of the brain of mammals, or as benzodiazepine antagonists.
摘要翻译：具有式（I）的咪唑并喹唑啉化合物，其中Q为（a），（b），（c）或（d）-COOR 8或-CN; 其中R 1是H，烷基，未取代或取代的环烷基，烷氧基，烷氧基烷基或CF 3; R 8是烷基; R 2和R 3独立地是H，任选取代的烷基，环烷基，羟基烷基，烷氧基，烷氧基烷基，烷氧基羰基烷基，甲酰基烷基或其缩醛，或R 2和R 3与N-原子形成4-6元环状氨基，其中一个或多个碳原子的一个或多个可以与N，O或S，亚磺酰基，磺酰基或羰基或其缩醛交换，这些环系中的每一个任选被取代; R 4，R 5，R 6和R 7独立地是H，OH，卤素，CF 3 NO 2，NH 2，CN，烷基，烯基，炔基，烷氧基，烷氧基烷基或烷氧基羰基。这些化合物可用作精神药物制剂，如抗惊厥药，抗焦虑药，催眠药，抗精神病药，止吐药，改善哺乳动物脑部认知功能或作为苯二氮卓类药物。

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