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1. 发明申请

US20110130402A1 HETEROAROMATIC GLUCOKINASE ACTIVATORS 审中-公开
标题翻译：异氟烷激酶
公开(公告)号：US20110130402A1
公开(公告)日：2011-06-02
申请号：US13022937
申请日：2011-02-08
申请人： Lone Jeppesen , Marit Kristiansen
发明人： Lone Jeppesen , Marit Kristiansen
IPC分类号： A61K31/426 , C07D277/46 , C07D417/12 , C07D417/04 , C07D277/54 , A61K31/496 , A61K31/5377 , A61K31/454 , A61P3/10
CPC分类号： C07D277/46 , C07D277/54
摘要： The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, 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 which increase insulin secretion for the treatment of type II diabetes.
摘要翻译：本发明描述了2,3-二取代的N-杂芳族丙酰胺，其中3-位上的取代是任选取代的苯环，2-位上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。丙酰胺是增加胰岛素分泌以治疗II型糖尿病的葡糖激酶激活剂。

2. 发明申请

US20090105482A1 Urea Glucokinase Activators 失效
标题翻译：尿素葡萄糖激酶活化剂
公开(公告)号：US20090105482A1
公开(公告)日：2009-04-23
申请号：US11994862
申请日：2006-07-14
申请人： Jesper Lau , Anthony Murray , Per Vedso , Marit Kristiansen , Lone Jeppesen
发明人： Jesper Lau , Anthony Murray , Per Vedso , Marit Kristiansen , Lone Jeppesen
IPC分类号： C07D277/54 , C07D285/135
CPC分类号： C07D277/48
摘要： The invention provides a compound of general formula (I) wherein the substituents are defined further 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。

3. 发明申请

US20080319028A1 Dicycloalkylcarbamoyl Ureas As Glucokinase Activators 失效
标题翻译：二环烷基氨基甲酰脲作为葡萄糖激酶活化剂
公开(公告)号：US20080319028A1
公开(公告)日：2008-12-25
申请号：US11994718
申请日：2006-07-07
申请人： Anthony Murray , Jesper Lau , Per Vedso , Lone Jeppesen , Marit Kristiansen
发明人： Anthony Murray , Jesper Lau , Per Vedso , Lone Jeppesen , Marit Kristiansen
IPC分类号： C07C275/62 , A61K31/175 , A61K31/4406 , C07D213/02 , C07D213/72 , A61K31/426 , A61P3/00 , A61P3/10
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。

4. 发明授权

US07192952B2 Heterocyclic compounds that are inhibitors of the enzyme DPP-IV 失效
标题翻译：作为DPP-IV酶抑制剂的杂环化合物
公开(公告)号：US07192952B2
公开(公告)日：2007-03-20
申请号：US11070056
申请日：2005-03-02
申请人： Anders Bendtz Kanstrup , Christian Klarner Sams , Jane Marie Lundbeck , Lise Brown Christiansen , Marit Kristiansen
发明人： Anders Bendtz Kanstrup , Christian Klarner Sams , Jane Marie Lundbeck , Lise Brown Christiansen , Marit Kristiansen
IPC分类号： C07D473/08 , C07D473/06 , A61K31/522 , A61K31/55 , A61P3/10
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
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

5. 发明申请

US20070054897A1 Heteroaryl-ureas and their use as glucokinase activators 有权
标题翻译：杂芳基和它们作为葡萄糖激酶活化剂的用途
公开(公告)号：US20070054897A1
公开(公告)日：2007-03-08
申请号：US11453330
申请日：2006-06-14
申请人： Anthony Murray , Jesper Lau , Lone Jeppesen , Per Vedso , Michael Ankersen , Jane Lundbeck , Marit Kristiansen , Maria Valcarce-Lopez , Dharma Polisetti , Govindan Subramanian , Robert Andrews , Daniel Christen , Jeremy Cooper , Kalpathy Santhosh
发明人： Anthony Murray , Jesper Lau , Lone Jeppesen , Per Vedso , Michael Ankersen , Jane Lundbeck , Marit Kristiansen , Maria Valcarce-Lopez , Dharma Polisetti , Govindan Subramanian , Robert Andrews , Daniel Christen , Jeremy Cooper , Kalpathy Santhosh
IPC分类号： A61K31/551 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/428 , C07D417/02
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 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：本发明涉及作为葡萄糖激酶活化剂的式（I）化合物，因此可用于治疗，治疗，控制或辅助治疗疾病，其中增加葡糖激酶活性是有益的。

6. 发明授权

US5952363A Pyrrolidine compounds useful in the treatment of diabetes 失效
标题翻译：可用于治疗糖尿病的吡咯烷类化合物
公开(公告)号：US5952363A
公开(公告)日：1999-09-14
申请号：US35494
申请日：1998-03-05
申请人： Marit Kristiansen , Palle Jakobsen , Jane Marie Lundbeck
发明人： Marit Kristiansen , Palle Jakobsen , Jane Marie Lundbeck
IPC分类号： C07D207/12 , A61K31/40 , C07D207/09 , C07D207/14
CPC分类号： C07D207/12
摘要： The present invention relates to novel pyrrolidine compounds having the general formula I ##STR1## and pharmaceutically acceptable acid addition salts or hydrates or prodrugs thereof, wherein R.sup.1 is straight or branched C.sub.1-14 -alkyl optionally substituted with C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkoxy, phenoxy, perhalomethyl, halogen, optionally substituted phenyl;CR.sup.2 is optionally C.dbd.R.sup.2 or C--R.sup.2R.sup.2 is oxygen, hydroxy, halogen, amino or mercapto,R.sup.3 and R.sup.4 independently are hydroxy, halogen, amino or mercapto, the use of these compounds as medicament, the use of these medicaments in the treatment of diabetes, pharmaceutical compositions containing these compounds and methods of preparing the compounds.
摘要翻译：本发明涉及具有通式I的新型吡咯烷化合物及其药学上可接受的酸加成盐或水合物或前药，其中R 1为任选被C 3-7 - 环烷基，C 1-6 - 烷氧基取代的直链或支链C 1-14 - 烷基，苯氧基，全卤代甲基，卤素，任选取代的苯基; C + Z R2任选是C = R 2或C-R 2 R 2是氧，羟基，卤素，氨基或巯基，R 3和R 4独立地是羟基，卤素，氨基或巯基，使用这些化合物作为药物，用于治疗糖尿病的药物，含有这些化合物的药物组合物和制备化合物的方法。

7. 发明授权

US5371080A Imidazoquinazoline compounds and their use 失效
标题翻译：咪唑喹唑啉化合物及其用途
公开(公告)号：US5371080A
公开(公告)日：1994-12-06
申请号：US991077
申请日：1992-12-15
申请人： Holger C. Hansen , Marit Kristiansen
发明人： Holger C. Hansen , Marit Kristiansen
IPC分类号： A61K31/505 , A61K31/535 , C07D487/04 , A61K31/54
CPC分类号： C07D487/04 , A61K31/505 , A61K31/535
摘要： Imidazoquinazoline compounds having the formula ##STR1## wherein Q is ##STR2## --COOR.sup.8 or --CN; wherein R.sup.1 is H, alkyl, unsubstituted or substituted cycloalkyl, alkoxy, alkoxyalkyl or CF.sub.3 ; R.sup.8 is alkyl; R.sup.2 and R.sup.3 independently are H, alkyl optionally substituted, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonylalkyl, formylalkyl, or an acetal thereof, or R.sup.2 and R.sup.3 together with the N-atom form a 4-6 membered monocyclic 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.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently are H, OH, halogen, CF.sub.3, NO.sub.2, NH.sub.2, 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是-COOR 8或-CN; 其中R1是H，烷基，未取代或取代的环烷基，烷氧基，烷氧基烷基或CF3; R8是烷基; R2和R3独立地是H，烷基任选取代的，羟基烷基，烷氧基，烷氧基烷基，烷氧基羰基烷基，甲酰基烷基或缩醛，或者R2和R3与N-原子一起形成4-6元单环氨基，其中环系一或更多的碳原子可以与N，O或S，亚磺酰基，磺酰基或羰基或其缩醛交换，这些环体系中的每一个任选被取代; R4，R5，R6和R7独立地是H，OH，卤素，CF3，NO2，NH2，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。

8. 发明授权

US5246935A Piperazinyl derivatives and methods of treating central nervous system ailments relating to the 5-HT.sub.2 receptor system 失效
标题翻译：哌嗪衍生物和治疗与5-HT2受体系统相关的中枢神经系统药物的方法
公开(公告)号：US5246935A
公开(公告)日：1993-09-21
申请号：US744556
申请日：1991-08-13
申请人： Lone Jeppesen , Marit Kristiansen , John B. Hansen
发明人： Lone Jeppesen , Marit Kristiansen , John B. Hansen
IPC分类号： A61K31/495 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/24 , A61P25/26 , C07D20060101 , C07D215/40 , C07D215/42 , C07D277/62 , C07D277/82 , C07D295/08 , C07D295/084 , C07D295/088 , C07D295/13 , C07D317/50 , C07D317/66 , C07D319/08 , C07D319/18 , C07D321/10 , C07D405/12 , C07D471/04
CPC分类号： C07D277/62 , C07D295/088 , C07D295/13 , C07D317/66 , C07D319/18
摘要： Piperazinyl derivatives of the general formula I ##STR1## wherein R.sup.1 represents substituted phenyl, 1- or 2-diazanaphthyl, azadiazanaphtyl or diazanaphtyl groups; n is 1, 2, 3 or 4; X is --O-- or ##STR2## wherein R.sup.2 is hydrogen, C.sub.1-6 -alkyl or C.sub.3-8 -cycloalkyl; Y is .dbd.O or .dbd.S or .dbd.NZ wherein Z is hydrogen, C.sub.1-6 -alkyl or --CN and R.sup.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.sub.2 receptor, the 5-HT.sub.1A receptor, the alpha.sub.1 receptor the dopamine receptor or a combination of these and may therefore be useful for treating CNS system, cardiovascular system and gastrointestinal disorders.
摘要翻译：通式I（I）的哌嗪基衍生物，其中R 1表示取代的苯基，1-或2-二氮萘基，氮杂二萘甲酰基或二氮萘基; n为1,2,3或4; X是-O-或者其中R 2是氢，C 1-6 - 烷基或C 3-8 - 环烷基; Y是= O或= S或= NZ，其中Z是氢，C 1-6 - 烷基或-CN，并且R 3选自由各种结构组成的组，其表现出对各种受体亚型的高亲和力，包括5-HT2 受体，5-HT 1A受体，α1受体多巴胺受体或其组合，因此可用于治疗CNS系统，心血管系统和胃肠道疾病。

9. 发明授权

US07999114B2 Dicycloalkylcarbamoyl ureas as glucokinase activators 失效
标题翻译：二环烷基氨基甲酰脲作为葡糖激酶活化剂
公开(公告)号：US07999114B2
公开(公告)日：2011-08-16
申请号：US11994718
申请日：2006-07-07
申请人： Anthony Murray , Jesper Lau , Per Vedso , Lone Jeppesen , Marit Kristiansen
发明人： Anthony Murray , Jesper Lau , Per Vedso , Lone Jeppesen , Marit Kristiansen
IPC分类号： C07D277/00 , A61K31/425
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。

10. 发明授权

US07598391B2 Heteroaryl-ureas and their use as glucokinase activators 有权
标题翻译：杂芳基和它们作为葡萄糖激酶活化剂的用途
公开(公告)号：US07598391B2
公开(公告)日：2009-10-06
申请号：US11453330
申请日：2006-06-14
申请人： Anthony Murray , Jesper Lau , Lone Jeppesen , Per Vedsø , Michael Ankersen , Jane Marie Lundbeck , Marit Kristiansen , Maria Carmen Valcarce-Lopez , Dharma Rao Polisetti , Govindan Subramanian , Robert Carl Andrews , Daniel P. Christen , Jeremy T. Cooper , Kalpathy Chidambareswaran Santhosh
发明人： Anthony Murray , Jesper Lau , Lone Jeppesen , Per Vedsø , Michael Ankersen , Jane Marie Lundbeck , Marit Kristiansen , Maria Carmen Valcarce-Lopez , Dharma Rao Polisetti , Govindan Subramanian , Robert Carl Andrews , Daniel P. Christen , Jeremy T. Cooper , Kalpathy Chidambareswaran Santhosh
IPC分类号： C07D277/26
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 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：本发明涉及作为葡萄糖激酶活化剂的式（I）化合物，因此可用于治疗，治疗，控制或辅助治疗疾病，其中增加葡糖激酶活性是有益的。

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