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公开(公告)号：US07235538B2
公开(公告)日：2007-06-26
申请号：US10621302
申请日：2003-07-17
申请人： Anders Bendtz Kanstrup , Lise Brown Christiansen , Jane Marie Lundbeck , Christian K. Sams , Marit Kristiansen
发明人： Anders Bendtz Kanstrup , Lise Brown Christiansen , Jane Marie Lundbeck , Christian K. Sams , Marit Kristiansen
IPC分类号： A61K31/522 , A61K3/10 , A61K3/04 , C07D473/08 , C07D473/06
CPC分类号： C07D473/04 , C07D473/08
摘要： The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3, R6, R7, R9, and R10 are defined herein. The present invention also relates to pharmaceutical compositions comprising the compounds of formula I and the use of the compounds 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： 本发明涉及酶DPP-IV的治疗活性和选择性抑制剂，其具有式I，其中每个n独立地为一个或两个，R 1，R 2， R 3，R 6，R 7，R 9，R 9和R 10， >在本文中定义。 本发明还涉及包含式I化合物的药物组合物和该化合物用于治疗与通过DPP-IV失活的蛋白质例如2型糖尿病和肥胖相关的疾病的用途。
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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
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公开(公告)号：US06869947B2
公开(公告)日：2005-03-22
申请号：US10186498
申请日：2002-06-28
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： A61P3/10 , C07D473/00 , C07D473/02 , C07D473/08 , A61K31/522 , A61K31/55 , C07D473/06
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
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4.发明授权公开(公告)号：US06645995B2
公开(公告)日：2003-11-11
申请号：US10076577
申请日：2002-02-08
IPC分类号： A61K314025
CPC分类号： C07D401/06 , A61K31/00 , A61K31/40 , A61K31/44 , A61K31/4439 , C07D207/16 , C07D207/22 , C07D401/12 , C07D403/06 , C07D417/06
摘要： Described are compounds of formula I wherein at least one of the bonds in the five-membered ring is a double bond; B is any alpha or beta amino acid connected to the ring with an amide or peptide bond; or a salt thereof with a pharmaceutically acceptable acid or base. Pharmaceutical compositions containing these compounds are also described. These compounds are useful for treating type II diabetes.
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5.发明授权Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV 失效作为DPP-IV酶抑制剂的治疗活性和选择性杂环化合物公开(公告)号：US06380398B2
公开(公告)日：2002-04-30
申请号：US09767354
申请日：2001-01-23
IPC分类号： C07D20718
CPC分类号： C07D401/06 , A61K31/00 , A61K31/40 , A61K31/44 , A61K31/4439 , C07D207/16 , C07D207/22 , C07D401/12 , C07D403/06 , C07D417/06
摘要： Described are compounds of formula I wherein at least one of the bonds in the five-membered ring is a double bond; B is any alpha or beta amino acid connected to the ring with an amide or peptide bond; or a salt thereof with a pharmaceutically acceptable acid or base. Pharmaceutical compositions containing these compounds are also described. These compounds are useful for treating type II diabetes.
摘要翻译： 描述的是式I的化合物，其中五元环中的至少一个键是双键; B是与酰胺或肽键连接到环上的任何α或β氨基酸; 或其盐与药学上可接受的酸或碱反应。 还描述了含有这些化合物的药物组合物。 这些化合物可用于治疗II型糖尿病。
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公开(公告)号：US07872139B2
公开(公告)日：2011-01-18
申请号：US12188402
申请日：2008-08-08
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 Chidambareswaram 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 Chidambareswaram Santhosh
IPC分类号： C07D417/06
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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公开(公告)号：US20100204288A1
公开(公告)日：2010-08-12
申请号：US12757217
申请日：2010-04-09
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： A61K31/426 , C07D277/54 , A61P3/10 , A61P3/06 , A61P9/12
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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公开(公告)号：US06590118B1
公开(公告)日：2003-07-08
申请号：US09672460
申请日：2000-09-28
IPC分类号： C07C25500
CPC分类号： C07D209/48 , C07C205/38 , C07C205/57 , C07C233/75 , C07C235/56 , C07C235/64 , C07C235/78 , C07C235/84 , C07C237/42 , C07C255/54 , C07C255/57 , C07C309/42 , C07C311/21 , C07C317/44 , C07C317/50 , C07C323/62 , C07D213/81 , C07D213/82 , C07D257/04 , C07D307/68 , C07D307/79 , C07D317/68 , C07D333/24 , C07D333/38 , C07F9/3834 , C07F9/4021
摘要： Disclosed are compounds of formula I wherein A, R1, R2, R3, R4 and R5 are described in the specification, pharmaceutical formulations comprising these compounds, the use of these compounds are medicaments, the use of these medicaments in the treatment of and/or prevention of diabetes, especially non-insulin dependent diabetes (NIDDM or Type 2 diabetes), as well as methods for treating diabetes comprising administration of these compounds.
摘要翻译： 公开了式I的化合物，其中A，R 1，R 2，R 3，R 4和R 5在本说明书中描述，包含这些化合物的药物制剂，这些化合物的用途是药物，这些药物在治疗和/或预防中的用途 的糖尿病，特别是非胰岛素依赖性糖尿病（NIDDM或2型糖尿病），以及治疗糖尿病的方法，包括给予这些化合物。
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公开(公告)号：US5952363A
公开(公告)日：1999-09-14
申请号：US35494
申请日：1998-03-05
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。
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公开(公告)号：US08263634B2
公开(公告)日：2012-09-11
申请号：US12942297
申请日：2010-11-09
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 Chidambareswarak 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 Chidambareswarak Santhosh
IPC分类号： A61K31/426 , A61P3/10 , A61P3/04 , A61P3/06 , A61P9/12
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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