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1.发明申请CYCLOHEXYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 有权作为11-羟基脱氢酶脱氢酶抑制剂的环己基取代的吡咯烷酮公开(公告)号：US20090239911A1
公开(公告)日：2009-09-24
申请号：US12297877
申请日：2007-04-24
申请人： Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Jeremy Schulenburg York , Alexei Pavlovych Krasutsky
发明人： Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Jeremy Schulenburg York , Alexei Pavlovych Krasutsky
IPC分类号： A61K31/4439 , C07D207/12 , A61K31/40 , C07D231/10 , A61K31/415 , C07D401/02 , A61P3/10
CPC分类号： C07D207/26 , C07D401/10 , C07D403/10
摘要： The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11β-HSD 1型拮抗剂活性的式I化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征和与11beta-HSD 1型相关的其它病症的方法 活动。
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2.发明申请BIPHENYL AMIDE LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 有权作为11-羟基脱氢酶脱氢酶1的抑制剂的二苯胺衍生物衍生物公开(公告)号：US20090156571A1
公开(公告)日：2009-06-18
申请号：US12297349
申请日：2007-04-19
申请人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
发明人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
IPC分类号： A61K31/453 , C07D405/14 , C07D403/08 , C07D413/08 , C07D417/08 , A61K31/497 , A61K31/5377 , A61K31/541 , A61K31/553
CPC分类号： C07D207/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
摘要： The present invention discloses novel compounds of Formula I: possessing 11 β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11个β-HSD 1型拮抗剂活性的新颖的式I化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍和与11β相关的其它病症的方法 -HSD类型1活动。
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3.发明授权Biphenyl amide lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 有权联苯酰胺内酰胺衍生物作为11-β-羟基类固醇脱氢酶的抑制剂1公开(公告)号：US08088776B2
公开(公告)日：2012-01-03
申请号：US12297349
申请日：2007-04-19
申请人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
发明人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
IPC分类号： A61K31/496 , A61K31/453 , C07D403/02 , C07D405/14
CPC分类号： C07D207/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
摘要： The present invention discloses novel compounds of Formula I: possessing 11 β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11＆amp; b -HSD 1型拮抗剂活性的式I化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍以及与其相关的其它病症的方法 ; -HSD 1型活动。
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4.发明授权Cyclohexyl substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 有权环己基取代的吡咯烷酮作为11-β-羟基类固醇脱氢酶的抑制剂1公开(公告)号：US07998999B2
公开(公告)日：2011-08-16
申请号：US12297877
申请日：2007-04-24
申请人： Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Jeremy Schulenburg York , Alexei Pavlovych Krasutsky
发明人： Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Jeremy Schulenburg York , Alexei Pavlovych Krasutsky
IPC分类号： A61K31/4015 , C07D207/26
CPC分类号： C07D207/26 , C07D401/10 , C07D403/10
摘要： The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11＆amp; b -HSD 1型拮抗剂活性的新颖的式I化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征以及与其相关的其它病症的方法。 1活动。
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5.发明申请SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 失效取代的吡咯烷酮作为11-羟基脱氢酶脱氢酶1的抑制剂公开(公告)号：US20090069326A1
公开(公告)日：2009-03-12
申请号：US12297969
申请日：2007-04-23
申请人： John Gordon Allen , Alexei Pavlovych Krasutsky , Owen Brendan Wallace , Yanping Xu , Jeremy Schulenburg York
发明人： John Gordon Allen , Alexei Pavlovych Krasutsky , Owen Brendan Wallace , Yanping Xu , Jeremy Schulenburg York
IPC分类号： A61K31/5377 , C07D207/46 , A61K31/4015 , C07D401/08 , A61K31/454 , A61P3/10 , C07D403/08 , A61K31/497 , C07D413/08
CPC分类号： C07D207/26 , C07D401/10
摘要： The present invention discloses novel compounds of Formula I: (I) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了新的式I化合物：（I）具有11β-HSD 1型拮抗剂活性，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍以及与其相关的其它病症的方法。 HSD 1型活动。
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6.发明授权Substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 失效取代的吡咯烷酮作为11-β-羟基类固醇脱氢酶1的抑制剂公开(公告)号：US07816349B2
公开(公告)日：2010-10-19
申请号：US12297969
申请日：2007-04-23
申请人： John Gordon Allen , Alexei Pavlovych Krasutsky , Owen Brendan Wallace , Yanping Xu , Jeremy Schulenburg York
发明人： John Gordon Allen , Alexei Pavlovych Krasutsky , Owen Brendan Wallace , Yanping Xu , Jeremy Schulenburg York
IPC分类号： A61K31/54 , A61K31/535 , A61K31/445 , A61K31/497 , C07D401/10 , C07D403/10 , C07D413/10 , C07D417/10
CPC分类号： C07D207/26 , C07D401/10
摘要： The present invention discloses novel compounds of Formula I: (I) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了新颖的式I化合物：（I）具有11＆amp; -HSD 1型拮抗剂活性，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍以及与其相关的其它病症的方法。 -HSD类型1活动。
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7.发明申请PIERIDINYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 失效作为11-羟基脱氢酶脱氢酶1的抑制剂的狄氏剂替代吡咯烷酮公开(公告)号：US20090088430A1
公开(公告)日：2009-04-02
申请号：US12297951
申请日：2007-04-27
IPC分类号： A61K31/454 , C07D401/04 , C07D401/14 , C07D413/14 , A61P3/10 , A61K31/5377 , A61K31/496 , A61K31/4545
CPC分类号： C07D401/04
摘要： The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11β-HSD 1型拮抗剂活性的式I化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征和与11beta-HSD 1型相关的其它病症的方法 活动。
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8.发明授权Piperidinyl substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 失效哌啶基取代的吡咯烷酮作为11-β-羟基类固醇脱氢酶1的抑制剂公开(公告)号：US07829582B2
公开(公告)日：2010-11-09
申请号：US12297951
申请日：2007-04-27
IPC分类号： A61K31/445 , C07D211/56 , C07D211/92
CPC分类号： C07D401/04
摘要： The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11＆amp; b -HSD 1型拮抗剂活性的新颖的式I化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征以及与其相关的其它病症的方法。 1活动。
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公开(公告)号：US07608639B2
公开(公告)日：2009-10-27
申请号：US10571961
申请日：2004-10-08
IPC分类号： A61K31/44 , C07D211/92
CPC分类号： C07D213/30 , C07C59/68 , C07C59/70 , C07C59/90 , C07C317/22 , C07C323/52 , C07D213/64 , C07D213/643 , C07D213/69 , C07D239/26
摘要： The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR), such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物，水合物或立体异构体，其可用于治疗或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，例如综合征X ，II型糖尿病，高血糖症，高脂血症，肥胖症，凝血病，高血压，动脉硬化以及与X综合症和心血管疾病相关的其它疾病。
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公开(公告)号：US06743794B2
公开(公告)日：2004-06-01
申请号：US10130800
申请日：2002-05-21
申请人： Rosanne Bonjouklian , Jeffrey Daniel Cohen , Joseph Michael Gruber , Douglas Webb Johnson , Louis Nickolaus Jungheim , Julian Stanley Kroin , Peter Ambrose Lander , Ho-Shen Lin , Mark Christopher Lohman , Brian Stephen Muehl , Bryan Hurst Norman , Vinod Francis Patel , Michael Enrico Richett , Kenneth Jeff Thrasher , Sreenivasarao Vepachedu , Wesley Todd White , Yongping Xie , Jeremy Schulenburg York , Brandon Lee Parkhurst , Qiupang Wang
发明人： Rosanne Bonjouklian , Jeffrey Daniel Cohen , Joseph Michael Gruber , Douglas Webb Johnson , Louis Nickolaus Jungheim , Julian Stanley Kroin , Peter Ambrose Lander , Ho-Shen Lin , Mark Christopher Lohman , Brian Stephen Muehl , Bryan Hurst Norman , Vinod Francis Patel , Michael Enrico Richett , Kenneth Jeff Thrasher , Sreenivasarao Vepachedu , Wesley Todd White , Yongping Xie , Jeremy Schulenburg York , Brandon Lee Parkhurst , Qiupang Wang
IPC分类号： A61K31496
CPC分类号： C07D471/04
摘要： The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).
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