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公开(公告)号：US08471027B2
公开(公告)日：2013-06-25
申请号：US13437984
申请日：2012-04-03
申请人： Adrian Wai-Hing Cheung , Kevin Richard Guertin , Nancy-Ellen Haynes , Eric Mertz , Lida Qi , Yimin Qian , Nathan Robert Scott
发明人： Adrian Wai-Hing Cheung , Kevin Richard Guertin , Nancy-Ellen Haynes , Eric Mertz , Lida Qi , Yimin Qian , Nathan Robert Scott
IPC分类号： C07D215/233 , C07D471/04
CPC分类号： C07D215/233 , C07D215/48 , C07D401/04 , C07D401/06 , C07D413/04 , C07D471/04
摘要： The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译： 本发明涉及JNK抑制剂和用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。 本申请公开了如下式I所述的JNK抑制剂：其中变量如本文所定义。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。
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公开(公告)号：US20120258982A1
公开(公告)日：2012-10-11
申请号：US13437984
申请日：2012-04-03
申请人： Adrian Wai-Hing Cheung , Kevin Richard Guertin , Nancy-Ellen Haynes , Eric Mertz , Lida Qi , Yimin Qian , Nathan Robert Scott
发明人： Adrian Wai-Hing Cheung , Kevin Richard Guertin , Nancy-Ellen Haynes , Eric Mertz , Lida Qi , Yimin Qian , Nathan Robert Scott
IPC分类号： A61K31/4375 , C07D215/233 , A61K31/47 , A61P19/02 , A61P11/06 , A61P13/12 , A61P25/28 , A61P25/16 , A61P9/10 , A61P35/00 , A61P35/02 , C07D471/04 , A61P3/10
CPC分类号： C07D215/233 , C07D215/48 , C07D401/04 , C07D401/06 , C07D413/04 , C07D471/04
摘要： The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译： 本发明涉及JNK抑制剂和用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。 本申请公开了如下式I所述的JNK抑制剂：其中变量如本文所定义。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。
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公开(公告)号：US08258134B2
公开(公告)日：2012-09-04
申请号：US12400319
申请日：2009-03-09
申请人： Steven Joseph Berthel , Nancy-Ellen Haynes , Robert Francis Kester , Lee Apostle McDermott , Yimin Qian , Ramakanth Sarabu , Nathan Robert Scott , Jefferson Wright Tilley
发明人： Steven Joseph Berthel , Nancy-Ellen Haynes , Robert Francis Kester , Lee Apostle McDermott , Yimin Qian , Ramakanth Sarabu , Nathan Robert Scott , Jefferson Wright Tilley
IPC分类号： C07D401/06 , C07D401/14 , C07D237/32 , C07D237/10 , A61K31/501 , A61K31/502 , A61P5/50
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D407/14
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗代谢疾病和病症，例如II型糖尿病。
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4.发明授权Adamantyl-pyrazole carboxamides as inhibitors of 11β-hdroxysteroid dehydrogenase 有权金刚烷基 - 吡唑甲酰胺作为11＆amp; - 类固醇脱氢酶的抑制剂公开(公告)号：US07728029B2
公开(公告)日：2010-06-01
申请号：US11717996
申请日：2007-03-14
申请人： Kevin William Anderson , Nader Fotouhi , Paul Gillespie , Robert Alan Goodnow, Jr. , Kevin Richard Guertin , Nancy-Ellen Haynes , Michael Paul Myers , Sherrie Lynn Pietranico-Cole , Lida Qi , Pamela Loreen Rossman , Nathan Robert Scott , Kshitij Chhabilbhai Thakkar , Jefferson Wright Tilley , Qiang Zhang
发明人： Kevin William Anderson , Nader Fotouhi , Paul Gillespie , Robert Alan Goodnow, Jr. , Kevin Richard Guertin , Nancy-Ellen Haynes , Michael Paul Myers , Sherrie Lynn Pietranico-Cole , Lida Qi , Pamela Loreen Rossman , Nathan Robert Scott , Kshitij Chhabilbhai Thakkar , Jefferson Wright Tilley , Qiang Zhang
IPC分类号： A61K31/4155 , A61K31/415 , A61K31/454 , A61K31/5377 , C07D231/14 , C07D401/04 , C07D413/04 , C07D403/04
CPC分类号： C07D403/04 , C07D231/12 , C07D231/16 , C07D231/38 , C07D401/04 , C07D403/02 , C07D407/14 , C07D413/04 , C07D417/04
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗疾病，例如II型糖尿病和代谢综合征。
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公开(公告)号：US20090264445A1
公开(公告)日：2009-10-22
申请号：US12400065
申请日：2009-03-09
申请人： Steven Joseph Berthel , John A. Brinkman , Stuart Hayden , Nancy-Ellen Haynes , Robert Francis Kester , Lee Apostle McDermott , Yimin Qian , Ramakanth Sarabu , Nathan Robert Scott , Jefferson Wright Tilley
发明人： Steven Joseph Berthel , John A. Brinkman , Stuart Hayden , Nancy-Ellen Haynes , Robert Francis Kester , Lee Apostle McDermott , Yimin Qian , Ramakanth Sarabu , Nathan Robert Scott , Jefferson Wright Tilley
IPC分类号： A61K31/497 , C07D403/12 , A61K31/4155
CPC分类号： C07D403/12 , C07D401/12 , C07D405/14 , C07D413/14 , C07D417/12
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗代谢疾病和病症，例如II型糖尿病。
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公开(公告)号：US20090005383A1
公开(公告)日：2009-01-01
申请号：US12194643
申请日：2008-08-20
申请人： Nancy-Ellen Haynes , Denis J. Kertesz , Sherrie Lynn Pietranico-Cole , Yimin Qian , Nathan Robert Scott , Sung-Sau So , Kshitij Chhabilbhai Thakkar , Jefferson Wright Tilley
发明人： Nancy-Ellen Haynes , Denis J. Kertesz , Sherrie Lynn Pietranico-Cole , Yimin Qian , Nathan Robert Scott , Sung-Sau So , Kshitij Chhabilbhai Thakkar , Jefferson Wright Tilley
IPC分类号： A61K31/50 , A61K31/53 , C07D403/10 , C07D237/14 , A61P3/00
CPC分类号： C07D237/14 , C07D237/16 , C07D237/18 , C07D403/10 , C07D403/12
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.
摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗诸如肥胖症，高脂血症，高胆固醇血症和糖尿病等疾病和疾病的疾病，并且可用于其它疾病如NASH，动脉粥样硬化，心血管疾病，甲状腺机能减退 ，甲状腺癌及其相关疾病和疾病。
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公开(公告)号：US07452882B2
公开(公告)日：2008-11-18
申请号：US11488870
申请日：2006-07-18
申请人： Nancy-Ellen Haynes , Denis J. Kertesz , Sherrie Lynn Pietranico-Cole , Yimin Qian , Nathan Robert Scott , Sung-Sau So , Kshitij Chhabilbhai Thakkar , Jefferson Wright Tilley
发明人： Nancy-Ellen Haynes , Denis J. Kertesz , Sherrie Lynn Pietranico-Cole , Yimin Qian , Nathan Robert Scott , Sung-Sau So , Kshitij Chhabilbhai Thakkar , Jefferson Wright Tilley
IPC分类号： A61K31/53 , C07D403/10 , C07D237/14 , C07D409/10 , A61P3/06
CPC分类号： C07D237/14 , C07D237/16 , C07D237/18 , C07D403/10 , C07D403/12
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.
摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗诸如肥胖症，高脂血症，高胆固醇血症和糖尿病等疾病和其它疾病和疾病的疾病，并且可用于其他疾病如NASH，动脉粥样硬化，心血管疾病，甲状腺机能减退 ，甲状腺癌及其相关疾病和疾病。
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公开(公告)号：US07223868B2
公开(公告)日：2007-05-29
申请号：US11098717
申请日：2005-04-04
申请人： Fred Thomas Bizzarro , Wendy Lea Corbett , Joseph Francis Grippo , Nancy-Ellen Haynes , George William Holland , Robert Francis Kester , Paige Erin Mahaney , Ramakanth Sarabu
发明人： Fred Thomas Bizzarro , Wendy Lea Corbett , Joseph Francis Grippo , Nancy-Ellen Haynes , George William Holland , Robert Francis Kester , Paige Erin Mahaney , Ramakanth Sarabu
IPC分类号： C07D213/75 , C07D213/84
CPC分类号： C07D213/75 , C07C275/50 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D213/80 , C07D213/82 , C07D233/88 , C07D237/20 , C07D237/22 , C07D239/42 , C07D239/47 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/56 , C07D277/58 , C07D285/135
摘要： 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
摘要翻译： 所述3-取代的N-取代的N-杂芳族丙酰胺，其3-位取代为取代苯基，2-位是甲基环烷基环，所述丙酰胺为增加胰岛素分泌的葡萄糖激酶活化剂 II型糖尿病
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公开(公告)号：US20070049632A1
公开(公告)日：2007-03-01
申请号：US11507080
申请日：2006-08-18
申请人： Bruce Banner , Joseph Bilotta , Nader Fotouhi , Paul Gillespie , Robert Goodnow , Matthew Hamilton , Nancy-Ellen Haynes , Agnieszka Kowalczyk , Alexander Mayweg , Michael Myers , Sherrie Pietranico-Cole , Nathan Scott , Kshitij Thakkar , Jefferson Tilley
发明人： Bruce Banner , Joseph Bilotta , Nader Fotouhi , Paul Gillespie , Robert Goodnow , Matthew Hamilton , Nancy-Ellen Haynes , Agnieszka Kowalczyk , Alexander Mayweg , Michael Myers , Sherrie Pietranico-Cole , Nathan Scott , Kshitij Thakkar , Jefferson Tilley
IPC分类号： A61K31/416 , C07D231/54
CPC分类号： C07D231/54
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗疾病，例如II型糖尿病和代谢综合征。
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公开(公告)号：US06951945B2
公开(公告)日：2005-10-04
申请号：US10616359
申请日：2003-07-09
申请人： Fred Thomas Bizzarro , Wendy Lea Corbett , Joseph Francis Grippo , Nancy-Ellen Haynes , George William Holland , Robert Francis Kester , Paige Erin Mahaney , Ramakanth Sarabu
发明人： Fred Thomas Bizzarro , Wendy Lea Corbett , Joseph Francis Grippo , Nancy-Ellen Haynes , George William Holland , Robert Francis Kester , Paige Erin Mahaney , Ramakanth Sarabu
IPC分类号： C07C275/50 , C07C317/44 , C07C323/62 , C07D213/75 , C07D213/80 , C07D213/82 , C07D233/88 , C07D237/22 , C07D239/42 , C07D241/20 , C07D241/28 , C07D253/07 , C07D261/14 , C07D263/48 , C07D277/18 , C07D277/38 , C07D277/46 , C07D277/56 , C07D277/58 , C07D285/12 , C07D285/135 , C07D285/06 , C07D275/02 , C07D277/04
CPC分类号： C07D213/75 , C07C275/50 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D213/80 , C07D213/82 , C07D233/88 , C07D237/20 , C07D237/22 , C07D239/42 , C07D239/47 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/56 , C07D277/58 , C07D285/135
摘要： 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
摘要翻译： 所述3-取代的N-取代的N-杂芳族丙酰胺，其3-位取代为取代苯基，2-位是甲基环烷基环，所述丙酰胺为增加胰岛素分泌的葡萄糖激酶活化剂 II型糖尿病
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