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1.发明申请ARYL LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 有权芳基链接的咪唑和三唑衍生物及其用于改善药物药代动力学的方法公开(公告)号：US20160297809A1
公开(公告)日：2016-10-13
申请号：US15036274
申请日：2014-11-07
申请人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Chun Sing Li , Tingting Yu
发明人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Chun Sing Li , Tingting Yu
IPC分类号： C07D417/14 , C07D417/12 , A61K31/496 , C07D487/04 , A61K31/4985 , A61K31/4439 , A61K31/427 , C07D401/12 , C07D405/14 , A61K31/4178 , C07D403/10 , A61K31/5377 , A61K31/4545 , C07D401/14 , A61K45/06 , A61K31/4725
CPC分类号： C07D417/14 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
摘要翻译： 本发明涉及芳基连接的咪唑和三唑衍生物，包含所述化合物单独或与其它药物组合的组合物，以及使用该化合物改善药物药代动力学的方法。 本发明的化合物可用于抑制CYP3A4的人和兽医药物，并且用于改善由CYP3A4代谢的治疗化合物的药代动力学。
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公开(公告)号：US20150266895A1
公开(公告)日：2015-09-24
申请号：US14431462
申请日：2013-09-26
申请人： Kevin J. WILSON , David J. WITTER , Phieng SILIPHAIVANH , Kathryn KIPFORD , David SLOMAN , Danielle FALCONE , Brendan O'BOYLE , Umar Faruk MANSOOR , Jongwon LIM , Joey L. METHOT , Christopher BOYCE , Lei CHEN , Matthew H. DANIELS , Salem FEVRIER , Xianhai HUANG , Ravi KURUKULASURIYA , Ling TONG , Wei ZHOU , Joseph KOZLOWSKI , Milana M. MALETIC , Bidhan A. SHINKRE , Jayanth Thiruvellore THATAI , Raman Kumar BAKSHI , Ganesh Babu KARUNAKARAN , MERCK SHARP & DOHME CORP.
发明人： Kevin J. Wilson , David J. Witter , Phieng Siliphaivanh , Kathryn Lipford , David Sloman , Danielle Falcone , Brendan O'Boyle , Umar Faruk Mansoor , Jongwon Lim , Joey L. Methot , Christopher Boyce , Lei Chen , Matthew H. Daniels , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Ling Tong , Wei Zhou , Joseph Kozlowski , Milana M. Maletic , Bidhan A. Shinkre , Jayanth Thiruvellore Thatai , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号： C07D498/18 , A61K31/437 , A61K31/5377 , A61K31/496 , A61K45/06 , A61K31/4375 , C07D498/14 , A61K31/553 , C07D519/00 , C07D471/04 , C07D471/14
CPC分类号： C07D498/18 , A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/16 , C07D498/14 , C07D498/16 , C07D519/00 , A61K2300/00
摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译： 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。
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公开(公告)号：US10745377B2
公开(公告)日：2020-08-18
申请号：US15036268
申请日：2014-11-07
申请人： MERCK SHARP & DOHME CORP. , Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Tingting Yu , Richard Soll
发明人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Tingting Yu , Richard Soll
IPC分类号： A61K31/4178 , A61K31/4439 , A61K31/4436 , A61K31/443 , A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/496 , C07D401/06 , C07D401/14 , C07D401/04 , C07D403/06 , C07D403/14 , C07D409/06 , C07D413/04 , C07D417/04 , A61K45/06 , A61K31/454 , C07D405/14 , C07D413/14 , C07D417/14 , C07D249/08 , C07D233/61 , A61P31/18 , C07D213/14 , C07D471/04 , A61K31/4545 , C07D471/10
摘要： The present invention relates to piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
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公开(公告)号：US20160068532A1
公开(公告)日：2016-03-10
申请号：US14787280
申请日：2014-04-25
申请人： Jongwon LIM , Xianhai HUANG , Ronald D. FERGUSON , Wei ZHOU , Christopher W. BOYCE , Phieng SILIPHAIVANH , David J. WITTER , Milana M. MALETIC , Joseph A. KOZLOWSKI , Kevin J. WILSON , MERCK SHARP & DOHME CORP.
发明人： Jongwon Lim , Xianhai Huang , Ronald D. Ferguson , Wei Zhou , Christopher W. Boyce , Phieng Siliphaivanh , David J. Witter , Milana M. Maletic , Joseph A. Kozlowski , Kevin J. Wilson
IPC分类号： C07D487/04 , C07D471/14 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要： Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).
摘要翻译： 公开了式（I）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（I）化合物治疗癌症的方法。 本发明还提供了包含有效量的至少一种式（I）化合物和药学上可接受的载体的药物组合物。 本发明还提供一种药物组合物，其包含有效量的至少一种式（I）化合物和有效量的至少一种其它药学活性成分（例如化学治疗剂）和药学上可接受的载体 。 本发明还提供了在需要这种治疗的患者中抑制ERK（即，抑制ERK2的活性）的方法，包括向所述患者施用有效量的至少一种式（I）化合物。
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5.发明申请PIPERIDINE OR PIPERAZINE LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 审中-公开哌啶或哌嗪联结的咪唑和三唑衍生物及其用于改善药物药代动力学的方法公开(公告)号：US20160297792A1
公开(公告)日：2016-10-13
申请号：US15036268
申请日：2014-11-07
申请人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Tingting Yu , Richard Soll
发明人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Tingting Yu , Richard Soll
IPC分类号： C07D401/06 , C07D417/14 , C07D405/14 , C07D413/14 , A61K31/4545 , A61K45/06 , A61K31/4178 , C07D403/06 , A61K31/551 , C07D471/10 , A61K31/541 , A61K31/454 , C07D401/14
摘要： The present invention relates to piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
摘要翻译： 本发明涉及哌啶或哌嗪连接的咪唑和三唑衍生物，包含所述化合物单独或与其它药物组合的组合物，以及使用该化合物改善药物药代动力学的方法。 本发明的化合物可用于抑制CYP3A4的人和兽医药物，并且用于改善由CYP3A4代谢的治疗化合物的药代动力学。
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公开(公告)号：US09023865B2
公开(公告)日：2015-05-05
申请号：US14353381
申请日：2012-10-25
申请人： Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
发明人： Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
IPC分类号： C07D401/14 , A61K31/437 , C07D471/04 , C07D519/00 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D519/00
摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译： 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。
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7.发明授权Triazole derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase-1 有权作为11-β-羟基类固醇脱氢酶-1抑制剂的三唑衍生物公开(公告)号：US07504402B2
公开(公告)日：2009-03-17
申请号：US11011889
申请日：2004-12-14
申请人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
发明人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
IPC分类号： A61K31/4196 , C07D249/08 , C07D401/04 , C07D403/04 , C07D413/02
CPC分类号： C07D249/08 , C07D401/04 , C07D403/04 , C07D403/08 , C07D405/04 , C07D409/04 , C07D413/08 , C07D417/08
摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
摘要翻译： 结构式I的三唑衍生物是11b-羟基类固醇脱氢酶-1的选择性抑制剂。 该化合物可用于治疗糖尿病，例如非胰岛素依赖性糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，血脂异常，高脂血症，高血压，代谢综合征和与NIDDM相关的其他症状。
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公开(公告)号：US06849636B2
公开(公告)日：2005-02-01
申请号：US10739716
申请日：2003-12-18
申请人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
发明人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
IPC分类号： A61K31/4196 , A61P3/10 , C07D249/00 , C07D249/08 , C07D401/04 , C07D403/04 , C07D403/08 , C07D405/04 , C07D409/04 , C07D413/02 , C07D413/08 , C07D417/08
CPC分类号： C07D249/08 , C07D401/04 , C07D403/04 , C07D403/08 , C07D405/04 , C07D409/04 , C07D413/08 , C07D417/08
摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
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9.发明授权Triazole derivatives as inhibitors of 11-β hydroxysteroid dehydrogenase-1 有权作为11-和bgr的抑制剂的三唑衍生物 羟基类固醇脱氢酶-1公开(公告)号：US08026264B2
公开(公告)日：2011-09-27
申请号：US10558454
申请日：2004-05-26
申请人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
发明人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
IPC分类号： A61K31/4196 , C07D249/08
CPC分类号： C07D249/08 , C07D249/16 , C07D413/08 , C07D487/04
摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
摘要翻译： 结构式I的三唑衍生物是11-羟基类固醇脱氢酶-1的选择性抑制剂。 该化合物可用于治疗糖尿病，例如非胰岛素依赖性糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，血脂异常，高脂血症，高血压，代谢综合征和与NIDDM相关的其他症状。
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10.发明申请TRIAZOLE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1 审中-公开作为11-羟基脱氢酶脱氢酶-1的抑制剂的三唑衍生物公开(公告)号：US20090181994A1
公开(公告)日：2009-07-16
申请号：US12364902
申请日：2009-02-03
申请人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
发明人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
IPC分类号： A61K31/4196 , C07D249/08 , A61K31/506 , A61P25/28
CPC分类号： C07D249/08 , C07D401/04 , C07D403/04 , C07D403/08 , C07D405/04 , C07D409/04 , C07D413/08 , C07D417/08
摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
摘要翻译： 结构式I的三唑衍生物是11b-羟基类固醇脱氢酶-1的选择性抑制剂。 该化合物可用于治疗糖尿病，例如非胰岛素依赖性糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，血脂异常，高脂血症，高血压，代谢综合征和与NIDDM相关的其他症状。
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