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公开(公告)号:US06503949B1
公开(公告)日:2003-01-07
申请号:US09572553
申请日:2000-05-16
申请人: Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Josef Vagner , Inge Thøger Christensen , Behrend Frederik Lundt , Ulla Grove Sidelmann , Henning Thøgersen , Anthony L. Ling , Michael Bruno Plewe , Larry Kenneth Truesdale , Shenghua Shi
发明人: Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Josef Vagner , Inge Thøger Christensen , Behrend Frederik Lundt , Ulla Grove Sidelmann , Henning Thøgersen , Anthony L. Ling , Michael Bruno Plewe , Larry Kenneth Truesdale , Shenghua Shi
IPC分类号: A01N3718
CPC分类号: C07D209/48 , C07B2200/07 , C07C237/36 , C07C237/42 , C07C243/38 , C07C271/56 , C07C271/58 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/42 , C07C275/60 , C07C275/62 , C07C311/47 , C07C317/22 , C07C317/32 , C07C317/42 , C07C323/21 , C07C323/44 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2603/18 , C07C2603/68 , C07C2603/94 , C07D209/08 , C07D211/58 , C07D213/75 , C07D215/38 , C07D231/40 , C07D235/30 , C07D257/06 , C07D277/72 , C07D295/13 , C07D295/135 , C07D307/68 , C07D317/66 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/60 , C07D333/68 , C07D333/70 , C07D409/12 , C07D417/12 , C07D487/04
摘要: Disclosed is a novel class of compounds of formula (I) wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
摘要翻译: 公开了一类新的式(I)化合物,其中V,A,Y,Z,R 1,E,X和D如说明书中所定义。 这些化合物用于拮抗胰高血糖素激素对胰高血糖素受体的作用。 由于其拮抗胰高血糖素受体的作用,该化合物适用于治疗或预防胰高血糖素介导的病症和疾病如高血糖症,1型糖尿病,2型糖尿病和肥胖症。
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公开(公告)号:US06875760B2
公开(公告)日:2005-04-05
申请号:US10233851
申请日:2002-08-30
申请人: Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Inge Thøger Christensen , Behrend Frederik Lundt , Ulla Grove Sidelmann , Henning Thøgersen , Anthony L. Ling , Michael Bruno Plewe , Larry Kenneth Truesdale , Anker Steen Jøgensen , Janos Tibor Kodra , Shenghua Shi
发明人: Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Inge Thøger Christensen , Behrend Frederik Lundt , Ulla Grove Sidelmann , Henning Thøgersen , Anthony L. Ling , Michael Bruno Plewe , Larry Kenneth Truesdale , Anker Steen Jøgensen , Janos Tibor Kodra , Shenghua Shi
IPC分类号: C07C237/36 , C07C237/42 , C07C243/38 , C07C271/56 , C07C271/58 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/42 , C07C275/60 , C07C275/62 , C07C311/47 , C07C317/22 , C07C317/32 , C07C317/42 , C07C323/21 , C07C323/44 , C07D209/08 , C07D209/48 , C07D211/58 , C07D213/75 , C07D215/38 , C07D231/40 , C07D235/30 , C07D257/06 , C07D277/72 , C07D295/13 , C07D295/135 , C07D307/68 , C07D317/66 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/60 , C07D333/68 , C07D333/70 , C07D409/12 , C07D417/12 , C07D487/04 , A61K31/33 , A61K31/695 , C07D257/00
CPC分类号: C07D209/48 , C07B2200/07 , C07C237/36 , C07C237/42 , C07C243/38 , C07C271/56 , C07C271/58 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/42 , C07C275/60 , C07C275/62 , C07C311/47 , C07C317/22 , C07C317/32 , C07C317/42 , C07C323/21 , C07C323/44 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2603/18 , C07C2603/68 , C07C2603/94 , C07D209/08 , C07D211/58 , C07D213/75 , C07D215/38 , C07D231/40 , C07D235/30 , C07D257/06 , C07D277/72 , C07D295/13 , C07D295/135 , C07D307/68 , C07D317/66 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/60 , C07D333/68 , C07D333/70 , C07D409/12 , C07D417/12 , C07D487/04
摘要: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
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公开(公告)号:US20090143592A1
公开(公告)日:2009-06-04
申请号:US11949075
申请日:2007-12-03
申请人: Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Josef Vagner , Inge Thoger Christensen , Behrend Frederik Lundt , Ulla Grove Sidelmann , Henning Thogersen , Anthony L. Ling , Michael Bruno Plewe , Larry Kenneth Truesdale , Anker Steen Jogensen , Janos Tibor Kodra , Shenghua Shi
发明人: Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Josef Vagner , Inge Thoger Christensen , Behrend Frederik Lundt , Ulla Grove Sidelmann , Henning Thogersen , Anthony L. Ling , Michael Bruno Plewe , Larry Kenneth Truesdale , Anker Steen Jogensen , Janos Tibor Kodra , Shenghua Shi
IPC分类号: C07D211/88 , C07D257/06 , C07D333/24 , C07C57/62
CPC分类号: C07D209/48 , C07B2200/07 , C07C237/36 , C07C237/42 , C07C243/38 , C07C271/56 , C07C271/58 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/42 , C07C275/60 , C07C275/62 , C07C311/47 , C07C317/22 , C07C317/32 , C07C317/42 , C07C323/21 , C07C323/44 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2603/18 , C07C2603/68 , C07C2603/94 , C07D209/08 , C07D211/58 , C07D213/75 , C07D215/38 , C07D231/40 , C07D235/30 , C07D257/06 , C07D277/72 , C07D295/13 , C07D295/135 , C07D307/68 , C07D317/66 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/60 , C07D333/68 , C07D333/70 , C07D409/12 , C07D417/12 , C07D487/04
摘要: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
摘要翻译: 一类新颖的化合物,其作用是拮抗胰高血糖素激素对胰高血糖素受体的作用。 由于它们对胰高血糖素受体的拮抗作用,所述化合物可适用于治疗和/或预防任何胰高血糖素介导的病症和疾病如高血糖症,1型糖尿病,2型糖尿病和肥胖症。
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公开(公告)号:US06613942B1
公开(公告)日:2003-09-02
申请号:US09220003
申请日:1998-12-23
申请人: Anthony Ling , Vlad Gregor , Javier Gonzalez , Yufeng Hong , Dan Kiel , Atsuo Kuki , Shenghua Shi , Lars Naerum , Peter Madsen , Christian Sams , Jesper Lau , Michael Bruno Plewe , Jun Feng , Min Teng , Michael David Johnson , Kimberly Ann Teston , Ulla Grove Sidelmann , Lotte Bjerre Knudsen
发明人: Anthony Ling , Vlad Gregor , Javier Gonzalez , Yufeng Hong , Dan Kiel , Atsuo Kuki , Shenghua Shi , Lars Naerum , Peter Madsen , Christian Sams , Jesper Lau , Michael Bruno Plewe , Jun Feng , Min Teng , Michael David Johnson , Kimberly Ann Teston , Ulla Grove Sidelmann , Lotte Bjerre Knudsen
IPC分类号: C07C23300
CPC分类号: C07D295/192 , C07C251/86 , C07C255/29 , C07C271/12 , C07C271/22 , C07C271/24 , C07C271/28 , C07C309/65 , C07C311/16 , C07C311/20 , C07C311/49 , C07C317/28 , C07C323/45 , C07C323/60 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D209/48 , C07D209/86 , C07D213/30 , C07D213/80 , C07D215/12 , C07D215/26 , C07D231/12 , C07D295/135 , C07D295/185 , C07D295/26 , C07D307/12 , C07D307/52 , C07D307/84 , C07D309/06 , C07D317/58 , C07D333/24 , C07D401/06 , C07D405/06 , C07D409/06
摘要: Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.
摘要翻译: 公开了包含中心酰肼基序的非肽化合物及其合成方法。 该化合物起拮抗胰高血糖素肽激素的作用。
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5.HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use 失效
标题翻译: HIV整合酶抑制剂,药物组合物及其使用方法公开(公告)号:US07135482B2
公开(公告)日:2006-11-14
申请号:US10699068
申请日:2003-10-30
申请人: Qiyue Hu , Ted William Johnson , Atsuo Kuki , Michael Bruno Plewe , Dawn Marie Nowlin , Hai Wang , Junhu Zhang
发明人: Qiyue Hu , Ted William Johnson , Atsuo Kuki , Michael Bruno Plewe , Dawn Marie Nowlin , Hai Wang , Junhu Zhang
IPC分类号: A61K31/44
CPC分类号: C07D471/04 , C07D471/12 , C07D471/14
摘要: Bicyclic hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.
摘要翻译: 描述由式I表示的双环氧肟酸酯化合物。 双环异羟肟酸酯化合物和含有这些化合物的组合物可用于抑制或调节HIV整合酶的酶活性并治疗HIV介导的疾病和病症。
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公开(公告)号:US20090170846A1
公开(公告)日:2009-07-02
申请号:US12088583
申请日:2006-09-22
申请人: Klaus Ruprecht Dress , Michael Bruno Plewe , Ted William Johnson , Steven Paul Tanis , Khanh Tuan Tran
发明人: Klaus Ruprecht Dress , Michael Bruno Plewe , Ted William Johnson , Steven Paul Tanis , Khanh Tuan Tran
IPC分类号: A61K31/5377 , C07D471/04 , A61K31/437 , C07D413/14 , A61P31/18 , C12N7/06
CPC分类号: C07D471/04
摘要: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus “HIV” integrase enzyme. Formula (I).
摘要翻译: 本发明涉及式(I)化合物及其药学上可接受的盐和溶剂化物,它们的合成及其作为人免疫缺陷病毒“HIV”整合酶的调节剂或抑制剂的用途。 式(I)。
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7.HIV integrase inhibitors, pharmaceutical compositions and methods for their use 失效
标题翻译: HIV整合酶抑制剂,药物组合物及其使用方法公开(公告)号:US07138408B2
公开(公告)日:2006-11-21
申请号:US11251344
申请日:2005-10-14
申请人: Atsuo Kuki , Xinqiang Li , Michael Bruno Plewe , Hai Wang , Junhu Zhang
发明人: Atsuo Kuki , Xinqiang Li , Michael Bruno Plewe , Hai Wang , Junhu Zhang
IPC分类号: A61K31/437 , C07D471/12
CPC分类号: C07D471/04
摘要: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.
摘要翻译: 描述了由式(I)表示的β-咔啉异羟肟酸化合物。 含有这些化合物的β-咔啉异羟肟酸化合物和组合物可用于抑制或调节HIV整合酶的活性并且用于治疗HIV整合酶介导的疾病和病症。
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公开(公告)号:US07692014B2
公开(公告)日:2010-04-06
申请号:US11114813
申请日:2005-04-25
申请人: Klaus Ruprecht Dress , Qiyue Hu , Ted William Johnson , Michael Bruno Plewe , Steven Paul Tanis , Huichun Zhu , Junhu Zhang
发明人: Klaus Ruprecht Dress , Qiyue Hu , Ted William Johnson , Michael Bruno Plewe , Steven Paul Tanis , Huichun Zhu , Junhu Zhang
IPC分类号: C07D471/04 , A61K31/437
CPC分类号: C07D491/14 , C07D471/14
摘要: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIV”) integrase enzyme.
摘要翻译: 本发明涉及式(I)化合物及其药学上可接受的盐和溶剂合物,它们的合成及其作为人免疫缺陷病毒(“HIV”)整合酶的调节剂或抑制剂的用途。
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公开(公告)号:US08633204B2
公开(公告)日:2014-01-21
申请号:US13587825
申请日:2012-08-16
申请人: Hengmiao Cheng , Dilip Bhumralkar , Klaus Ruprecht Dress , Jacqui Elizabeth Hoffman , Mary Catherine Johnson , Robert Steven Kania , Phuong Thi Quy Le , Mitchell David Nambu , Mason Alan Pairish , Michael Bruno Plewe , Khanh Tuan Tran
发明人: Hengmiao Cheng , Dilip Bhumralkar , Klaus Ruprecht Dress , Jacqui Elizabeth Hoffman , Mary Catherine Johnson , Robert Steven Kania , Phuong Thi Quy Le , Mitchell David Nambu , Mason Alan Pairish , Michael Bruno Plewe , Khanh Tuan Tran
IPC分类号: A01N43/90
CPC分类号: C07D471/04
摘要: The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα).
摘要翻译: 本发明涉及式(I)的新颖的4-甲基吡啶并嘧啶酮化合物及其盐,它们的合成及其作为磷酸肌醇3-激酶α(PI3-Kalpha)抑制剂的用途。
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公开(公告)号:US08273755B2
公开(公告)日:2012-09-25
申请号:US12702937
申请日:2010-02-09
申请人: Hengmiao Cheng , Dilip Bhumralkar , Klaus Ruprecht Dress , Jacqui Elizabeth Hoffman , Mary Catherine Johnson , Robert Steven Kania , Phuong Thi Quy Le , Mitchell David Nambu , Mason Alan Pairish , Michael Bruno Plewe , Khanh Tuan Tran
发明人: Hengmiao Cheng , Dilip Bhumralkar , Klaus Ruprecht Dress , Jacqui Elizabeth Hoffman , Mary Catherine Johnson , Robert Steven Kania , Phuong Thi Quy Le , Mitchell David Nambu , Mason Alan Pairish , Michael Bruno Plewe , Khanh Tuan Tran
IPC分类号: C07D471/04 , A61K31/519 , A61P35/00
CPC分类号: C07D471/04
摘要: The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα).
摘要翻译: 本发明涉及新的式(I)的4-甲基吡啶并嘧啶酮化合物及其盐,它们的合成及其作为磷酸肌醇3-激酶α(PI3-Kα)抑制剂的用途。
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