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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:US06469021B1
公开(公告)日:2002-10-22
申请号:US09831572
申请日:2001-10-26
申请人: Larry Kenneth Truesdale , Richard A. Bychowski , Javier Gonzalez , Atsuo Kuki , Ranjan Jagath Rajapakse , Min Teng , Dan Kiel , Daljit S. Dhanoa , Yufeng Hong , Tso-sheng Chou , Anthony L. Ling , Michael David Johnson , Vlad Edward Gregor
发明人: Larry Kenneth Truesdale , Richard A. Bychowski , Javier Gonzalez , Atsuo Kuki , Ranjan Jagath Rajapakse , Min Teng , Dan Kiel , Daljit S. Dhanoa , Yufeng Hong , Tso-sheng Chou , Anthony L. Ling , Michael David Johnson , Vlad Edward Gregor
IPC分类号: A61K31437
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14
摘要: Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
摘要翻译: 作为肠激素胰高血糖素样肽1(GLP-1)的拮抗剂的非肽化合物具有9H-b-咔啉中心基序。 该化合物表现出有利的物理,化学和生物学特性,并且抑制GLP-1肽与GLP-1受体的结合和/或通过结合的GLP-1阻止受体活化。 本发明还涉及抑制GLP-1与GLP-1受体结合的方法以及抑制GLP-1受体活化的方法。 还描述了可用于制备非肽GLP-1受体拮抗剂的中间体化合物。
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