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公开(公告)号：US20130053304A1
公开(公告)日：2013-02-28
申请号：US13643840
申请日：2011-04-29
申请人： Yinxiang Wang , Fenlai Tan , Shaojing Hu , Xiangdong Zhao , Cunbo Ma , Yanping Wang , Xiaoyan Shen , Lieming Ding , Yunyan Hu , Hong Cao , Wei Long
发明人： Yinxiang Wang , Fenlai Tan , Shaojing Hu , Xiangdong Zhao , Cunbo Ma , Yanping Wang , Xiaoyan Shen , Lieming Ding , Yunyan Hu , Hong Cao , Wei Long
IPC分类号： A61K38/26 , A61P3/10 , A61P3/08 , A61P3/04 , A61P9/12 , A61P1/04 , A61P25/00 , A61P9/10 , A61P9/00 , A61P7/02 , A61P1/00 , C07K14/605 , A61P3/06
CPC分类号： C07K14/605 , A61K38/00
摘要： Provided is a glucagon-like peptide-1 (GLP-1) analogue shown as the following formula, wherein X is selected from glycine and glycinamide. The GLP-1 analogue has a non-proteogenic amino acid residue in position 8 relative to the sequence GLP-1, and is acylated with a moiety comprising two acidic groups to the lysine residue in position 26. The GLP-1 analogue is resistant to dipeptidyl peptidase IV so as to have an extended half-life in vivo. Also provided is a use of the GLP-1 analogue in conquering blood sugar.
摘要翻译： 本发明提供如下式所示的胰高血糖素样肽-1（GLP-1）类似物，其中X选自甘氨酸和甘氨酰胺。 GLP-1类似物相对于序列GLP-1具有位置8的非蛋白原性氨基酸残基，并且用包含两个酸性基团的部分酰化至位置26的赖氨酸残基。GLP-1类似物对 二肽基肽酶IV，以使体内延长半衰期。 还提供了GLP-1类似物在征服血糖中的用途。
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公开(公告)号：US09487570B2
公开(公告)日：2016-11-08
申请号：US13698819
申请日：2010-05-17
申请人： Shaojing Hu , Fenlai Tan , Yanping Wang , Cunbo Ma , Yunyan Hu , Hong Cao , Xiangdong Zhao , Wei Long , Yinxiang Wang , Lieming Ding
发明人： Shaojing Hu , Fenlai Tan , Yanping Wang , Cunbo Ma , Yunyan Hu , Hong Cao , Xiangdong Zhao , Wei Long , Yinxiang Wang , Lieming Ding
IPC分类号： A61K38/26 , A61P3/10 , A61P7/12 , C07K14/605 , A61K38/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , A61K9/00
CPC分类号： C07K14/605 , A61K9/0019 , A61K38/00
摘要： The present invention relates to novel analogs of glucagon like peptide and compositions that are useful for up-regulating insulin expression in mammals and for treating diabetes. In particular, these peptide derivatives have a peptide mimic linker and provides long duration of action for the treatment of diabetes and other insulinotropic peptide related diseases, gastrointestinal function and activities associated with glucagon levels.
摘要翻译： 本发明涉及胰高血糖素样肽的新型类似物和可用于上调哺乳动物胰岛素表达和治疗糖尿病的组合物。 特别地，这些肽衍生物具有肽模拟接头并且提供用于治疗糖尿病和其它促胰岛素肽相关疾病，胃肠功能和与胰高血糖素水平相关的活性的长期作用。
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公开(公告)号：US08742138B2
公开(公告)日：2014-06-03
申请号：US13384097
申请日：2010-07-14
申请人： Xinshan Kang , Wei Long , Cunbo Ma , Yanping Wang , Hong Cao , Yinxiang Wang , Fenlai Tan , Yunyan Hu
发明人： Xinshan Kang , Wei Long , Cunbo Ma , Yanping Wang , Hong Cao , Yinxiang Wang , Fenlai Tan , Yunyan Hu
IPC分类号： C07D311/02
CPC分类号： A61K31/37 , C07D311/56 , C07D405/04
摘要： This invention relates to new compounds that can serve as hypoxia mimetics. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one of these compounds.
摘要翻译： 本发明涉及可用作缺氧模拟物的新化合物。 本发明还涉及通过向受试者施用这些化合物中的至少一种来提高受试者中HIF水平或活性或治疗与受试者中HIF水平或活性相关的病症的方法。
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公开(公告)号：US09409900B2
公开(公告)日：2016-08-09
申请号：US13884470
申请日：2011-11-09
申请人： Xinshan Kang , Wei Long , Cunbo Ma , Yanping Wang , Xiaoyan Shen , Yunyan Hu , Fenlai Tan , Yinxiang Wang
发明人： Xinshan Kang , Wei Long , Cunbo Ma , Yanping Wang , Xiaoyan Shen , Yunyan Hu , Fenlai Tan , Yinxiang Wang
IPC分类号： C07D417/12 , C07D233/88 , C07D405/14 , C07D417/14 , C07D213/74 , C07D213/80 , C07D213/803 , C07D241/20 , C07D277/42 , C07D285/08 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D401/14
CPC分类号： C07D417/14 , C07D213/74 , C07D213/80 , C07D213/803 , C07D233/88 , C07D241/20 , C07D277/42 , C07D285/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D417/12
摘要： The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders.
摘要翻译： 提供式（I）的化合物，其药学上可接受的盐，其溶剂化物，其螯合物，其非共价络合物或上述化合物的产物或上述任何形式的混合物。 化合物在制备用于治疗和/或预防糖尿病，肥胖症和相关疾病的药物中的用途。
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公开(公告)号：US08951959B2
公开(公告)日：2015-02-10
申请号：US13643840
申请日：2011-04-29
申请人： Yinxiang Wang , Fenlai Tan , Shaojing Hu , Xiangdong Zhao , Cunbo Ma , Yanping Wang , Xiaoyan Shen , Lieming Ding , Yunyan Hu , Hong Cao , Wei Long
发明人： Yinxiang Wang , Fenlai Tan , Shaojing Hu , Xiangdong Zhao , Cunbo Ma , Yanping Wang , Xiaoyan Shen , Lieming Ding , Yunyan Hu , Hong Cao , Wei Long
IPC分类号： A61K38/00 , A61P9/10 , C07K14/47 , A61P3/04 , A61K38/22 , A61P3/08 , A61P3/10 , A61K38/26 , A61P7/12 , C07K14/605 , A61K38/28 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K14/605 , A61K38/00
摘要： Provided is a glucagon-like peptide-1 (GLP-1) analog shown as the following formula, wherein X is selected from glycine and glycinamide. The GLP-1 analog has a non-proteogenic amino acid residue in position 8 relative to the sequence GLP-1, and is acylated with a moiety comprising two acidic groups to the lysine residue in position 26. The GLP-1 analog is resistant to dipeptidyl peptidase IV so as to have an extended half-life in vivo. Also provided is a use of the GLP-1 analog in conquering blood sugar.
摘要翻译： 本发明提供如下式所示的胰高血糖素样肽-1（GLP-1）类似物，其中X选自甘氨酸和甘氨酰胺。 GLP-1类似物相对于序列GLP-1具有位置8的非蛋白原性氨基酸残基，并且用包含两个酸性基团的部分酰化至位置26的赖氨酸残基。GLP-1类似物对 二肽基肽酶IV，以使体内延长半衰期。 还提供了GLP-1类似物在征服血糖中的用途。
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6.发明申请公开(公告)号：US20140343137A1
公开(公告)日：2014-11-20
申请号：US14166203
申请日：2012-07-30
申请人： Xinshan Kang , Wei Long , Fei Wang , Cunbo Ma , Liufeng Zhou , Yunyan Hu , Yanping Wang , Hong Cao , Yinxiang Wang , Fenlai Tan
发明人： Xinshan Kang , Wei Long , Fei Wang , Cunbo Ma , Liufeng Zhou , Yunyan Hu , Yanping Wang , Hong Cao , Yinxiang Wang , Fenlai Tan
IPC分类号： C07D311/56
CPC分类号： C07D311/56
摘要： The polymorphic forms of the compound of Formula I, the preparation thereof including the preparation of the intermediates, the pharmaceutical compositions thereof and the uses of a polymorph above in the manufacture of medicaments for treating a disease, a disorder or a condition are disclosed.
摘要翻译： 公开了式I化合物的多晶型物，其制备方法，包括制备中间体，其药物组合物，以及上述多晶型物在制备用于治疗疾病，病症或病症的药物中的用途。
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7.发明授权Stable polymorphic forms of compound as hypoxia mimetics, and uses thereof 有权作为缺氧模拟物的化合物的稳定多晶形式及其用途公开(公告)号：US09238637B2
公开(公告)日：2016-01-19
申请号：US14166203
申请日：2012-07-30
申请人： Xinshan Kang , Wei Long , Fei Wang , Cunbo Ma , Liufeng Zhou , Yunyan Hu , Yanping Wang , Hong Cao , Yinxiang Wang , Fenlai Tan
发明人： Xinshan Kang , Wei Long , Fei Wang , Cunbo Ma , Liufeng Zhou , Yunyan Hu , Yanping Wang , Hong Cao , Yinxiang Wang , Fenlai Tan
IPC分类号： A01N43/16 , C07D311/56
CPC分类号： C07D311/56
摘要： The polymorphic forms of the compound of Formula I, the preparation thereof including the preparation of the intermediates, the pharmaceutical compositions thereof and the uses of a polymorph above in the manufacture of medicaments for treating a disease, a disorder or a condition are disclosed.
摘要翻译： 公开了式I化合物的多晶型物，其制备方法，包括制备中间体，其药物组合物，以及上述多晶型物在制备用于治疗疾病，病症或病症的药物中的用途。
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公开(公告)号：US20130225587A1
公开(公告)日：2013-08-29
申请号：US13884470
申请日：2011-11-09
申请人： Xinshan Kang , Wei Long , Cunbo Ma , Yanping Wang , Xiaoyan Shen , Yunyan Hu , Fenlai Tan , Yinxiang Wang
发明人： Xinshan Kang , Wei Long , Cunbo Ma , Yanping Wang , Xiaoyan Shen , Yunyan Hu , Fenlai Tan , Yinxiang Wang
IPC分类号： C07D417/14 , C07D405/14 , C07D233/88 , C07D417/12 , C07D241/20 , C07D285/08 , C07D401/14 , C07D405/12
CPC分类号： C07D417/14 , C07D213/74 , C07D213/80 , C07D213/803 , C07D233/88 , C07D241/20 , C07D277/42 , C07D285/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D417/12
摘要： The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders.
摘要翻译： 提供式（I）的化合物，其药学上可接受的盐，其溶剂化物，其螯合物，其非共价络合物或上述化合物的产物或上述任何形式的混合物。 化合物在制备用于治疗和/或预防糖尿病，肥胖症和相关疾病的药物中的用途。
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公开(公告)号：US20130203672A1
公开(公告)日：2013-08-08
申请号：US13698819
申请日：2010-05-17
申请人： Shaojing Hu , Fenlai Tan , Yanping Wang , Cunbo Ma , Yunyan Hu , Hong Cao , Xiangdong Zhao , Wei Long , Yinxiang Wang , Lieming Ding
发明人： Shaojing Hu , Fenlai Tan , Yanping Wang , Cunbo Ma , Yunyan Hu , Hong Cao , Xiangdong Zhao , Wei Long , Yinxiang Wang , Lieming Ding
IPC分类号： C07K14/605
CPC分类号： C07K14/605 , A61K9/0019 , A61K38/00
摘要： The present invention relates to novel analogs of glucagon like peptide and compositions that are useful for up-regulating insulin expression in mammals and for treating diabetes. In particular, these peptide derivatives have a peptide mimic linker and provides long duration of action for the treatment of diabetes and other insulinotropic peptide related diseases, gastrointestinal function and activities associated with glucagon levels.
摘要翻译： 本发明涉及胰高血糖素样肽的新型类似物和可用于上调哺乳动物胰岛素表达和治疗糖尿病的组合物。 特别地，这些肽衍生物具有肽模拟接头并且提供用于治疗糖尿病和其它促胰岛素肽相关疾病，胃肠功能和与胰高血糖素水平相关的活性的长期作用。
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10.发明申请公开(公告)号：US20120172399A1
公开(公告)日：2012-07-05
申请号：US13384097
申请日：2010-07-14
申请人： Xinshan Kang , Wei Long , Cunbo Ma , Yanping Wang , Hong Cao , Yinxiang Wang , Fenlai Tan , Yunyan Hu
发明人： Xinshan Kang , Wei Long , Cunbo Ma , Yanping Wang , Hong Cao , Yinxiang Wang , Fenlai Tan , Yunyan Hu
IPC分类号： A61K31/4433 , C07D405/10 , A61K31/37 , A61P3/10 , A61P35/00 , A61P7/00 , A61P7/06 , A61P17/02 , A61P37/06 , A61P9/12 , A61P29/00 , C07D311/56 , A61P9/10
CPC分类号： A61K31/37 , C07D311/56 , C07D405/04
摘要： This invention relates to new compounds that can serve as hypoxia mimetics. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one of these compounds.
摘要翻译： 本发明涉及可用作缺氧模拟物的新化合物。 本发明还涉及通过向受试者施用这些化合物中的至少一种来提高受试者中HIF水平或活性或治疗与受试者中HIF水平或活性相关的病症的方法。
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