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公开(公告)号：US08263608B2
公开(公告)日：2012-09-11
申请号：US13074070
申请日：2011-03-29
申请人： Yi-Qun Shi , John H. Dodd , Elizabeth G. Rowley , Gary L. Olson , Axel Metzger
发明人： Yi-Qun Shi , John H. Dodd , Elizabeth G. Rowley , Gary L. Olson , Axel Metzger
IPC分类号： A61K31/415 , A61K31/445 , A61K31/454 , A61K31/4545 , C07D221/00 , C07D233/00
CPC分类号： A61K31/497
摘要： Melanocortin receptor-specific compounds of formula I below: wherein the variables are as defined in the specification, and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders.
摘要翻译： 以下式I的黑皮质素受体特异性化合物：其中变量如说明书中所定义，及其对映异构体，非对映异构体和药学上可接受的盐。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或病症。
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公开(公告)号：US20110178080A1
公开(公告)日：2011-07-21
申请号：US13074070
申请日：2011-03-29
申请人： Yi-Qun Shi , John H. Dodd , Elizabeth G. Rowley , Gary L. Olson , Axel Metzger
发明人： Yi-Qun Shi , John H. Dodd , Elizabeth G. Rowley , Gary L. Olson , Axel Metzger
IPC分类号： C07D471/10 , A61K31/438 , A61K31/496 , A61K31/5377 , A61P3/00 , A61P3/10 , A61P15/00
CPC分类号： A61K31/497
摘要： Melanocortin receptor-specific compounds of formula I below: wherein the variables are as defined in the specification, and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders.
摘要翻译： 以下式I的黑皮质素受体特异性化合物：其中变量如说明书中所定义，及其对映异构体，非对映异构体和药学上可接受的盐。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或病症。
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公开(公告)号：US08455617B2
公开(公告)日：2013-06-04
申请号：US12795469
申请日：2010-06-07
申请人： John H. Dodd , Yi-Qun Shi , Wei Yang
发明人： John H. Dodd , Yi-Qun Shi , Wei Yang
摘要： The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I) or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4a, R4b, R4c, R5, x and y are as defined in the specification. These compounds are particularly useful in the treatments of energy homeostasis and metabolism related (e.g. diabetes), food intake related and/or energy balance and body weight related diseases, disorders and/or conditions, including obesity, overweight and diseases, disorders and/or conditions associated with obesity and/or overweight, such as type 2 diabetes and metabolic syndrome.
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公开(公告)号：US08455618B2
公开(公告)日：2013-06-04
申请号：US13282227
申请日：2011-10-26
申请人： John H. Dodd , Yi-Qun Shi , Wei Yang
发明人： John H. Dodd , Yi-Qun Shi , Wei Yang
摘要： The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I) or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4a, R4b, R4c, R5, x and y are as defined in the specification. These compounds are particularly useful in the treatments of energy homeostasis and metabolism related (e.g. diabetes), food intake related and/or energy balance and body weight related diseases, disorders and/or conditions, including obesity, overweight and diseases, disorders and/or conditions associated with obesity and/or overweight, such as type 2 diabetes and metabolic syndrome.
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公开(公告)号：US20100311648A1
公开(公告)日：2010-12-09
申请号：US12795469
申请日：2010-06-07
申请人： John H. DODD , Yi-Qun Shi , Wei Yang
发明人： John H. DODD , Yi-Qun Shi , Wei Yang
IPC分类号： A61P3/04 , C07K7/64 , A61K38/12 , A61P5/50 , A61P3/06 , A61P9/12 , A61P9/00 , A61P19/02 , A61P25/00 , A61P3/08 , A61P3/10 , A61P3/00 , A61P1/16 , A61P9/10 , A61P1/04
摘要： The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I) or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4a, R4b, R4c, R5, x and y are as defined in the specification. These compounds are particularly useful in the treatments of energy homeostasis and metabolism related (e.g. diabetes), food intake related and/or energy balance and body weight related diseases, disorders and/or conditions, including obesity, overweight and diseases, disorders and/or conditions associated with obesity and/or overweight, such as type 2 diabetes and metabolic syndrome.
摘要翻译： 本发明涉及式（I）的黑皮质素受体特异性环肽或其药学上可接受的盐，其中R1，R2，R3，R4a，R4b，R4c，R5，x和y如说明书中所定义。 这些化合物特别可用于治疗能量体内平衡和相关代谢（例如糖尿病），与食物相关的和/或能量平衡以及与体重有关的疾病，病症和/或病症，包括肥胖，超重和疾病，障碍和/或 与肥胖和/或超重相关的病症，如2型糖尿病和代谢综合征。
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公开(公告)号：US20120046219A1
公开(公告)日：2012-02-23
申请号：US13282227
申请日：2011-10-26
申请人： John H. DODD , Yi-Qun Shi , Wei Yang
发明人： John H. DODD , Yi-Qun Shi , Wei Yang
IPC分类号： A61K38/12 , A61P3/10 , A61P3/04 , A61P3/06 , A61P9/12 , A61P9/00 , A61P19/02 , A61P25/00 , A61P9/10 , A61P1/04 , A61P3/00 , A61P3/08 , A61P1/16 , A61P7/00 , A61P43/00 , C07K7/56
摘要： The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I) or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4a, R4b, R4c, R5, x and y are as defined in the specification. These compounds are particularly useful in the treatments of energy homeostasis and metabolism related (e.g. diabetes), food intake related and/or energy balance and body weight related diseases, disorders and/or conditions, including obesity, overweight and diseases, disorders and/or conditions associated with obesity and/or overweight, such as type 2 diabetes and metabolic syndrome.
摘要翻译： 本发明涉及式（I）的黑皮质素受体特异性环肽或其药学上可接受的盐，其中R1，R2，R3，R4a，R4b，R4c，R5，x和y如说明书中所定义。 这些化合物特别可用于治疗能量体内平衡和相关代谢（例如糖尿病），与食物相关的和/或能量平衡以及与体重有关的疾病，病症和/或病症，包括肥胖，超重和疾病，障碍和/或 与肥胖和/或超重相关的病症，如2型糖尿病和代谢综合征。
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公开(公告)号：US20120225828A1
公开(公告)日：2012-09-06
申请号：US13472914
申请日：2012-05-16
申请人： Wei Yang , Yi-Qun Shi
发明人： Wei Yang , Yi-Qun Shi
CPC分类号： C07K7/56 , A61K31/407 , A61K38/00 , C07K7/54 , C07K14/68
摘要： Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula or salts thereof, and methods of preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes.
摘要翻译： 其中R1，R2，R3，R4，R5，R6，R7，R8和R9如说明书中所定义的黑皮质素受体特异性环肽，包括上述式的肽的组合物和制剂或其盐，以及方法 预防，改善或治疗黑皮质素-1受体介导或反应性疾病，适应症，病症和综合征。
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公开(公告)号：US07964601B2
公开(公告)日：2011-06-21
申请号：US12131822
申请日：2008-06-02
申请人： Shubh D. Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Zhijun Wu , Papireddy Purma , Annette M. Shadiack , Kevin D. Burris
发明人： Shubh D. Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Zhijun Wu , Papireddy Purma , Annette M. Shadiack , Kevin D. Burris
IPC分类号： A61K31/497 , C07D403/06 , C07D241/04 , C07D241/06
CPC分类号： C07D403/10 , C07D241/04 , C07D403/06
摘要： A melanocortin receptor-specific compound of the general formula of structure I: where X, R1, R2a, R2b, R3, R4a, R4b, R5a and R5b are as defined in the specification, which compound binds with high affinity to one or more melanocortin receptors and is optionally an agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.
摘要翻译： 结构I通式的黑皮质素受体特异性化合物：其中X，R1，R2a，R2b，R3，R4a，R4b，R5a和R5b如本说明书中所定义，该化合物以高亲和力结合一种或多种黑皮质素 受体，并且任选地是激动剂，拮抗剂，反向激动剂的反向激动剂或拮抗剂，并且可以用于治疗一种或黑皮质素受体相关病症或病症，以及使用本发明化合物的方法。
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公开(公告)号：US07456184B2
公开(公告)日：2008-11-25
申请号：US10837519
申请日：2004-04-30
申请人： Shubh D. Sharma , Yi-Qun Shi , Zhijun Wu , Ramesh Rajpurohit , Annette M. Shadiack , Papireddy Purma , Kevin D. Burris
发明人： Shubh D. Sharma , Yi-Qun Shi , Zhijun Wu , Ramesh Rajpurohit , Annette M. Shadiack , Papireddy Purma , Kevin D. Burris
IPC分类号： A61K31/497 , C07D403/02
CPC分类号： C07D403/10 , C07D241/04 , C07D403/06
摘要： A melanocortin receptor-specific compound of the general formula of structure I: where X, R1, R2a, R2b, R3, R4a, R4b, R5a and R5b are as defined in the specification, which compound binds with high affinity to one or more melanocortin receptors and is optionally an agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.
摘要翻译： 结构I的通式的黑皮质素受体特异性化合物：其中X，R 1，R 2a，R 2b，R SUB R 3，R 4a，R 4b，R 5a和R 5b如本文所定义。 说明书，该化合物以高亲和力结合一种或多种黑皮质素受体，并且任选地是反向激动剂的激动剂，拮抗剂，反向激动剂或拮抗剂，并且可用于治疗一种或黑皮质素受体相关病症或 病症和使用本发明化合物的方法。
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公开(公告)号：US20080255033A1
公开(公告)日：2008-10-16
申请号：US12136233
申请日：2008-06-10
IPC分类号： A61K38/04
CPC分类号： A61K38/04 , A61K38/105 , A61K38/34 , C07K14/68 , A61K2300/00
摘要： Metallopeptides with a sequence of a biologically active gamma-melanocyte stimulating hormone sequence of length n residues, wherein a residue including a nitrogen atom and sulfur atom each available for complexation to a metal ion is inserted at any position from between the two and three position to the C-terminus side of the n position, or alternatively is substituted for the residue at any position from the three position to the n position, with a metal ion complexed thereto, with any proline (Pro) residue which is either of the two residues on the immediately adjacent N-terminus side of the inserted or substituent residue comprising a nitrogen atom and sulfur atom available for complexation to a metal ion is substituted with a homolog.
摘要翻译： 具有长度为n个残基的生物活性γ-黑素细胞刺激激素序列序列的金属肽，其中包含可用于与金属离子络合的氮原子和硫原子的残基被插入到两个和三个位置之间的任何位置， 或者在n位置的任何位置用n位置的任何位置取代残基，其中与其配合的金属离子与任何两个残基中的任一种的脯氨酸（Pro）残基 在包含可与金属离子络合的氮原子和硫原子的插入或取代残基的紧邻N末端侧被同系物取代。
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