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公开(公告)号：US08846601B2
公开(公告)日：2014-09-30
申请号：US13311824
申请日：2011-12-06
申请人： Yi-qun Shi , Shubh D. Sharma , John H. Dodd , Wei Yang , Xin Chen
发明人： Yi-qun Shi , Shubh D. Sharma , John H. Dodd , Wei Yang , Xin Chen
IPC分类号： A61K38/00 , C07K14/685 , C07K7/56 , C07K5/117
CPC分类号： C07K7/64 , A61K38/00 , A61K38/12 , C07K5/1024 , C07K7/56 , C07K14/685 , Y02A50/401
摘要： Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and z are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes.
摘要翻译： 其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和z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，以及 预防，改善或治疗黑皮质素受体介导的疾病，适应症，病症和综合征的方法。
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公开(公告)号：US20120178701A1
公开(公告)日：2012-07-12
申请号：US13311824
申请日：2011-12-06
申请人： Yi-qun Shi , Shubh D. Sharma , John H. Dodd , Wei Yang , Xin Chen
发明人： Yi-qun Shi , Shubh D. Sharma , John H. Dodd , Wei Yang , Xin Chen
CPC分类号： C07K7/64 , A61K38/00 , A61K38/12 , C07K5/1024 , C07K7/56 , C07K14/685 , Y02A50/401
摘要： Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and z are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes.
摘要翻译： 其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和z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，以及 预防，改善或治疗黑皮质素受体介导的疾病，适应症，病症和综合征的方法。
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3.发明申请公开(公告)号：US20110065652A1
公开(公告)日：2011-03-17
申请号：US12952238
申请日：2010-11-23
申请人： Yi-Qun Shi , Shubh D. Sharma , Wei Yang , Xin Chen
发明人： Yi-Qun Shi , Shubh D. Sharma , Wei Yang , Xin Chen
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , A61K45/06 , C07K14/685
摘要： A melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.
摘要翻译： 下式的黑皮质素受体激动剂环肽其中R，x和y如说明书中所定义，包括上述式的肽的组合物和制剂，以及预防，改善或治疗黑皮质素受体介导的疾病，适应症，条件 和综合征，包括性功能障碍如男性勃起功能障碍和女性性功能障碍。
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4.发明授权公开(公告)号：US08487073B2
公开(公告)日：2013-07-16
申请号：US12952238
申请日：2010-11-23
申请人： Yi-Qun Shi , Shubh D. Sharma , Wei Yang , Xin Chen
发明人： Yi-Qun Shi , Shubh D. Sharma , Wei Yang , Xin Chen
IPC分类号： A61K38/00
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , A61K45/06 , C07K14/685
摘要： A melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.
摘要翻译： 下式的黑皮质素受体激动剂环肽其中R，x和y如说明书中所定义，包括上述式的肽的组合物和制剂，以及预防，改善或治疗黑皮质素受体介导的疾病，适应症，条件 和综合征，包括性功能障碍如男性勃起功能障碍和女性性功能障碍。
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5.发明申请公开(公告)号：US20090305960A1
公开(公告)日：2009-12-10
申请号：US12480420
申请日：2009-06-08
申请人： Xin Chen , Shubh D. Sharma , Yi-Qun Shi , Wei Yang
发明人： Xin Chen , Shubh D. Sharma , Yi-Qun Shi , Wei Yang
摘要： Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, x and y are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including obesity, diabetes, modulation of feeding behavior and related metabolic syndrome.
摘要翻译： 其中R1，R2，R3，R4，x和y如说明书中所定义的组合物和制剂，包括上述式的肽的黑皮质素受体特异性环肽，以及预防，改善或治疗黑皮质素受体 - 介导的疾病，适应症，病症和综合症，包括肥胖症，糖尿病，调节摄食行为和相关的代谢综合征。
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6.发明授权公开(公告)号：US07968548B2
公开(公告)日：2011-06-28
申请号：US11464053
申请日：2006-08-11
申请人： Shubh D. Sharma , Yi-Qun Shi , Kevin D. Burris , Zhijun Wu , Papireddy Purma , Yadi Reddy Bonuga
发明人： Shubh D. Sharma , Yi-Qun Shi , Kevin D. Burris , Zhijun Wu , Papireddy Purma , Yadi Reddy Bonuga
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： C07D241/04 , C07D403/06 , C07D403/10 , C07D403/12
摘要： Melanocortin receptor-specific compounds with diamine groups of the general formula and pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L1, L2, L3, R1a, R1b, R2a, R2b and X are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. 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, including specifically treatment of obesity and related conditions.
摘要翻译： 具有通式的二胺基的黑皮质素受体特异性化合物及其药学上可接受的盐，其中W是具有至少一个阳离子中心，氢键供体或氢键受体的二胺杂原子单元，J，Q，L1，L2，L3， R1a，R1b，R2a，R2b和X如本说明书中所定义，并且带有星号的碳原子可具有任何立体化学构型。 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障碍，包括特别治疗肥胖症和相关病症。
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公开(公告)号：US20110009341A1
公开(公告)日：2011-01-13
申请号：US11557408
申请日：2006-11-07
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1024
摘要： A melanocortin-4 receptor agonist cyclic peptide of the formula where R1, R2, R3, R4a, R4b, R5, R6, R7a, R7b, x, y and z are as defined in the specification, and a method of treating sexual dysfunction, including male erectile dysfunction and female sexual dysfunction, and other melanocortin 4 receptor responsive conditions and disorders.
摘要翻译： R1，R2，R3，R4a，R4b，R5，R6，R7a，R7b，x，y，z和z如说明书中所定义的黑皮质素-4受体激动剂环肽，以及治疗性功能障碍的方法， 包括男性勃起功能障碍和女性性功能障碍，以及其他黑皮质素4受体反应性病症和障碍。
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公开(公告)号：US07807678B2
公开(公告)日：2010-10-05
申请号：US10776419
申请日：2004-02-10
申请人： Shubh D. Sharma , Yi-Qun Shi , Zhijun Wu , Ramesh Rajpurohit
发明人： Shubh D. Sharma , Yi-Qun Shi , Zhijun Wu , Ramesh Rajpurohit
IPC分类号： A61K31/497 , C07D241/36 , C07D403/06 , C07D241/04 , C07D295/02
CPC分类号： C07D487/04 , A61K38/12 , C07D207/16 , C07D241/04 , C07D241/08 , C07D317/72 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/12 , C07K5/0202 , C07K5/021 , C07K5/06078 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0823 , C07K5/0827 , C07K5/1008 , C07K5/101 , G06F19/16 , G06F19/706
摘要： The invention relates to a method of deriving a peptidomimetic of a biologically active metallopeptide, wherein the peptidomimetic includes at least one non-peptide ring structure defining a template space superimposable on a corresponding defined template space of the metallopeptide, and where the peptidomimetic further includes at least two elements independently including an amino acid residue, amino acid side chain moiety or derivative thereof, the elements defining and occupying a similar descriptor space as corresponding elements of the metallopeptide. The invention further relates to peptidomimetics with a template space heterocyclic ring structure, including 5-, 6- and 8-membered and 5-5- and 6-5-bicyclic fused ring structure melanocortin receptor-specific peptidomimetics.
摘要翻译： 本发明涉及一种衍生生物活性金属肽的拟肽的方法，其中拟肽包括至少一个限定模板空间的非肽环结构，该模板空间可重叠在金属肽的相应限定的模板空间上，并且其中拟肽进一步包括在 至少两个元素独立地包括氨基酸残基，氨基酸侧链部分或其衍生物，限定和占据与金属肽相应元素相似的描述空间的元件。 本发明还涉及具有模板空间杂环结构的肽模拟物，包括5-，6-和8-元和5-5-和6-5-双环稠合环结构黑皮质素受体特异性肽模拟物。
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公开(公告)号：US07385025B2
公开(公告)日：2008-06-10
申请号：US11188552
申请日：2005-07-25
CPC分类号： A61K38/04 , A61K38/105 , A61K38/34 , C07K14/68 , A61K2300/00
摘要： Metallopeptides with a sequence of a biologically active alpha-melanocyte stimulating hormone (α-MSH), gamma-melanocyte stimulating hormone (γ-MSH), or bombesin 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： 具有生物活性α-黑素细胞刺激激素（α-MSH），γ-黑素细胞刺激激素（γ-MSH）或长度为n个残基的铃蟾肽序列的序列的金属肽，其中包含氮原子和硫原子的残基各自可用 用于与金属离子的络合被插入到位于n位置的两个和三个位置到C末端侧的任何位置处，或者替代地在从三个位置到n个位置的任何位置处的残基代替， 金属离子与其中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直接相邻的N末端侧的两个残基中的任一种的脯氨酸（Pro）残基替换为 同系物
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公开(公告)号：US07326707B2
公开(公告)日：2008-02-05
申请号：US10761889
申请日：2004-01-21
申请人： Shubh D. Sharma , Yi-Qun Shi , Zhijun Wu , Ramesh Rajpurohit
发明人： Shubh D. Sharma , Yi-Qun Shi , Zhijun Wu , Ramesh Rajpurohit
IPC分类号： A01N43/60 , C07D241/36 , C07D241/38
CPC分类号： C07D487/04 , A61K38/12 , C07D207/16 , C07D241/04 , C07D241/08 , C07D317/72 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/12 , C07K5/0202 , C07K5/021 , C07K5/06078 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0823 , C07K5/0827 , C07K5/1008 , C07K5/101 , G06F19/16 , G06F19/706
摘要： Melanocortin receptor-specific bicyclic compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, R3 X and z are as described in the specification, which are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
摘要翻译： 具有以下结构的黑皮质素受体特异性双环化合物及其立体异构体和药学上可接受的盐，其中R 1，R 2，R 3 X和 z如说明书所述，其是一种或多种黑皮质素受体的激动剂，拮抗剂或混合激动剂和拮抗剂，并且可用于治疗黑皮质素受体相关疾病和病症。 还公开了含有结构（I）化合物和与其用途有关的方法的药物组合物。
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