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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：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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公开(公告)号：US07351690B2
公开(公告)日：2008-04-01
申请号：US10769695
申请日：2004-01-30
IPC分类号： A61K38/16
CPC分类号： C07K5/1008 , C07K1/047 , C07K5/1016 , C07K5/1024 , G01N33/6803
摘要： The invention provides methods for identification and determination of target-specific sites in peptides and proteins, including a method for determining the primary sequence of a secondary structure within a known parent polypeptide that binds to the target of interest. In one embodiment of the invention, a residue or mimetic containing a nitrogen atom and a sulfur atom available for binding to a metal ion is serially substituted for single residues in or inserted between adjacent residues in a known primary sequence of a peptide or protein. The resulting sequence is complexed with a metal ion thereby forming a metallopeptide. The resulting metallopeptides are then used in binding or functional assays related to the target of interest, and the metallopeptide(s) which result in significant or substantially decreased or changed binding or functionality are determined to identify the primary sequence involved in such binding or functionality.
摘要翻译： 本发明提供用于鉴定和确定肽和蛋白质中靶特异性位点的方法，包括确定结合目的靶标的已知亲本多肽内的二级结构的一级序列的方法。 在本发明的一个实施方案中，含有可与金属离子结合的氮原子和硫原子的残基或模拟物连续取代肽或蛋白质的已知一级序列中相邻残基之间或插入其中的单个残基。 所得到的序列与金属离子络合，从而形成金属肽。 然后将所得金属肽用于与感兴趣靶标相关的结合或功能测定，并确定导致显着或显着降低或改变的结合或功能的金属肽，以鉴定涉及这种结合或功能的一级序列。
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公开(公告)号：US20050282739A1
公开(公告)日：2005-12-22
申请号：US11188552
申请日：2005-07-25
申请人： Shubh Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Hui-Zhi Cai , Margarita Bastos
发明人： Shubh Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Hui-Zhi Cai , Margarita Bastos
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）残基取代， 同系物
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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：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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公开(公告)号：US08247530B2
公开(公告)日：2012-08-21
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：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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