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1. 发明申请

US20050282739A1 Metallopeptide compounds 有权
标题翻译：金属肽化合物
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
IPC分类号： A61K38/04 , A61K38/10 , A61K38/16 , A61K38/34
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

2. 发明授权

US07385025B2 Metallopeptide compounds 有权
标题翻译：金属肽化合物
公开(公告)号：US07385025B2
公开(公告)日：2008-06-10
申请号：US11188552
申请日：2005-07-25
申请人： Shubh D. Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Hui-Zhi Cai , Margarita Bastos
发明人： Shubh D. Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Hui-Zhi Cai , Margarita Bastos
IPC分类号： A61K38/04 , A61K51/08 , C07K7/00
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

3. 发明申请

US20080255033A1 Metallopeptide gamma-Melanocyte Stimulating Hormone Compounds 审中-公开
标题翻译：金属肽γ-黑素细胞刺激激素化合物
公开(公告)号：US20080255033A1
公开(公告)日：2008-10-16
申请号：US12136233
申请日：2008-06-10
申请人： Shubh D. Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Hui-Zhi Cai , Margarita Bastos
发明人： Shubh D. Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Hui-Zhi Cai , Margarita Bastos
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。

4. 发明授权

US07351690B2 Knockout identification of target-specific sites in peptides 有权
标题翻译：敲除肽中靶特异性位点的鉴定
公开(公告)号：US07351690B2
公开(公告)日：2008-04-01
申请号：US10769695
申请日：2004-01-30
申请人： Shubh D. Sharma , Yi-Qun Shi , Margarita Bastos , Ramesh Rajpurohit , Hui-Zhi Cai
发明人： Shubh D. Sharma , Yi-Qun Shi , Margarita Bastos , Ramesh Rajpurohit , Hui-Zhi Cai
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。

5. 发明授权

US07307063B2 Melanocortin metallopeptides for treatment of sexual dysfunction 有权
标题翻译：黑皮质素金属肽用于治疗性功能障碍
公开(公告)号：US07307063B2
公开(公告)日：2007-12-11
申请号：US10640755
申请日：2003-08-13
申请人： Shubh Sharma , Annette Shadiack , Yi-Qun Shi , Wei Yang , Hui-Zhi Cai
发明人： Shubh Sharma , Annette Shadiack , Yi-Qun Shi , Wei Yang , Hui-Zhi Cai
IPC分类号： C07K5/10
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1024 , C07K14/575 , C07K14/68
摘要： Metallopeptides are provided for use in treatment of sexual dysfunction in mammals. The metallopeptides are agonists for at least one of melanocortin-3 or melanocortin-4 receptors. The metallopeptides are conformationally fixed on complexation of a metal ion-binding portion thereof with a metal ion. Also provided are metallopeptides that are antagonists for at least one of melanocortin-3 or melanocortin-4 receptors.
摘要翻译：金属肽被用于治疗哺乳动物的性功能障碍。金属肽是黑皮质素-3或黑皮质素-4受体中的至少一种的激动剂。金属肽在与金属离子的金属离子结合部分的络合作用下被构象地固定。还提供了作为黑皮质素-3或黑皮质素-4受体中的至少一种的拮抗剂的金属肽。

6. 发明申请

US20070155670A1 Pyrrolidine Melanocortin-Specific Compounds 有权
标题翻译：吡咯烷黑皮质素特异性化合物
公开(公告)号：US20070155670A1
公开(公告)日：2007-07-05
申请号：US11680932
申请日：2007-03-01
申请人： Shubh Sharma , Yi-Qun Shi , Zhijun Wu , Ramesh Rajpurohit
发明人： Shubh Sharma , Yi-Qun Shi , Zhijun Wu , Ramesh Rajpurohit
IPC分类号： A61K38/04 , C07K5/06
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 pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group or from one to three additional amino acid residues, optionally with an amine capping group, which compounds 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. Methods of synthesis of compounds of structure (I), 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吡咯烷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和R 3是如说明书中所述，优选其中R 3是具有至少一个取代或未取代的苯基或萘基芳环的D-氨基酸，并且其中R 3'任选地进一步包括胺封端基团或一至三个另外的氨基酸残基，任选具有胺封端基团，该化合物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。还公开了结构（I）化合物的合成方法，含有结构（I）化合物的药物组合物及其使用方法。

7. 发明申请

US20060014676A1 Cyclic peptides for treatment of cachexia 有权
标题翻译：循环肽用于治疗恶病质
公开(公告)号：US20060014676A1
公开(公告)日：2006-01-19
申请号：US11174845
申请日：2005-07-05
申请人： Shubh Sharma , Ramesh Rajpurohit , Annette Shadiack , Yi-Qun Shi , Kevin Burris
发明人： Shubh Sharma , Ramesh Rajpurohit , Annette Shadiack , Yi-Qun Shi , Kevin Burris
IPC分类号： C07K5/12 , A61K38/12
CPC分类号： C07K7/06 , A61K38/12 , C07K5/0821 , C07K5/1024 , C07K7/60 , Y10S436/811
摘要： A highly selective melanocortin-4 receptor antagonist cyclic peptide of the formula where R1, R2, R3, R4a, R4b, R5, R6, R7, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.
摘要翻译：下式的高选择性黑皮质素-4受体拮抗剂环肽其中R 1，R 2，R 3，R 4a， R 4b，R 5，R 6，R 7，x，y和z分别为如本说明书中所定义的，以及治疗体重障碍（包括恶病质，肌营养不良和消瘦综合征或疾病）以及治疗炎症和免疫疾病的方法。

8. 发明申请

US20060014194A1 Cyclic peptides for treatment of cachexia 有权
标题翻译：循环肽用于治疗恶病质
公开(公告)号：US20060014194A1
公开(公告)日：2006-01-19
申请号：US11174851
申请日：2005-07-05
申请人： Shubh Sharma , Ramesh Rajpurohit , Annette Shadiack , Yi-Qun Shi , Kevin Burris
发明人： Shubh Sharma , Ramesh Rajpurohit , Annette Shadiack , Yi-Qun Shi , Kevin Burris
IPC分类号： A61K38/12 , C07K7/64 , C12Q1/68
CPC分类号： A61K38/12 , C07K5/0821 , C07K5/1024 , C07K7/06 , C07K7/56 , C07K7/60 , Y10S436/811
摘要： A highly selective melanocortin-4 receptor antagonist cyclic hexapeptide of the formula where R1, R2, R3a, R3b, R4, R5, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.
摘要翻译：具有下式的高选择性黑皮质素-4受体拮抗剂环状六肽其中R 1，R 2，R 3a，R 3b， R 3，R 5，R 5，x，y和z如说明书中所定义，以及治疗体重紊乱的方法，包括恶病质，肌肉减少症和浪费综合征或疾病，以及治疗炎症和免疫疾病。

9. 发明申请

US20050176728A1 Substituted melanocortin receptor-specific piperazine compounds 有权
标题翻译：取代的黑皮质素受体特异性哌嗪化合物
公开(公告)号：US20050176728A1
公开(公告)日：2005-08-11
申请号：US11099814
申请日：2005-04-05
申请人： Shubh Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Zhijun Wu
发明人： Shubh Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Zhijun Wu
IPC分类号： A61K31/496 , C07D43/02
CPC分类号： C07D241/04 , C07D403/06
摘要： Melanocortin receptor-specific compounds of the general formulas and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, L is a linker, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q includes a substituted or unsubstituted aromatic carbocyclic ring, R6, R7, y and z are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration, and optionally with one or two additional ring substituents as defined, which compounds bind to one or more melanocortin receptors and are optionally an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.
摘要翻译：其中J为取代或未取代的单环或双环结构的黑皮质素受体特异性化合物及其药学上可接受的盐，L为连接基，W为至少一个阳离子中心，氢键供体或氢的杂原子单元键接受体，Q包括取代或未取代的芳族碳环，R 6，R 7，y和z如说明书中所定义，并且用星号可以具有任何立体化学构型，并且任选地具有如所定义的一个或两个另外的环取代基，这些化合物结合一种或多种黑皮质素受体，并且任选地是激动剂，部分激动剂，拮抗剂，反向激动剂或逆反应的拮抗剂激动剂，并且可以用于治疗一种或多种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。

10. 发明授权

US07964601B2 Melanocortin receptor-specific compounds 有权
标题翻译：黑皮质素受体特异性化合物
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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