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    Metallopeptide compounds
    1.
    发明授权
    Metallopeptide compounds 有权
    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

    Metallopeptide gamma-Melanocyte Stimulating Hormone Compounds
    2.
    发明申请
    Metallopeptide gamma-Melanocyte Stimulating Hormone Compounds 审中-公开
    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。

    Knockout identification of target-specific sites in peptides
    3.
    发明授权
    Knockout identification of target-specific sites in peptides 有权
    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。

    Metallopeptide compounds
    4.
    发明申请
    Metallopeptide compounds 有权
    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

    Substituted melanocortin receptor-specific piperazine compounds
    9.
    发明授权
    Substituted melanocortin receptor-specific piperazine compounds 有权
    取代的黑皮质素受体特异性哌嗪化合物

    公开(公告)号：US07709484B1

    公开(公告)日：2010-05-04

    申请号：US11110060

    申请日：2005-04-19

    申请人： Shubh D. Sharma ,  Yi-Qun Shi ,  Zhijun Wu ,  Bolun Hu ,  Ramesh Rajpurohit

    发明人： Shubh D. Sharma ,  Yi-Qun Shi ,  Zhijun Wu ,  Bolun Hu ,  Ramesh Rajpurohit

    IPC分类号： A61K31/497 ,  C07D241/04 ,  C07D403/04 ,  C07D405/04 ,  C07D295/04

    CPC分类号： C07D241/04 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12

    摘要： A substituted piperazine compound having the structure I: or the structure IX: or an enantomeric, stereoisomeric or diastereomeric form of the foregoing, and pharmaceutically acceptable salts thereof, where J, L, Q, W, A, R6, R7, z and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration, which compounds bind to one or more melanocortin receptors and may be employed in pharmaceutical preparations 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，L，Q，W，A，R6，R7，z和y具有结构I或结构IX的取代哌嗪化合物或其前体的烯醇，立体异构体或非对映体形式及其药学上可接受的盐 标记有星号的碳原子可以具有任何立体化学构型，该化合物结合一种或多种黑皮质素受体并可用于治疗一种或多种黑皮质素受体相关病症或病症的药物制剂中 以及使用本发明化合物的方法。

    Piperazine melanocortin-specific compounds
    10.
    发明授权
    Piperazine melanocortin-specific compounds 有权
    哌嗪黑皮质素特异性化合物

    公开(公告)号：US07354923B2

    公开(公告)日：2008-04-08

    申请号：US10762079

    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： A61K31/497 ,  C07D403/04

    CPC分类号： C07D401/12 ,  A61K38/00 ,  C07D241/04 ,  C07D241/08 ,  C07D403/06 ,  C07D403/12 ,  C07D417/12 ,  C07D487/04 ,  C07K5/0202 ,  C07K5/021 ,  C07K5/06078 ,  C07K5/06191 ,  C07K5/081 ,  C07K5/0821 ,  C07K5/0823 ,  C07K5/0827 ,  C07K5/1008 ,  C07K5/101

    摘要： Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C═O, 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, a second amino acid residue or a second amino acid residue 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哌嗪或酮哌嗪化合物及其立体异构体和药学上可接受的盐，其中X为CH 2或CO，R 1，R 2 R 3和R 3 3如说明书中所述，优选其中R 3为具有至少一个取代或未取代的苯基或萘基芳基的D-氨基酸 环，并且其中R 3 3任选地进一步包括胺封端基团，第二氨基酸残基或具有胺封端基团的第二氨基酸残基，所述化合物是激动剂，拮抗剂或混合激动剂和拮抗剂 一种或多种黑皮质素受体，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。