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    Melanocortin metallopeptides for treatment of sexual dysfunction
    1.
    发明授权
    Melanocortin metallopeptides for treatment of sexual dysfunction 有权
    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。

    Pyrrolidine Melanocortin-Specific Compounds
    2.
    发明申请
    Pyrrolidine Melanocortin-Specific Compounds 有权
    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。

    Metallopeptide compounds
    6.
    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
    7.
    发明申请
    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：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。

    Identification of target-specific folding sites in peptides and proteins
    8.
    发明申请
    Identification of target-specific folding sites in peptides and proteins 审中-公开
    鉴定肽和蛋白质中的靶标特异性折叠位点

    公开(公告)号：US20050014193A1

    公开(公告)日：2005-01-20

    申请号：US10464117

    申请日：2003-06-17

    申请人： Shubh Sharma ,  Yi-Qun Shi

    发明人： Shubh Sharma ,  Yi-Qun Shi

    IPC分类号： C40B30/04 ,  G01N33/53 ,  G01N33/68

    CPC分类号： C40B30/04 ,  G01N33/6818

    摘要： The invention provides methods for identification and determination of target-specific folding sites in peptides and proteins, including a method for determining a secondary structure binding to a target of interest 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 two adjacent residues in a known primary sequence of a peptide or protein. The resulting sequence, which includes a minimum of the residue or mimetic containing a nitrogen atom and a sulfur atom available for binding to a metal ion and two residues on the amino terminus side thereof, 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 demonstrating binding or functional activity is selected. The invention further provides methods to determine the specific sequence and local three-dimensional structure of that portion of peptides or proteins that bind to a receptor or target of interest, or mediate a biological activity of interest and methods to determine the pharmacophore of receptors or targets of interest. The invention provides for defined pharmacophores of receptors or targets of interest and directed libraries for identification and determination of target-specific folding sites in peptides and proteins and for identification and determination of pharmacophores of receptors or targets of interest.

    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折叠位点的方法，包括确定结合感兴趣靶标的已知亲本多肽中与目的靶标结合的二级结构的方法。 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在肽或蛋白质的已知一级序列中的两个相邻残基之间被连续取代或插入两个相邻残基之间的单个残基。 所得到的序列与金属离子络合，其中包含最少的含有氮原子的残基或模拟物，可用于与金属离子结合的硫原子和氨基末端侧的两个残基，由此形成金属肽。 然后将所得金属肽用于与感兴趣的靶标相关的结合或功能测定中，并且选择显示结合或功能活性的金属肽。 本发明还提供了确定结合感兴趣受体或靶标的肽或蛋白质部分的特定序列和局部三维结构或介导感兴趣的生物活性的方法，以及确定受体或靶标的药效团的方法 出于兴趣。 本发明提供了感兴趣的受体或靶标的定义的药效团和用于鉴定和测定肽和蛋白质中的靶特异性折叠位点的定向文库，以及用于鉴定和测定感兴趣的受体或靶标的药效团。

    Melanocortin-1 Receptor-Specific Cyclic Peptides
    9.
    发明申请
    Melanocortin-1 Receptor-Specific Cyclic Peptides 有权
    黑皮质素-1受体特异性环肽

    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

    IPC分类号： A61K38/12 ,  A61P37/06 ,  A61P19/02 ,  C07K7/64 ,  A61P29/00

    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。