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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
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。
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公开(公告)号：US07417027B2
公开(公告)日：2008-08-26
申请号：US10756212
申请日：2004-01-12
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1008 , C07K5/1013 , C07K5/1027 , C07K7/56 , C07K14/68
摘要： Linear and cyclic peptides are provided specific to one or melanocortin receptors, and which exhibit agonist, antagonist, or mixed agonist-antagonist activity. In one embodiment, a linear peptide of the following general formula is provided:
摘要翻译： 线性和环肽提供特异于一种或黑皮质素受体，并且其表现出激动剂，拮抗剂或混合的激动剂 - 拮抗剂活性。 在一个实施方案中，提供以下通式的线性肽：
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公开(公告)号：US07795378B2
公开(公告)日：2010-09-14
申请号：US11031898
申请日：2005-01-07
CPC分类号： C07K5/0827 , A61K38/00 , C07K5/0806 , C07K5/081 , C07K5/1024
摘要： A peptide of the structural formula: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, m and n are as defined. Further provided are methods for treatment of sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and combination drugs and method of use thereof, including a peptide of the invention and one or more second sexual dysfunction pharmaceutical agents.
摘要翻译： 结构式的肽或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，m和n如上所定义。 还提供了治疗性功能障碍的方法，包括勃起功能障碍和女性性功能障碍，以及联合药物及其使用方法，包括本发明的肽和一种或多种第二性功能障碍药剂。
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公开(公告)号：US20090076029A1
公开(公告)日：2009-03-19
申请号：US12130316
申请日：2008-05-30
IPC分类号： A61K31/496 , G01N33/53 , A61P3/04
CPC分类号： G01N33/74 , A61K31/496 , G01N2500/02 , G01N2800/044
摘要： Methods for selection of compounds for treatment of obesity, compounds selected by the disclosed methods, and methods of treatment of obesity, wherein a selective melanocortin-4 receptor compound is identified, which compound is further characterized in that it attenuates the binding of both an agonist, including alpha-melanocyte stimulating hormone, and an inverse agonist, including agouti-related protein, to a melanocortin receptor, including melanocortin-4 receptor.
摘要翻译： 用于选择用于治疗肥胖症的化合物的方法，通过公开的方法选择的化合物和治疗肥胖症的方法，其中鉴定了选择性黑皮质素-4受体化合物，该化合物的特征还在于其减弱激动剂 ，包括α-黑素细胞刺激激素和包括agouti相关蛋白的反向激动剂，包括黑皮质素受体，包括黑皮质素-4受体。
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公开(公告)号：US07396814B2
公开(公告)日：2008-07-08
申请号：US11036273
申请日：2005-01-14
IPC分类号： A61K38/16
CPC分类号： C07K7/06 , A61K38/00 , A61K51/0497 , A61K2121/00 , A61K2123/00 , C07K5/1024 , C07K14/575 , C07K14/68
摘要： Metallopeptide compositions are provided for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction. The metallopeptides include at least one, and preferably two, aromatic amino acid side chain moieties, and are further characterized in that the metallopeptides preferably do not bind or significantly bind to a melanocortin receptor.
摘要翻译： 提供金属肽组合物用于治疗哺乳动物的性功能障碍，包括男性性功能障碍，如勃起功能障碍和女性性功能障碍。 金属肽包括至少一个，优选两个芳族氨基酸侧链部分，其特征还在于金属肽优选不结合或显着结合黑皮质素受体。
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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
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。
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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：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
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。
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公开(公告)号：US20050124553A1
公开(公告)日：2005-06-09
申请号：US11031898
申请日：2005-01-07
申请人： Shubh Sharma , Annette Shadiack , Ramesh Rajpurohit , Wei Yang
发明人： Shubh Sharma , Annette Shadiack , Ramesh Rajpurohit , Wei Yang
CPC分类号： C07K5/0827 , A61K38/00 , C07K5/0806 , C07K5/081 , C07K5/1024
摘要： A peptide of the structural formula: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, m and n are as defined. Further provided are methods for treatment of sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and combination drugs and method of use thereof, including a peptide of the invention and one or more second sexual dysfunction pharmaceutical agents.
摘要翻译： 一种结构式的肽或其药学上可接受的盐，其中R 1，R 2，R 3，R 4 R 5，R 6，m和n如上所定义。 还提供了治疗性功能障碍的方法，包括勃起功能障碍和女性性功能障碍，以及联合药物及其使用方法，包括本发明的肽和一种或多种第二性功能障碍药剂。
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公开(公告)号：US20050038230A1
公开(公告)日：2005-02-17
申请号：US10756212
申请日：2004-01-12
申请人： Shubh Sharma , Annette Shadiack , Wei Yang , Ramesh Rajpurohit
发明人： Shubh Sharma , Annette Shadiack , Wei Yang , Ramesh Rajpurohit
IPC分类号： A61K38/00 , A61P1/14 , A61P3/04 , A61P15/00 , A61P15/10 , C07K5/10 , C07K5/103 , C07K7/06 , C07K7/52 , C07K7/56 , C07K14/68 , C07K14/705
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1008 , C07K5/1013 , C07K5/1027 , C07K7/56 , C07K14/68
摘要： Linear and cyclic peptides are provided specific to one or melanocortin receptors, and which exhibit agonist, antagonist, or mixed agonist-antagonist activity. In one embodiment, a linear peptide of the following general formula is provided:
摘要翻译： 线性和环肽提供为特异于一种或黑皮质素受体，并且其表现出激动剂，拮抗剂或混合的激动剂 - 拮抗剂活性。 在一个实施方案中，提供以下通式的线性肽：
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