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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：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：US07345144B2
公开(公告)日：2008-03-18
申请号：US11174851
申请日：2005-07-05
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：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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公开(公告)号：US20080234289A1
公开(公告)日：2008-09-25
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： A61K31/495 , C07D241/04 , A61K31/496 , A61P3/04 , C07D403/06
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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公开(公告)号：US07732451B2
公开(公告)日：2010-06-08
申请号：US11036282
申请日：2005-01-14
申请人： Shubh D. Sharma , Annette M. Shadiack , Yiqun Shi , Zhijun Wu , Ramesh Rajpurohit , Kevin D. Burris , Papireddy Purma
发明人： Shubh D. Sharma , Annette M. Shadiack , Yiqun Shi , Zhijun Wu , Ramesh Rajpurohit , Kevin D. Burris , Papireddy Purma
IPC分类号： A61K31/4965 , C07D295/023
CPC分类号： A61K31/495 , A61K31/496
摘要： A method of modulating energy homeostasis in a mammal without eliciting a sexual response by administration of a therapeutically effective amount of a pharmaceutical composition including a melanocortin receptor compound of the formula: where R1 is a bond or a linker unit including from one to six backbone atoms and an unsubstituted naphthalene group, and L, R2, R3 and Rx are as defined in the specification.
摘要翻译： 一种通过施用治疗有效量的药物组合物调节哺乳动物体内能量稳态的方法，其不引起性反应，所述药物组合物包括下式的黑皮质素受体化合物：其中R 1是键或包含一至六个骨架原子的连接体单元 和未取代的萘基，L，R2，R3和Rx如说明书中所定义。
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公开(公告)号：US07342089B2
公开(公告)日：2008-03-11
申请号：US11174845
申请日：2005-07-05
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：US07235625B2
公开(公告)日：2007-06-26
申请号：US11139730
申请日：2005-05-26
CPC分类号： C07K14/685 , A61K31/519 , A61K33/24 , A61K38/12 , A61K45/06 , Y10S436/811 , A61K2300/00
摘要： Multiple agent therapy for treatment of sexual dysfunction, including male erectile dysfunction, with sequential administration a type V phosphodiesterase inhibitor (PDE-5), such as sildenafil, preferably wherein the PDE-5 inhibitor is administered by oral dose means, and a melanocortin 3 and/or 4 receptor agonist, such as Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)-OH (PT-141) preferably wherein the PT-141 is formulated for and administered by intranasal means, and further preferably wherein the PDE-5 inhibitor is administered prior to PT-141.
摘要翻译： 用于治疗性功能障碍（包括男性勃起功能障碍）的多药物治疗，连续施用V型磷酸二酯酶抑制剂（PDE-5），例如西地那非，其中PDE-5抑制剂通过口服剂量方式施用，黑皮质素3 和/或4受体激动剂，例如Ac-Nle-cyclo（-Asp-His-D-Phe-Arg-Trp-Lys）-OH（PT-141），优选其中PT-141配制用于鼻内给药 是指，进一步优选其中PDE-5抑制剂在PT-141之前施用。
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