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11. 发明授权

US08247530B2 N-alkylated cyclic peptide melanocortin agonists 有权
标题翻译： N-烷基化环肽黑皮质素激动剂
公开(公告)号：US08247530B2
公开(公告)日：2012-08-21
申请号：US11557408
申请日：2006-11-07
申请人： Shubh D. Sharma , Yi-Qun Shi , Kevin D. Burris , Annette Shadiack , Ramesh Rajpurohit
发明人： Shubh D. Sharma , Yi-Qun Shi , Kevin D. Burris , Annette Shadiack , Ramesh Rajpurohit
IPC分类号： A61K38/16 , A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1024
摘要： A melanocortin-4 receptor agonist cyclic peptide of the formula where R1, R2, R3, R4a, R4b, R5, R6, R7a, R7b, x, y and z are as defined in the specification, and a method of treating sexual dysfunction, including male erectile dysfunction and female sexual dysfunction, and other melanocortin 4 receptor responsive conditions and disorders.
摘要翻译： R1，R2，R3，R4a，R4b，R5，R6，R7a，R7b，x，y，z和z如说明书中所定义的黑皮质素-4受体激动剂环肽，以及治疗性功能障碍的方法，包括男性勃起功能障碍和女性性功能障碍，以及其他黑皮质素4受体反应性病症和障碍。

12. 发明授权

US07727991B2 Substituted melanocortin receptor-specific single acyl piperazine compounds 有权
标题翻译：取代的黑皮质素受体特异性单酰哌嗪化合物
公开(公告)号：US07727991B2
公开(公告)日：2010-06-01
申请号：US11464051
申请日：2006-08-11
申请人： Shubh D. Sharma , Yi-Qun Shi , Kevin D. Burris , Zhijun Wu , Papireddy Purma , Yadi Reddy Bonuga
发明人： Shubh D. Sharma , Yi-Qun Shi , Kevin D. Burris , Zhijun Wu , Papireddy Purma , Yadi Reddy Bonuga
IPC分类号： A61K31/495 , C07D295/10
CPC分类号： C07D241/04 , C07D403/12
摘要： Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q is a substituted or unsubstituted aromatic carbocyclic ring group, L, R2a, R2b, R3a, R3b, r, x and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.
摘要翻译：其中J是取代或未取代的单环或双环结构，W是具有至少一个阳离子中心，氢键给体或氢键受体的杂原子单元，Q是通式的黑皮质素受体特异性化合物及其药学上可接受的盐取代或未取代的芳族碳环基，L，R2a，R2b，R3a，R3b，r，x和y如说明书中所定义，并且带有星号的碳原子可以具有任何立体化学构型。本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。

13. 发明授权

US07727990B2 Melanocortin receptor-specific piperazine and keto-piperazine compounds 有权
标题翻译：黑皮质素受体特异性哌嗪和酮 - 哌嗪化合物
公开(公告)号：US07727990B2
公开(公告)日：2010-06-01
申请号：US11464069
申请日：2006-08-11
申请人： Shubh D. Sharma , Yi-Qun Shi , Kevin D. Burris , Zhijun Wu , Papireddy Purma , Yadi Reddy Bonuga
发明人： Shubh D. Sharma , Yi-Qun Shi , Kevin D. Burris , Zhijun Wu , Papireddy Purma , Yadi Reddy Bonuga
IPC分类号： A61K31/497 , C07D295/067
CPC分类号： C07D241/04 , C07D403/06 , C07D403/10 , C07D403/12
摘要： Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where X, W, J, Q, L1, L2, L3, R1a, R1b, R2a, and R2b are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.
摘要翻译：通式的黑皮质素受体特异性化合物及其药学上可接受的盐，其中X，W，J，Q，L1，L2，L3，R1a，R1b，R2a和R2b如本说明书中所定义，星号可以具有任何立体化学构型。本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可以用于治疗一种或多种黑皮质素受体更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。

14. 发明授权

US07425608B2 Method of making metallopeptides 失效
标题翻译：制备金属肽的方法
公开(公告)号：US07425608B2
公开(公告)日：2008-09-16
申请号：US11221210
申请日：2005-09-07
申请人： Shubh D. Sharma , Yi-Qun Shi
发明人： Shubh D. Sharma , Yi-Qun Shi
IPC分类号： C07K7/00 , C12Q1/38
CPC分类号： C07K7/06 , C07K1/047 , C07K5/0827 , C07K5/1027 , Y02P20/55
摘要： Method of making metallopeptides is provided, for use in biological, pharmaceutical and related applications. The metallopeptides are made of peptides, peptidomimetics and peptide-like constructs, and include a metal ion-binding region thereof which includes at least one orthogonal sulfur-protecting group, in which the peptide, peptidomimetic or construct is conformationally fixed on deprotection of the sulfur and complexation of the metal ion-binding region with a metal ion while the peptide, peptidomimetic or construct is cleavably bound to solid phase.
摘要翻译：提供制备金属肽的方法，用于生物，药物和相关应用。金属肽由肽，肽模拟物和肽样构建体制成，并且包括其金属离子结合区，其包含至少一个正交的硫保护基团，其中肽，拟肽或构建体在构象上固定在硫的脱保护并且金属离子结合区与金属离子的络合，而肽，拟肽或构建体可以与固相结合。

15. 发明授权

US07834017B2 Diamine-containing, tetra-substituted piperazine compounds having identical 1- and 4-substituents 有权
标题翻译：含二胺的四取代哌嗪化合物具有相同的1-取代基和4-取代基
公开(公告)号：US07834017B2
公开(公告)日：2010-11-16
申请号：US11836897
申请日：2007-08-10
申请人： Kevin Burris , Yi-Qun Shi , Shubh D. Sharma , Yadi Reddy Bonuga , Papireddy Purma
发明人： Kevin Burris , Yi-Qun Shi , Shubh D. Sharma , Yadi Reddy Bonuga , Papireddy Purma
IPC分类号： A61K31/497 , C07D403/00 , C07D295/00
CPC分类号： C07D241/04 , A61K31/495 , A61K31/496 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/12
摘要： There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.
摘要翻译：提供具有结构式I的化合物：其中基团-C（R 8）（CH 2）v CH（R 9）（CH 2）y Q和-C（R 8）（CH 2）v CH（R 9）（CH 2），R1a，R1b，R2a，R2b，R8，R9，J，Q，W，X，L2，v和y具有说明书中给出的含义。使用这些化合物治疗对人或非人哺乳动物（例如男性性功能障碍，女性性功能障碍，进食障碍，超过最佳体重，肥胖，低于最佳）的黑色素皮质素受体功能变化的病症体重或恶病质）也被描述。

16. 发明授权

US07718802B2 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：US07718802B2
公开(公告)日：2010-05-18
申请号：US11099814
申请日：2005-04-05
申请人： Shubh D. Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Zhijun Wu
发明人： Shubh D. Sharma , Yi-Qun Shi , Ramesh Rajpurohit , Zhijun Wu
IPC分类号： C07D241/04 , C07D403/06 , C07D295/023
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，R6，R7，y和z如说明书中所定义，并且具有星号的碳原子可以具有任何立体化学构型，并且任选具有一个或两个另外的环取代基定义为哪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，反向激动剂的反向激动剂或拮抗剂，并且可用于治疗一种或多种黑皮质素受体相关条件或障碍，以及使用本发明化合物的方法。

17. 发明授权

US07601753B2 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：US07601753B2
公开(公告)日：2009-10-13
申请号：US11680932
申请日：2007-03-01
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： A61K31/40 , C07D207/04
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的D-氨基酸或并且其中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，任选地具有胺封端基团，所述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，以及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。

18. 发明授权

US07342089B2 Cyclic peptides for treatment for cachexia 有权
标题翻译：循环肽治疗恶病质
公开(公告)号：US07342089B2
公开(公告)日：2008-03-11
申请号：US11174845
申请日：2005-07-05
申请人： Shubh D. Sharma , Ramesh Rajpurohit , Annette M. Shadiack , Yi-Qun Shi , Kevin D. Burris
发明人： Shubh D. Sharma , Ramesh Rajpurohit , Annette M. Shadiack , Yi-Qun Shi , Kevin D. Burris
IPC分类号： A61K38/00 , A61K38/12 , C07K7/00
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。

19. 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。

20. 发明授权

US07456184B2 Melanocortin receptor-specific compounds 失效
标题翻译：黑皮质素受体特异性化合物
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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