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1. 发明申请

WO2009152079A1 MELANOCORTIN RECEPTOR-SPECIFIC PEPTIDES FOR TREATMENT OF SEXUAL DYSFUNCTION 审中-公开
标题翻译： MELANOCORTIN受体特异性肽用于治疗性功能障碍
公开(公告)号：WO2009152079A1
公开(公告)日：2009-12-17
申请号：PCT/US2009/046571
申请日：2009-06-08
申请人： PALATIN TECHNOLOGIES, INC. , SHI, Yi-Qun , SHARMA, Shubh, D. , YANG, Wei , CHEN, Xin
发明人： SHI, Yi-Qun , SHARMA, Shubh, D. , YANG, Wei , CHEN, Xin
IPC分类号： A61K38/00 , A61K31/44
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , A61K45/06 , C07K14/685
摘要： A melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.
摘要翻译：下式的黑皮质素受体激动剂环肽其中R，x和y如说明书中所定义，包括上述式的肽的组合物和制剂，以及预防，改善或治疗黑皮质素受体介导的疾病，适应症，条件和综合征，包括性功能障碍如男性勃起功能障碍和女性性功能障碍。

2. 发明申请

WO2009151383A1 MELANOCORTIN RECEPTOR-SPECIFIC PEPTIDES FOR THE TREATMENT OF OBESITY AND OTHER DISEASES ASSOCIATED WITH MELANOCORTIN RECEPTOR FUNCTION 审中-公开
标题翻译：用于治疗与梅兰康宁受体功能相关的肥胖和其他疾病的梅兰康汀受体特异性肽
公开(公告)号：WO2009151383A1
公开(公告)日：2009-12-17
申请号：PCT/SE2009/050683
申请日：2009-06-08
申请人： PALATIN TECHNOLOGIES, INC. , ASTRAZENECA AB , CHEN, Xin , SHARMA, Shubh D , SHI, Yi-Qun , YANG, Wei
发明人： CHEN, Xin , SHARMA, Shubh D , SHI, Yi-Qun , YANG, Wei
IPC分类号： C07K7/64 , A61K38/12 , A61P3/06 , A61P3/08
CPC分类号： C07K7/54 , A61K38/00 , C07K7/06
摘要： Melanocortin receptor-specific cyclic peptides of the formula (I) where R 1 , R 2 , R 3 , R 4 , x and y are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including obesity, diabetes, modulation of feeding behavior and related metabolic syndrome.
摘要翻译：其中R1，R2，R3，R4，x和y如说明书中所定义的式（I）的黑皮质素受体特异性环肽，包括前述式的肽的组合物和制剂，以及预防，改善或治疗的方法黑皮质素受体介导的疾病，适应症，病症和综合征，包括肥胖症，糖尿病，饲养行为的调节和相关的代谢综合征。

3. 发明申请

WO2002064091A2 MELANOCORTIN METALLOPEPTIDES FOR TREATMENT OF SEXUAL DYSFUNCTION 审中-公开
标题翻译： MELANOCORTIN金属蛋白酶治疗性功能障碍
公开(公告)号：WO2002064091A2
公开(公告)日：2002-08-22
申请号：PCT/US2002/004431
申请日：2002-02-13
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yi-Qun , YANG, Wei , CAI, Hui-Zhi , SHADIACK, Annette
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun , YANG, Wei , CAI, Hui-Zhi , SHADIACK, Annette
IPC分类号： A61K
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。

4. 发明申请

WO2007021991A2 MELANOCORTIN RECEPTOR-SPECIFIC PIPERAZINE AND KETO-PIPERAZINE COMPOUNDS 审中-公开
标题翻译：黑色素受体特异性哌嗪和酮哌嗪化合物
公开(公告)号：WO2007021991A2
公开(公告)日：2007-02-22
申请号：PCT/US2006/031474
申请日：2006-08-11
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yi-Qun , BURRIS, Kevin , WU, Zhijun , PURMA, Papireddy , BONUGA, Yadi, Reddy
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun , BURRIS, Kevin , WU, Zhijun , PURMA, Papireddy , BONUGA, Yadi, Reddy
IPC分类号： A61K31/496 , A61K31/495 , C07D403/02
CPC分类号： C07D241/04 , C07D403/12
摘要： Melanocortin receptor-specific compounds of the general formula (I) and pharmaceutically acceptable salts thereof, where X, W, J, Q, L 1 , L 2 , L 3 , R 1a , R 1b , R 2a , and R 2b 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：其中X，W，J，Q，L 1，L 2 L 3，R 1a，R 1b，R 2a和R 2，其中R 1，R 2， 2b如说明书中所定义，且用星号标记的碳原子可以具有任何立体化学构型。本文公开的化合物与一种或多种黑皮质素受体结合，并且可以是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，并且可用于治疗一种或多种黑皮质素受体更多黑皮素受体相关的病症或障碍，包括特别治疗肥胖和相关病症。

5. 发明申请

WO2004098602A1 MELANOCORTIN RECEPTOR-SPECIFIC COMPOUNDS 审中-公开
标题翻译：甲氧苄啶受体特异性化合物
公开(公告)号：WO2004098602A1
公开(公告)日：2004-11-18
申请号：PCT/US2004/013803
申请日：2004-05-03
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yi-Qun , WU, Zhijun , RAJPUROHIT, Ramesh , SHADIACK, Annette, M. , PURMA, Papireddy , BURRIS, Kevin, D.
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun , WU, Zhijun , RAJPUROHIT, Ramesh , SHADIACK, Annette, M. , PURMA, Papireddy , BURRIS, Kevin, D.
IPC分类号： A61K31/495
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, R 1 , R 2a , R 2b , R 3 , R 4a , R 4b , R 5a and R 5b 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，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个或更多的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的病症或病症，以及使用该化合物的方法发明。

6. 发明申请

WO2006014559A3 CYCLIC PEPTIDES FOR TREATMENT OF CACHEXIA 审中-公开
公开(公告)号：WO2006014559A3
公开(公告)日：2006-02-09
申请号：PCT/US2005/024138
申请日：2005-07-06
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , RAJPUROHIT, Ramesh , BURRIS, Kevin, B. , SHI, Yi-Qun , SHADIACK, Annette, M.
发明人： SHARMA, Shubh, D. , RAJPUROHIT, Ramesh , BURRIS, Kevin, B. , SHI, Yi-Qun , SHADIACK, Annette, M.
IPC分类号： A61K38/12 , C07K7/64 , C12Q1/68
摘要： A highly selective melanocortin-4 receptor antagonist cyclic hexapeptide of the formula: (I) where R 1 , R 2 , R 3a , R 3b , R 4 , R 5, 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.

7. 发明申请

WO2008017852A1 DIAMINE-CONTAINING, TETRA- SUBSTITUTED PIPERAZINE COMPOUNDS AS MELANOCORTIN RECEPTOR MODULATORS 审中-公开
标题翻译：含有DIAMINE，作为MELANOCORTIN受体调节剂的替代哌替啶化合物
公开(公告)号：WO2008017852A1
公开(公告)日：2008-02-14
申请号：PCT/GB2007/003039
申请日：2007-08-10
申请人： PALATIN TECHNOLOGIES, INC. , SNODIN, Michael, David , SHARMA, Shubh, D. , SHI, Yi-Qun , BURRIS, Kevin , PURMA, Papireddy , BONUGA, Yadi, Reddy
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun , BURRIS, Kevin , PURMA, Papireddy , BONUGA, Yadi, Reddy
IPC分类号： C07D241/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/12 , A61K31/495 , A61P15/00 , A61P25/00
CPC分类号： C07D241/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/12
摘要： There is provided compounds having the formula of structure (I): wherein the groups -C(R 8 )(CH 2 ) v CH(R 9 )(CH 2 ) y -Q and -C(R 8 )(CH 2 ) v CH(R 9 )(CH 2 ) y -J are the same, and R 1a , R 1b , R 2a , R 2b , R 8 , R 9 , J, Q, W, X, L 2 , 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：提供具有式（I）结构式的化合物：其中基团-C（R 8）（CH 2）2 CH（CH 3）（CH 2）q（CH 3）q（CH 3）（CH 3）（CH 2）2 CH 2（CH 2）2 CH 2 CH（R 9）（CH 2），和R 1a，R 1b，R 2a，R 2b，R 8，O，，R 9，J，Q，W，X，L 2，v和y具有在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。

8. 发明申请

WO2006014552A2 CYCLIC PEPTIDES FOR TREATMENT OF CACHEXIA 审中-公开
标题翻译：用于治疗慢性乙型肝炎的循环肽
公开(公告)号：WO2006014552A2
公开(公告)日：2006-02-09
申请号：PCT/US2005/024125
申请日：2005-07-06
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , RAJPUROHIT, Ramesh , BURRIS, Kevin, B. , SHI, Yi-Qun , SHADIACK, Annette, M.
发明人： SHARMA, Shubh, D. , RAJPUROHIT, Ramesh , BURRIS, Kevin, B. , SHI, Yi-Qun , SHADIACK, Annette, M.
IPC分类号： C07K5/12 , A61K38/12
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 R 1 , R 2 , R 3 , R 4a , R 4b , R 5 , R 6 , R 7 , 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：一种高度选择性的黑皮质素-4受体拮抗剂环肽，其中R

9. 发明申请

WO2005102340A1 PIPERAZINE MELANOCORTIN-SPECIFIC COMPOUNDS 审中-公开
标题翻译：哌嗪吗啉特异性化合物
公开(公告)号：WO2005102340A1
公开(公告)日：2005-11-03
申请号：PCT/US2004/001462
申请日：2004-01-21
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yi-Qun , WU, Zhijun , RAJPUROHIT, Ramesh
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun , WU, Zhijun , RAJPUROHIT, Ramesh
IPC分类号： A61K31/495
CPC分类号： C07D403/12 , C07D241/08 , C07D403/06
摘要： Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or C=O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 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：具有结构（I）的黑皮质素受体特异性哌嗪或酮哌嗪化合物; 其中X为CH 2或C = O，R 1，R 2和R 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-氨基酸并且其中R 3任选地还包括胺封端基团，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，并且具有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。

10. 发明申请

WO2005079574A1 BICYCLIC MELANOCORIN-SPECIFIC COMPOUNDS 审中-公开
标题翻译：双相MELANOCORIN特异性化合物
公开(公告)号：WO2005079574A1
公开(公告)日：2005-09-01
申请号：PCT/US2004/001505
申请日：2004-01-21
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yi-Qun , WU, Zhijun , RAJPUROHIT, Ramesh
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun , WU, Zhijun , RAJPUROHIT, Ramesh
IPC分类号： A01N43/52
CPC分类号： C07D487/04
摘要： Melanocortin receptor-specific bicyclic compounds having the structure (I) and stereoisomer and pharmaceutically acceptable salts thereof, where R 1 , R 2 , R 3 X and z are as described in the specification, which are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptorrelated disorders and conditions. Pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
摘要翻译：具有结构（I）及其立体异构体和药学上可接受的盐的黑皮质素受体特异性双环化合物，其中R 1，R 2，R 3 X和Z如本说明书所述，其是一种或多种激动剂，拮抗剂或混合激动剂和拮抗剂黑皮质素受体，并且可用于治疗黑皮质素受体相关疾病和病症。还公开了含有结构（I）化合物和与其用途有关的方法的药物组合物。

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