专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2011063366A1 MELANOCORTIN-1 RECEPTOR-SPECIFIC CYCLIC PEPTIDES 审中-公开
标题翻译：梅毒素-1受体特异性循环肽
公开(公告)号：WO2011063366A1
公开(公告)日：2011-05-26
申请号：PCT/US2010/057699
申请日：2010-11-23
申请人： PALATIN TECHNOLOGIES, INC. , YANG, Wei , SHI, Yi-qun
发明人： YANG, Wei , SHI, Yi-qun
IPC分类号： C07K7/50 , C07K7/54 , C07K7/56
CPC分类号： C07K7/56 , A61K31/407 , A61K38/00 , C07K7/54 , C07K14/68
摘要： Melanocortin receptor-specific cyclic peptides of the formula (I) where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 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：式（I）的黑皮质素受体特异性环肽，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9如说明书中所定义，组合物和制剂包括前述式的肽或其盐以及预防，改善或治疗黑皮质素-1受体介导或反应性疾病，适应症，病症和综合征的方法。

2. 发明申请

WO2010144344A3 MELANOCORTIN RECEPTOR-SPECIFIC PEPTIDES 审中-公开
公开(公告)号：WO2010144344A3
公开(公告)日：2010-12-16
申请号：PCT/US2010/037589
申请日：2010-06-07
申请人： PALATIN TECHNOLOGIES, INC. , SHI, Yi-qun , SHARMA, Shubh, D. , DODD, John, H. , YANG, Wei , CHEN, Xin
发明人： SHI, Yi-qun , SHARMA, Shubh, D. , DODD, John, H. , YANG, Wei , CHEN, Xin
IPC分类号： A61K38/00 , C07K5/00 , A61K33/16
摘要： Melanocortin receptor-specific cyclic peptides of the formula where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and z 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.

3. 发明申请

WO2008090357A2 MELANOCORTIN RECEPTOR-SPECIFIC PIPERAZINE COMPOUNDS 审中-公开
标题翻译：梅兰康汀受体特异性哌嗪化合物
公开(公告)号：WO2008090357A2
公开(公告)日：2008-07-31
申请号：PCT/GB2008000263
申请日：2008-01-24
申请人： PALATIN TECHNOLOGIES INC , SHARMA SHUBH D , SHI YI-QUN
发明人： SHARMA SHUBH D , SHI YI-QUN
IPC分类号： C07D401/14 , A61K31/495 , A61P15/00 , A61P25/00 , C07D241/04 , C07D295/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D407/06 , C07D409/06 , C07D413/12 , C07D417/06 , C07D417/12
CPC分类号： C07D241/04 , C07D295/10 , C07D401/12 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： Melanocortin receptor-specific piperazine compounds, of the formula (I) wherein the variables are as defined in the specification, and pharmaceutically acceptable salts thereof. 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：式（I）的黑皮质素受体特异性哌嗪化合物，其中变量如说明书中所定义，及其药学上可接受的盐。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。

4. 发明申请

WO2004075830A3 KNOCKOUT IDENTIFICATION OF TARGET-SPECIFIC SITES IN PEPTIDES 审中-公开
标题翻译：针对目标特异性位点的筛选鉴定
公开(公告)号：WO2004075830A3
公开(公告)日：2006-09-28
申请号：PCT/US2004002933
申请日：2004-02-02
申请人： PALATIN TECHNOLOGIES INC , SHARMA SHUBH D , SHI YI-QUN , RAJPUROHIT RAMESH , BASTOS MARGARITA , CAI HUI-ZHI
发明人： SHARMA SHUBH D , SHI YI-QUN , RAJPUROHIT RAMESH , BASTOS MARGARITA , CAI HUI-ZHI
IPC分类号： G01N33/53 , A61K20060101 , A61K6/00 , C07K1/04 , C07K5/103 , C07K5/107 , C07K5/117 , G01N33/567 , G01N33/68
CPC分类号： C07K5/1008 , C07K1/047 , C07K5/1016 , C07K5/1024 , G01N33/6803
摘要： The invention provides methods for identification and determination of target-specific sites in peptides and proteins, including a method for determining the primary sequence of a secondary structure 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 adjacent residues in a known primary sequence of a peptide or protein. The resulting sequence 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(s) which result in significant or substantially decreased or changed binding or functionality are determined to identify the primary sequence involved in such binding or functionality.
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位点的方法，包括确定结合目的靶标的已知亲本多肽内的二级结构的一级序列的方法。在本发明的一个实施方案中，含有可用于与金属离子结合的氮原子和硫原子的残基或模拟物连续取代肽或蛋白质的已知一级序列中相邻残基之间或插入其中的单个残基。所得到的序列与金属离子络合，从而形成金属肽。然后将所得金属肽用于与感兴趣靶标相关的结合或功能测定，并确定导致显着或显着降低或改变的结合或功能的金属肽，以鉴定涉及这种结合或功能的一级序列。

5. 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。

6. 发明申请

WO2007021990A3 MELANOCORTIN RECEPTOR-SPECIFIC PIPERAZINE COMPOUNDS WITH DIAMINE GROUPS 审中-公开
公开(公告)号：WO2007021990A3
公开(公告)日：2007-02-22
申请号：PCT/US2006/031472
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 , C07D241/04
摘要： Melanocortin receptor-specific compounds with diamine groups of the general formula (I) and pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L 1 , L 2 , L 3 , R 1a , R 1b , R 2a , R 2b and X 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.

7. 发明申请

WO2007021990A2 MELANOCORTIN RECEPTOR-SPECIFIC PIPERAZINE COMPOUNDS WITH DIAMINE GROUPS 审中-公开
标题翻译：具有DIAMINE组的MELANOCORTIN受体特异性哌嗪化合物
公开(公告)号：WO2007021990A2
公开(公告)日：2007-02-22
申请号：PCT/US2006031472
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 with diamine groups of the general formula (I) and pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L 1 , L 2 , L 3 , R 1a , R 1b , R 2a , R 2b and X 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：具有通式（I）的二胺基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W是具有至少一个阳离子中心，氢键供体或氢键受体的二胺杂原子单元，J，Q，L _{2a，R 2b和X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。}

8. 发明申请

WO2004075830A2 KNOCKOUT IDENTIFICATION OF TARGET-SPECIFIC SITES IN PEPTIDES 审中-公开
标题翻译：针对目标特异性位点的筛选鉴定
公开(公告)号：WO2004075830A2
公开(公告)日：2004-09-10
申请号：PCT/US2004/002933
申请日：2004-02-02
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yi-Qun , RAJPUROHIT, Ramesh , BASTOS, Margarita , CAI, Hui-Zhi
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun , RAJPUROHIT, Ramesh , BASTOS, Margarita , CAI, Hui-Zhi
IPC分类号： A61K
CPC分类号： C07K5/1008 , C07K1/047 , C07K5/1016 , C07K5/1024 , G01N33/6803
摘要： The invention provides methods for identification and determination of target-specific sites in peptides and proteins, including a method for determining the primary sequence of a secondary structure 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 adjacent residues in a known primary sequence of a peptide or protein. The resulting sequence 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(s) which result in significant or substantially decreased or changed binding or functionality are determined to identify the primary sequence involved in such binding or functionality.
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位点的方法，包括确定结合目的靶标的已知亲本多肽内的二级结构的一级序列的方法。在本发明的一个实施方案中，含有可用于与金属离子结合的氮原子和硫原子的残基或模拟物连续取代肽或蛋白质的已知一级序列中相邻残基之间或插入其中的单个残基。所得到的序列与金属离子络合，从而形成金属肽。然后将所得金属肽用于与感兴趣靶标相关的结合或功能测定，并确定导致显着或显着降低或改变的结合或功能的金属肽，以鉴定涉及这种结合或功能的一级序列。

9. 发明申请

WO2002064734A3 IDENTIFICATION OF TARGET-SPECIFIC FOLDING SITES IN PEPTIDES AND PROTEINS 审中-公开
公开(公告)号：WO2002064734A3
公开(公告)日：2002-08-22
申请号：PCT/US2001/050075
申请日：2001-12-19
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yi-Qun
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun
IPC分类号： A61K51/00
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 or 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.

10. 发明申请

WO2002064734A2 IDENTIFICATION OF TARGET-SPECIFIC FOLDING SITES IN PEPTIDES AND PROTEINS 审中-公开
标题翻译：鉴定目标特异性折叠位点在蛋白质和蛋白质中的鉴定
公开(公告)号：WO2002064734A2
公开(公告)日：2002-08-22
申请号：PCT/US2001/050075
申请日：2001-12-19
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yi-Qun
发明人： SHARMA, Shubh, D. , SHI, Yi-Qun
IPC分类号： C12N
CPC分类号： C07K14/4711 , C07K1/047 , C07K5/1008 , C07K5/1016 , C07K5/1024 , G01N33/6803
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 or 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。本发明提供了确定的药效团或感兴趣的受体或靶标和用于鉴定和确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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式