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1. 发明申请

WO2007021991A3 MELANOCORTIN RECEPTOR-SPECIFIC PIPERAZINE AND KETO-PIPERAZINE COMPOUNDS 审中-公开
标题翻译：梅兰康汀受体特异性哌嗪和酮哌啶化合物
公开(公告)号：WO2007021991A3
公开(公告)日：2007-07-12
申请号：PCT/US2006031474
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
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：通式（I）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，L 1，L 2，L

2. 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。

3. 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。

4. 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.

5. 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。}

6. 发明申请

WO2003013571A1 PEPTIDOMIMETICS OF BIOLOGICALLY ACTIVE METALLOPEPTIDES 审中-公开
标题翻译：生物活性金属蛋白酶的生物学功能
公开(公告)号：WO2003013571A1
公开(公告)日：2003-02-20
申请号：PCT/US2002/025574
申请日：2002-08-12
申请人： PALATIN TECHNOLOGIES, INC. , SHARMA, Shubh, D. , SHI, Yiqun , RAJPUROHIT, Ramesh , WU, Zhijun
发明人： SHARMA, Shubh, D. , SHI, Yiqun , RAJPUROHIT, Ramesh , WU, Zhijun
IPC分类号： A61K38/00
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： The invention relates to a method of deriving a peptidomimetic of a biologically active metallopeptide, wherein the peptidomimetic includes at least one non-peptide ring structure defining a template space superimposable on a corresponding defined template space of the metallopeptide, and where the peptidomimetic further includes at least two elements independently including an amino acid residu, amino acid side chain moiety or derivative thereof, the elements defining and occupying a similar descriptor space as corresponding elements of the metallopeptide. The invention further relates to peptidomimetics with a template space heterocyclic ring structure, including 5-,6 and 8-membered and 5-5 and 6-5 bicyclic fused ring structure melanocortin receptor-specific peptidomimetics.
摘要翻译：本发明涉及一种衍生生物活性金属肽的拟肽的方法，其中拟肽包括至少一个限定模板空间的非肽环结构，该模板空间可重叠在金属肽的相应限定的模板空间上，并且其中拟肽进一步包括在至少两个元素独立地包括氨基酸残基，氨基酸侧链部分或其衍生物，所述元素定义并占据与金属肽相应元素相似的描述空间。本发明还涉及具有模板空间杂环结构的肽模拟物，包括5-，6和8-元和5-5和6-5双环稠合环结构黑皮质素受体特异性肽模拟物。

7. 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。

8. 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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