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公开(公告)号：US20110118172A1
公开(公告)日：2011-05-19
申请号：US12989346
申请日：2009-04-23
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
IPC分类号： A61K38/08 , C07K7/06 , A61P35/04 , A61P35/00 , A61P15/00 , A61P25/28 , A61P25/00 , A61P15/04 , A61P3/08 , A61P3/00 , A61P15/08
摘要： The invention provides a stable metastin derivative having excellent biological activities (a cancer metastasis-inhibiting activity, a cancer proliferation-inhibiting activity, a gonadotropin secretion-promoting activity, a sex hormone secretion-promoting activity, etc.). By replacing the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, the blood stability and solubility of the metastin derivative can be more improved, the gel tendency of the metastin derivative can be reduced, the pharmacokinetics of the metastin derivative can be improved, and the metastin derivative can exhibit an excellent cancer metastasis-inhibiting activity and cancer proliferation-inhibiting activity. The metastin derivative can also exhibit a gonadotropin secretion-inhibiting activity, a sex hormone secretion-inhibiting activity, etc.
摘要翻译： 本发明提供了具有优异生物活性（癌转移抑制活性，癌增殖抑制活性，促性腺激素分泌促进活性，性激素分泌促进活性等）的稳定的转氨酶衍生物。 通过用本发明的转氨酶衍生物中的特定氨基酸替代组氨酸的氨基酸，可以进一步改善转氨酶衍生物的血液稳定性和溶解性，降低转氨酶衍生物的凝胶倾向，降低药代动力学 可以改善转氨酶衍生物，并且转氨酶衍生物可表现出优异的癌转移抑制活性和癌细胞增殖抑制活性。 转氨酶衍生物也可表现出促性腺激素分泌抑制活性，性激素分泌抑制活性等。
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公开(公告)号：US07786083B2
公开(公告)日：2010-08-31
申请号：US11977477
申请日：2007-10-24
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
IPC分类号： A61K38/08
CPC分类号： C07K14/4703 , A61K38/00
摘要： The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotropic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.).By substituting the constituent amino acids of metastin with specific amino acids, the metastin derivatives of the present invention achieve more improved blood stability, solubility, etc., reduced gelation tendency, improved pharmacokinetics, as well as exhibit an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity. The metastin derivatives of the present invention also have a gonadotropic hormone secretion suppressing activity, sex hormone secretion suppressing activity, etc.
摘要翻译： 本发明提供具有优异生物活性（癌转移抑制活性，癌生长抑制活性，促性腺激素分泌刺激活性，性激素分泌刺激活性等）的稳定的转氨酶衍生物。 通过用特定氨基酸取代组氨酸的氨基酸，本发明的转氨酶衍生物获得更好的血液稳定性，溶解性等，降低的凝胶化趋势，改善的药代动力学，以及表现出优异的癌转移抑制活性或 癌症生长抑制活性。 本发明的转氨酶衍生物也具有促性腺激素分泌抑制活性，性激素分泌抑制活性等。
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公开(公告)号：US20090298765A1
公开(公告)日：2009-12-03
申请号：US12286671
申请日：2008-10-01
申请人： Chieko Kitada , Taiji Asami , Naoki Nishizawa
发明人： Chieko Kitada , Taiji Asami , Naoki Nishizawa
CPC分类号： C07K14/4703 , A61K38/00
摘要： The invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, etc.). By modifying the constituent amino acids of metastin with specific modifying groups, metastin derivatives having more improved blood stability, etc. than native metastin and showing excellent cancer metastasis suppressing activity or cancer growth suppressing activity have been found. Furthermore, it has been found that these metastin derivatives exhibit effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc., which are wholly different from the effects heretofore known.
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公开(公告)号：US20060241051A1
公开(公告)日：2006-10-26
申请号：US10540494
申请日：2003-12-26
申请人： Chieko Kitada , Taiji Asami , Naoki Nishizawa , Tetsuya Ohtaki , Naoki Tarui , Hirokazu Matsumoto , Jiro Noguchi , Hisanori Matsui
发明人： Chieko Kitada , Taiji Asami , Naoki Nishizawa , Tetsuya Ohtaki , Naoki Tarui , Hirokazu Matsumoto , Jiro Noguchi , Hisanori Matsui
摘要： The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivitives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action.
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公开(公告)号：US09260500B2
公开(公告)日：2016-02-16
申请号：US13381737
申请日：2010-07-01
申请人： Taiji Asami , Naoki Nishizawa , Ayumu Niida , Yusuke Adachi
发明人： Taiji Asami , Naoki Nishizawa , Ayumu Niida , Yusuke Adachi
IPC分类号： A61K38/10 , A61P3/04 , C07K7/08 , C07K14/575 , A61K38/00
CPC分类号： C07K14/575 , A61K38/00
摘要： The present invention aims to provide a peptide having a superior Y2 receptor agonist action and useful as an agent for the prophylaxis or treatment of obesity and the like.A peptide represented by the formula: P1—X1-A25-A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-NH2 wherein each symbol is as described in the specification, or a salt thereof.
摘要翻译： 本发明的目的在于提供具有优异的Y2受体激动剂作用的肽，可用作预防或治疗肥胖症等的药剂。 由式：P1-X1-A25-A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-NH2表示的肽，其中每个符号如说明书中所述，或其盐 。
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公开(公告)号：US09175037B2
公开(公告)日：2015-11-03
申请号：US13263630
申请日：2010-04-08
申请人： Taiji Asami , Hiroshi Inooka , Naoki Nishizawa
发明人： Taiji Asami , Hiroshi Inooka , Naoki Nishizawa
摘要： An object of the present invention is to provide a novel anorectic agent. Another object of the invention is to provide an NMU derivative which exhibits a high anorectic effect even when administered in a usual manner, for example, peripherally. These objects can be achieved by the compound represented by formula (I) or a salt thereof. In formula (I), Y represents a polypeptide containing an amino acid sequence set forth in SEQ ID NO.: 1 wherein 1 to 4 amino acids are substituted; X represents a methoxypolyethylene glycol; X′ is absent or represents a methoxypolyethylene glycol; and a moiety represented by formula: La-Lb-[Lc]j represents a linker.
摘要翻译： 本发明的目的是提供一种新型的厌食剂。 本发明的另一个目的是提供即使以常规方式（例如外周）施用也显示出高的厌食症的NMU衍生物。 这些目的可以通过式（I）表示的化合物或其盐来实现。 式（I）中，Y表示含有1〜4个氨基酸被取代的SEQ ID NO：1所示的氨基酸序列的多肽。 X表示甲氧基聚乙二醇; X'不存在或表示甲氧基聚乙二醇; 并且由式：La-Lb- [Lc] j表示的部分代表连接体。
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公开(公告)号：US08404643B2
公开(公告)日：2013-03-26
申请号：US12258023
申请日：2008-10-24
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
IPC分类号： A61K38/08
CPC分类号： C07K14/4703 , A61K38/00
摘要： The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotrophic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, blood stability, solubility, etc. are more improved, gelation tendency is reduced, pharmacokinetics are also improved, and an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity is exhibited. Furthermore, the metastin derivative of the present invention has the effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc.
摘要翻译： 本发明提供具有优异生物活性（癌转移抑制活性，癌生长抑制活性，促性腺激素分泌刺激活性，性激素分泌刺激活性等）的稳定的转氨酶衍生物。 通过在本发明的转氨酶衍生物中代替具有特定氨基酸的组氨酸的氨基酸，血液稳定性，溶解性等进一步提高，凝胶化倾向降低，药代动力学改善，癌转移抑制活性优异， 显示出癌症生长抑制活性。 此外，本发明的转氨酶衍生物具有抑制促性腺激素分泌，抑制性激素分泌等作用。
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公开(公告)号：US20120094899A1
公开(公告)日：2012-04-19
申请号：US13263630
申请日：2010-04-08
申请人： Taiji Asami , Hiroshi Inooka , Naoki Nishizawa
发明人： Taiji Asami , Hiroshi Inooka , Naoki Nishizawa
摘要： An object of the present invention is to provide a novel anorectic agent. Another object of the invention is to provide an NMU derivative which exhibits a high anorectic effect even when administered in a usual manner, for example, peripherally. These objects can be achieved by the compound represented by formula (I) or a salt thereof. In formula (I), Y represents a polypeptide containing an amino acid sequence set forth in SEQ ID NO.: 1 wherein 1 to 4 amino acids are substituted; X represents a methoxypolyethylene glycol; X′ is absent or represents a methoxypolyethylene glycol; and a moiety represented by formula: La-Lb-[Lc]j represents a linker.
摘要翻译： 本发明的目的是提供一种新型的厌食剂。 本发明的另一个目的是提供即使以常规方式（例如外周）施用也显示出高的厌食症的NMU衍生物。 这些目的可以通过式（I）表示的化合物或其盐来实现。 式（I）中，Y表示含有1〜4个氨基酸被取代的SEQ ID NO：1所示的氨基酸序列的多肽。 X表示甲氧基聚乙二醇; X'不存在或表示甲氧基聚乙二醇; 并且由式：La-Lb- [Lc] j表示的部分代表连接体。
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公开(公告)号：US20120094898A1
公开(公告)日：2012-04-19
申请号：US13271763
申请日：2011-10-12
申请人： Taiji Asami , Naoki Nishizawa , Yoko Kanematsu
发明人： Taiji Asami , Naoki Nishizawa , Yoko Kanematsu
CPC分类号： C07K14/575 , A61K38/00
摘要： The present invention relates to a peptide derivative selected from the group consisting of PEG20k(AL)-β-Ala-Tyr-Nal(1)-Leu-Phe-Arg-Pro-Arg-Asn-NH2, PEG20k(AL)-β-Ala-Tyr-Nal(2)-Leu-Phe-Arg-Pro-Arg-Asn-NH2, PEG20k(AL)-NpipAc-Tyr-Nal(2)-Leu-Phe-Arg-Pro-Arg-Asn-NH2, PEG20k(AL)-NpipAc-Tyr-Nal(2)-Leu-Phe-Arg-Ala-Arg-Asn-NH2, PEG20k(AL)-PEG(2)-Tyr-Nal(2)-Leu-Phe-Arg-NMeAla-Arg-Asn-NH2, PEG20k(AL)-Pic(4)-Tyr-Nal(2)-Leu-Phe-Arg-NMeAla-Arg-Asn-NH2, PEG20k(AL)-Acp-Tyr-Nal(2)-Leu-Phe-Arg-NMeAla-Arg-Asn-NH2, and PEG20k(AL)-β-Ala-Tyr-Nal(2)-Leu-Pya(4)-Arg-Pro-Arg-Asn-NH2; or a salt thereof.
摘要翻译： 本发明涉及选自PEG20k（AL）-agr-Ala-Tyr-Nal（1）-Leu-Phe-Arg-Pro-Arg-Asn-NH2，PEG20k（AL） - （2）-Leu-Phe-Arg-Pro-Arg-Asn-NH 2，PEG20k（AL）-NpipAc-Tyr-Nal（2）-Leu-Phe-Arg-Pro-Arg- Asn-NH2，PEG20k（AL）-NpipAc-Tyr-Nal（2）-Leu-Phe-Arg-Ala-Arg-Asn-NH2，PEG20k（AL）-PEG（2）-Tyr-Nal（2）-Leu -Phe-Arg-NMeAla-Arg-Asn-NH2，PEG20k（AL）-Pic（4）-Tyr-Nal（2）-Leu-Phe-Arg-NMeAla-Arg-Asn-NH2，PEG20k（AL） -Tyr-Nal（2）-Leu-Phe-Arg-NMeAla-Arg-Asn-NH2和PEG20k（AL）-a-Tyr-Nal（2）-Leu-Pya（4）-Arg-Pro -Arg-Asn-NH2; 或其盐。
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公开(公告)号：US20090099334A1
公开(公告)日：2009-04-16
申请号：US12257931
申请日：2008-10-24
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
IPC分类号： C07K7/06
CPC分类号： C07K7/06
摘要： The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotrophic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, blood stability, solubility, etc. are more improved, gelation tendency is reduced, pharmacokinetics are also improved, and an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity is exhibited. Furthermore, the metastin derivative of the present invention has the effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc.
摘要翻译： 本发明提供具有优异生物活性（癌转移抑制活性，癌生长抑制活性，促性腺激素分泌刺激活性，性激素分泌刺激活性等）的稳定的转氨酶衍生物。 通过在本发明的转氨酶衍生物中代替具有特定氨基酸的组氨酸的氨基酸，血液稳定性，溶解性等进一步提高，凝胶化倾向降低，药代动力学改善，癌转移抑制活性优异， 显示出癌症生长抑制活性。 此外，本发明的转氨酶衍生物具有抑制促性腺激素分泌，抑制性激素分泌等作用。
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