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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：US08765909B2
公开(公告)日：2014-07-01
申请号：US12446142
申请日：2007-10-24
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
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：US20090215700A1
公开(公告)日：2009-08-27
申请号：US11977477
申请日：2007-10-24
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
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：US20090093615A1
公开(公告)日：2009-04-09
申请号：US12257981
申请日：2008-10-24
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
IPC分类号： C07K7/08
CPC分类号： C07K14/4703 , C07K7/02
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.
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公开(公告)号：US20120172293A1
公开(公告)日：2012-07-05
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
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：US08778871B2
公开(公告)日：2014-07-15
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.
摘要翻译： 本发明提供具有优异生物活性（癌转移抑制活性，癌生长抑制活性等）的稳定的转铁蛋白衍生物。 已经发现通过用特异性修饰基修饰转氨酶的构成氨基酸，具有比天然转移蛋白更多的改善的血液稳定性的转氨酶衍生物，并且显示出优异的癌症转移抑制活性或癌症生长抑制活性。 此外，已经发现这些转氨酶衍生物表现出抑制促性腺激素分泌，抑制性激素分泌等的作用，其完全不同于迄今已知的效果。
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公开(公告)号：US07960348B2
公开(公告)日：2011-06-14
申请号：US12158251
申请日：2006-12-21
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
CPC分类号： C07K14/4748 , A61K38/00 , C07K14/4703
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 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：US20110059888A1
公开(公告)日：2011-03-10
申请号：US12446142
申请日：2007-10-24
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
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：US20100331520A1
公开(公告)日：2010-12-30
申请号：US12158251
申请日：2006-12-21
申请人： Taiji Asami , Naoki Nishizawa
发明人： Taiji Asami , Naoki Nishizawa
IPC分类号： C07K7/06
CPC分类号： C07K14/4748 , A61K38/00 , C07K14/4703
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：US07625869B2
公开(公告)日：2009-12-01
申请号：US11630698
申请日：2005-06-23
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.
摘要翻译： 本发明提供具有优异生物活性（癌转移抑制活性，癌生长抑制活性等）的稳定的转铁蛋白衍生物。 已经发现通过用特异性修饰基修饰转氨酶的构成氨基酸，具有比天然转移蛋白更多的改善的血液稳定性的转氨酶衍生物，并且显示出优异的癌症转移抑制活性或癌症生长抑制活性。 此外，已经发现这些转氨酶衍生物表现出抑制促性腺激素分泌，抑制性激素分泌等的作用，其完全不同于迄今已知的效果。
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