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公开(公告)号：US07498297B2
公开(公告)日：2009-03-03
申请号：US10333485
申请日：2001-07-18
申请人： Hazel Szeto , Peter W. Schiller
发明人： Hazel Szeto , Peter W. Schiller
摘要： The present invention provides methods for stimulating a mu-opioid receptor agonist peptide in a mammal in need thereof. The methods comprise administering to the mammal an effective amount of a selective mu-opioid receptor agonist peptide that comprises at least two α-amino acid residues. At least one of the amino acid residues has a positive charge. The amino acid residue in the first position is a tyrosine or tyrosine derivative. The amino acid in the second position is a D-α-amino acid. The present invention also provides methods of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the peptides.
摘要翻译： 本发明提供了在有需要的哺乳动物中刺激μ-阿片受体激动剂肽的方法。 所述方法包括向哺乳动物施用有效量的包含至少两个α-氨基酸残基的选择性μ-阿片受体激动剂肽。 至少一个氨基酸残基具有正电荷。 第一位置的氨基酸残基是酪氨酸或酪氨酸衍生物。 第二个位置的氨基酸是D-α-氨基酸。 本发明还提供了通过向哺乳动物施用有效量的肽来治疗患有病症或疾病的哺乳动物的方法。
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公开(公告)号：US07732398B2
公开(公告)日：2010-06-08
申请号：US11427606
申请日：2006-06-29
申请人： Hazel Szeto , Peter W. Schiller
发明人： Hazel Szeto , Peter W. Schiller
摘要： The present invention provides methods for stimulating mu-opioid receptors with agonist peptides in a mammal in need thereof. The methods comprise administering to the mammal an effective amount of a selective mu-opioid receptor agonist peptide that comprises at least two α-amino acid residues. At least one of the amino acid residues has a positive charge. The amino acid residue in the first position is a tyrosine or tyrosine derivative. The amino acid in the second position is a D-α-amino acid. The present invention also provides methods of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the peptides.
摘要翻译： 本发明提供了在有需要的哺乳动物中用激动剂肽刺激μ-阿片受体的方法。 所述方法包括向哺乳动物施用有效量的包含至少两个α-氨基酸残基的选择性μ-阿片受体激动剂肽。 至少一个氨基酸残基具有正电荷。 第一位置的氨基酸残基是酪氨酸或酪氨酸衍生物。 第二个位置的氨基酸是D-α-氨基酸。 本发明还提供了通过向哺乳动物施用有效量的肽来治疗患有病症或疾病的哺乳动物的方法。
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公开(公告)号：US07576061B2
公开(公告)日：2009-08-18
申请号：US10771232
申请日：2004-02-03
申请人： Hazel H. Szeto , Kesheng Zhao , Peter W. Schiller
发明人： Hazel H. Szeto , Kesheng Zhao , Peter W. Schiller
CPC分类号： A61K38/07 , A61K38/03 , C07K5/1008 , C07K5/1016 , C07K5/1019 , C07K5/1024
摘要： The invention provides a method of reducing or preventing mitochondrial permeability transitioning. The method comprises administering an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3pm is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 2a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1.
摘要翻译： 本发明提供了减少或预防线粒体渗透性转换的方法。 该方法包括施用有效量的具有至少一个净正电荷的芳族阳离子肽; 至少4个氨基酸; 最多约20个氨基酸; 净正电荷（pm）的最小数量与氨基酸残基总数（r）之间的关系，其中3pm是小于或等于r + 1的最大数量; 以及芳族基团（a）的最小数目和净正电荷总数（pt）之间的关系，其中2a是小于或等于pt + 1的最大数目，除了当a为1时，pt可以 也是1。
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4.发明授权
公开(公告)号：US5455230A
公开(公告)日：1995-10-03
申请号：US21773
申请日：1993-02-24
申请人： Peter W. Schiller
发明人： Peter W. Schiller
CPC分类号： C07K5/0812 , C07K5/1016 , A61K38/00
摘要： Compounds of the formula I as well as a process for their preparation, their pharmaceutical preparations and their useH--Tyr--Tic--X (I)wherein X is--Phe--OH,--Phe--NH.sub.2,--Phe--Phe--OH,--Phe--Phe--NH.sub.2,--Trp--Phe--NH.sub.2,--Trp--Phe--OH,--Phe--Phe(p-NO.sub.2)--OH,--Trp--Phe(p-NO.sub.2)--H or--Phe--Trp--NH.sub.2.
摘要翻译： 式I化合物及其制备方法，其药物制剂及其用途H-Tyr-Tic-X（I）其中X为-Phe-OH，-Phe-NH 2，-Phe-Phe-OH， -Phe-Phe-NH 2，-Trp-Phe-NH 2，-Trp-Phe-OH，-Phe-Phe（p-NO 2）-OH，-Trp-Phe（p-NO 2）-H或-Phe-Trp- NH2。
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公开(公告)号：US20120329730A1
公开(公告)日：2012-12-27
申请号：US13519083
申请日：2011-01-24
申请人： Hazel H. Szeto , Peter W. Schiller
发明人： Hazel H. Szeto , Peter W. Schiller
CPC分类号： C07K7/06 , A61K38/00 , C07K5/0817 , C07K5/10 , C07K5/1019
摘要： The disclosure provides aromatic-cationic peptide compositions and methods of preventing or treating disease using the same. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof.
摘要翻译： 本公开提供了芳香族 - 阳离子肽组合物和使用其的预防或治疗疾病的方法。 所述方法包括向有需要的受试者施用有效量的芳族阳离子肽。
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6.发明授权公开(公告)号：US07718620B2
公开(公告)日：2010-05-18
申请号：US11427804
申请日：2006-06-30
申请人： Hazel H. Szeto , Kesheng Zhao , Peter W. Schiller
发明人： Hazel H. Szeto , Kesheng Zhao , Peter W. Schiller
IPC分类号： A61K38/07
CPC分类号： A61K38/07 , A61K38/03 , C07K5/1008 , C07K5/1016 , C07K5/1019 , C07K5/1024
摘要： The invention provides a method of treating or preventing ischemia-reperfusion injury of the kidney in a mammal. The method comprises administering an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3pm is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 2 a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1.
摘要翻译： 本发明提供了治疗或预防哺乳动物肾脏缺血再灌注损伤的方法。 该方法包括施用有效量的具有至少一个净正电荷的芳族阳离子肽; 至少四个氨基酸; 最多约20个氨基酸; 净正电荷（pm）的最小数量与氨基酸残基总数（r）之间的关系，其中3pm是小于或等于r + 1的最大数量; 以及芳族基团（a）的最小数量和净正电荷总数（pt）之间的关系，其中2 a是小于或等于pt + 1的最大数目，除了当a为1时，pt 也可能是1。
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公开(公告)号：US5602100A
公开(公告)日：1997-02-11
申请号：US238038
申请日：1994-04-21
CPC分类号： C07K7/06 , C07K5/1016 , A61K38/00
摘要： This invention relates to novel dermorphin analogs having pharmacological activity. More particularly, this invention relates to novel tetrapeptides having specific structural features and a net charge of +2 or greater. The peptides of this invention are useful in treating pain and gastro-intestinal disorders. Accordingly, this invention also relates to pharmaceutical compositions comprising those peptides and methods for treating pain and gastro-intestinal disorders.
摘要翻译： 本发明涉及具有药理学活性的新型皮质烯类似物。 更具体地说，本发明涉及具有特定结构特征和+2以上净电荷的新型四肽。 本发明的肽可用于治疗疼痛和胃肠道疾病。 因此，本发明还涉及包含这些肽的药物组合物和治疗疼痛和胃肠道疾病的方法。
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公开(公告)号：US5312899A
公开(公告)日：1994-05-17
申请号：US374521
申请日：1989-06-30
申请人： Peter W. Schiller
发明人： Peter W. Schiller
CPC分类号： C07K7/06 , C07K5/1016 , A61K38/00
摘要： Peptides are provided which are suitable for the treatment of pain and gastro-intestinal disorders, such as diarrhea, and are represented by the structure: ##STR1## where values for the substituents and n are disclosed herein. Methods for preparing these peptides by solution and solid phase syntheses are also provided. Pharmaceutical compositions utilizing these peptides in a pharmaceutically effective amount and methods of treatment using them are provided.
摘要翻译： 提供了适合于治疗疼痛和胃肠道疾病（例如腹泻）的肽，并且由以下结构表示：其中本文公开了取代基和n的值。 还提供了通过溶液和固相合成制备这些肽的方法。 提供了利用这些肽具有药学有效量的药物组合物和使用它们的治疗方法。
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公开(公告)号：US20130244957A1
公开(公告)日：2013-09-19
申请号：US13778994
申请日：2013-02-27
申请人： Hazel H. Szeto , Peter W. Schiller , Kesheng Zhao
发明人： Hazel H. Szeto , Peter W. Schiller , Kesheng Zhao
IPC分类号： A61K38/07
CPC分类号： A61K38/07 , A61K38/03 , C07K5/1008 , C07K5/1016 , C07K5/1019 , C07K5/1024
摘要： The invention provides a method of reducing or preventing mitochondrial permeability transitioning. The method comprises administering an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3pm is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 2 a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1.
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公开(公告)号：US08404646B2
公开(公告)日：2013-03-26
申请号：US13247648
申请日：2011-09-28
申请人： Peter W. Schiller , Hazel H. Szeto , Kesheng Zhao
发明人： Peter W. Schiller , Hazel H. Szeto , Kesheng Zhao
IPC分类号： A61K38/07
CPC分类号： A61K38/07 , A61K38/03 , C07K5/1008 , C07K5/1016 , C07K5/1019 , C07K5/1024
摘要： The invention provides a method of reducing or preventing mitochondrial permeability transitioning. The method comprises administering an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3pm is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 2 a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1.
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