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公开(公告)号：US20060233747A1
公开(公告)日：2006-10-19
申请号：US11446419
申请日：2006-06-05
申请人： Gerd Kochendoerfer , Paolo Botti , James Bradburne , Shiah -yun Chen , Sonya Cressman , Christie Hunter , Stephen Kent , Donald Low , Jill Wilken
发明人： Gerd Kochendoerfer , Paolo Botti , James Bradburne , Shiah -yun Chen , Sonya Cressman , Christie Hunter , Stephen Kent , Donald Low , Jill Wilken
IPC分类号： A61K38/19 , A61K38/20 , C07K14/52 , C07K14/53 , C07K14/54 , C07K14/56 , C07H21/04 , C12P21/02
CPC分类号： C07K14/52 , C07K1/1077 , C12P21/02
摘要： The present invention relates to methods and compositions for modifying peptides, polypeptides and proteins with polymers, especially glyco-mimetic polymers, so as to improve their biological activity or pharmacokinetic properties. The invention further provides methods and uses for such polymer-modified peptides, polypeptides and proteins. The invention is particularly suitable for use in the synthesis of polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.
摘要翻译： 本发明涉及用聚合物，特别是糖模拟聚合物修饰肽，多肽和蛋白质的方法和组合物，以改善其生物学活性或药代动力学性质。 本发明进一步提供了这种聚合物修饰的肽，多肽和蛋白质的方法和用途。 本发明特别适用于合成聚合物改性的合成生物活性蛋白质和含有这种蛋白质的药物组合物。
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公开(公告)号：US07118737B2
公开(公告)日：2006-10-10
申请号：US10332385
申请日：2001-07-12
申请人： Gerd G. Kochendoerfer , Paolo Botti , James A. Bradburne , Shiah-yun Chen , Sonya Cressman , Christie L. Hunter , Stephen B. H. Kent , Donald W. Low , Jill G. Wilken
发明人： Gerd G. Kochendoerfer , Paolo Botti , James A. Bradburne , Shiah-yun Chen , Sonya Cressman , Christie L. Hunter , Stephen B. H. Kent , Donald W. Low , Jill G. Wilken
CPC分类号： C07K14/52 , C07K1/1077 , C12P21/02
摘要： The present invention relates to methods and compositions for modifying peptides, polypeptides and proteins with polymers, especially glyco-mimetic polymers, so as to improve their biological activity or pharmacokinetic properties. The invention further provides methods and uses for such polymer-modified peptides, polypeptides and proteins. The invention is particularly suitable for use in the synthesis of polymer-modified synthetic bioactive proteins (FIG. 1D), and of pharmaceutical compositions that contain such proteins.
摘要翻译： 本发明涉及用聚合物，特别是糖模拟聚合物修饰肽，多肽和蛋白质的方法和组合物，以改善其生物学活性或药代动力学性质。 本发明进一步提供了这种聚合物修饰的肽，多肽和蛋白质的方法和用途。 本发明特别适用于合成聚合物改性的合成生物活性蛋白（图1D）和含有这种蛋白质的药物组合物。
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3.发明申请INDOLE COMPOUNDS HAVING C4-ACIDIC SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS 审中-公开具有C4-酸性取代基的单一化合物及其作为磷脂酶A2抑制剂的用途公开(公告)号：US20090318492A1
公开(公告)日：2009-12-24
申请号：US12092380
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Shiah-yun Chen , Jerry M. Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Shiah-yun Chen , Jerry M. Buysse
IPC分类号： A61K31/437 , A61K31/40 , C07D471/02 , C07D209/04
CPC分类号： C07D209/32
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.
摘要翻译： 公开了吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。
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公开(公告)号：US07030218B2
公开(公告)日：2006-04-18
申请号：US10332386
申请日：2001-07-12
申请人： Christie L. Hunter , Paolo Botti , James A. Bradburne , Shiah-yun Chen , Sonya Cressman , Stephen B. H. Kent , Gerd G. Kochendoerfer , Donald W. Low
发明人： Christie L. Hunter , Paolo Botti , James A. Bradburne , Shiah-yun Chen , Sonya Cressman , Stephen B. H. Kent , Gerd G. Kochendoerfer , Donald W. Low
CPC分类号： C07K14/505 , A61K38/00
摘要： The present invention concerns methods and compositions for extending the technique of native chemical ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond (see FIG. 1). The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.
摘要翻译： 本发明涉及通过酰胺键扩展更宽范围的肽，多肽，其它聚合物和其它分子的天然化学连接技术的方法和组合物（参见图1）。 本发明还提供了这些蛋白质和衍生化蛋白质的方法和用途。 本发明特别适用于合成任选的聚合物改性的合成生物活性蛋白质和含有这种蛋白质的药物组合物。
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5.发明申请Phospholipase inhibitors, including multi-valent phospholipase inhibitors, and use thereof, including as lumen-localized phospholipase inhibitors 审中-公开磷脂酶抑制剂，包括多价磷脂酶抑制剂及其用途，包括作为内腔定位的磷脂酶抑制剂公开(公告)号：US20070135383A1
公开(公告)日：2007-06-14
申请号：US11593176
申请日：2006-11-03
申请人： Han-Ting Chang , Dominque Charmot , Tomasz Glinka , Michael Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry Buysse
发明人： Han-Ting Chang , Dominque Charmot , Tomasz Glinka , Michael Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry Buysse
IPC分类号： A61K31/685 , A61K31/66 , A61K31/503 , A61K31/4745 , A61K31/405 , A61K31/365
CPC分类号： A61K31/404 , A61K9/0019 , A61K9/0095 , A61K31/41 , A61K31/66 , A61K47/10 , A61K47/20 , A61K47/55 , A61K47/58
摘要： The present invention provides methods and compositions for the treatment of phospholipase-related conditions. In particular, the invention provides a method of treating insulin-related, weight-related conditions and/or cholesterol-related conditions in an animal subject. The method generally involves the administration of a non-absorbed and/or effluxed phospholipase A2 inhibitor that is localized in a gastrointestinal lumen.
摘要翻译： 本发明提供了治疗磷脂酶相关病症的方法和组合物。 特别地，本发明提供了一种在动物受试者中治疗胰岛素相关，体重相关病症和/或胆固醇相关病症的方法。 该方法通常涉及施用定位在胃肠腔中的未吸收和/或流出的磷脂酶A2抑制剂。
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公开(公告)号：US20060149039A1
公开(公告)日：2006-07-06
申请号：US11340730
申请日：2006-01-27
申请人： Christie Hunter , Paolo Botti , James Bradburne , Shiah-yun Chen , Sonya Cressman , Stephen Kent , Gerd Kochendoerfer , Donald Low
发明人： Christie Hunter , Paolo Botti , James Bradburne , Shiah-yun Chen , Sonya Cressman , Stephen Kent , Gerd Kochendoerfer , Donald Low
CPC分类号： C07K14/505 , A61K38/00
摘要： The present invention concerns methods and compositions for extending the technique of native chemical ligation to permit the ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond. The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.
摘要翻译： 本发明涉及用于延伸天然化学连接技术以允许通过酰胺键连接更宽范围的肽，多肽，其它聚合物和其它分子的方法和组合物。 本发明还提供了这些蛋白质和衍生化蛋白质的方法和用途。 本发明特别适用于合成任选的聚合物改性的合成生物活性蛋白质和含有这种蛋白质的药物组合物。
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7.发明申请Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors 有权多价吲哚化合物及其作为磷脂酶A2抑制剂的用途公开(公告)号：US20070135385A1
公开(公告)日：2007-06-14
申请号：US11593177
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry Buysse
IPC分类号： A61K31/675 , A61K31/404 , C07D209/36
CPC分类号： C07D209/18 , C07D471/04 , C07D487/04
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.
摘要翻译： 公开了吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。
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8.发明授权Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors 有权多价吲哚化合物及其作为磷脂酶A2抑制剂的用途公开(公告)号：US07666898B2
公开(公告)日：2010-02-23
申请号：US11593177
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry M. Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Damien Cartigny , Shiah-yun Chen , Jerry M. Buysse
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D209/18 , C07D471/04 , C07D487/04
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.
摘要翻译： 公开了吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。
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9.发明申请INDOLE COMPOUNDS HAVING C4-AMIDE SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS 审中-公开具有C4酰胺取代基的单一化合物及其作为磷脂酶A2抑制剂的用途公开(公告)号：US20090306171A1
公开(公告)日：2009-12-10
申请号：US12092388
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Shiah-yun Chen , Jerry M. Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Shiah-yun Chen , Jerry M. Buysse
IPC分类号： A61K31/404 , C07D209/20
CPC分类号： C07D209/22
摘要： Indole and indole-related compounds according to the formula (I) or (II) optionally having additional heteroatoms, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. Formula (I), formula (II). R4 being a moiety represented by formula (C4-II-C), R3 being a moiety represented by formula (C3-I or C3-II).
摘要翻译： 公开了根据式（I）或（II）的任选具有其它杂原子的吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。 式（I），式（II）。 R4是由式（C4-II-C）表示的部分，R3是由式（C3-I或C3-II）表示的部分。
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10.发明申请公开(公告)号：US20090239896A1
公开(公告)日：2009-09-24
申请号：US12092385
申请日：2006-11-03
申请人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Tony Kwok-Kong Mong , Shiah-yun Chen , Jerry M. Buysse
发明人： Han-Ting Chang , Dominique Charmot , Tomasz Glinka , Michael James Cope , Elizabeth Goka , Jun Shao , Tony Kwok-Kong Mong , Shiah-yun Chen , Jerry M. Buysse
IPC分类号： A61K31/437 , C07D471/04 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. The compounds include azaindoles of the formula below [insert FIG. 6c] in which at least one of CR4, CR5, CR6 and CR7 is replaced by N, and the groups R1-R7 are defined as in claim 1.
摘要翻译： 公开了吲哚和吲哚相关化合物，组合物和方法。 本发明的化合物可用作磷脂酶抑制剂。 本发明的化合物和组合物可用于治疗动物受试者中磷脂酶相关病症，例如胰岛素相关，体重相关和/或胆固醇相关病症。 这些化合物包括下式的氮杂吲哚[ 6c]，其中CR4，CR5，CR6和CR7中的至少一个被N替代，基团R1-R7如权利要求1中所定义。
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