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1. 发明申请

WO2009155258A3 GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 审中-公开
标题翻译： GLUCAGON / GLP-1受体协同作用
公开(公告)号：WO2009155258A3
公开(公告)日：2010-02-18
申请号：PCT/US2009047438
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP , DIMARCHI RICHARD D , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
发明人： DIMARCHI RICHARD D , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
IPC分类号： A61K38/00
CPC分类号： C07K14/605
摘要： Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP- 1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C- terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).
摘要翻译：公开了相对于天然胰高血糖素在胰高血糖素受体上具有增强的效力的改良的胰高血糖素肽。通过形成分子内桥或通过酰胺基取代末端羧酸对胰高血糖素肽进一步修饰产生显示胰高血糖素/ GLP-1受体共激动剂活性的肽。通过聚乙二醇化，酰化，烷基化，羧基末端氨基酸的取代，C-末端截短或加入选自下组的羧基末端肽，可以进一步改善这些高效胰高血糖素类似物的溶解度和稳定性由SEQ ID NO：26（GPSSGAPPPS），SEQ ID NO：27（KRNRNNIA）和SEQ ID NO：28（KRNR）组成。

2. 发明公开

EP2300037A4 GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 有权
标题翻译：胰高血糖素COAGONISTEN / GLP-1受体
公开(公告)号：EP2300037A4
公开(公告)日：2011-07-06
申请号：EP09767568
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： DIMARCHI RICHARD D , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
IPC分类号： A61K38/00
CPC分类号： C07K14/605

3. 发明专利

AU2009260302B2 Glucagon/GLP-1 receptor co-agonists 未知
公开(公告)号：AU2009260302B2
公开(公告)日：2014-10-23
申请号：AU2009260302
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： DAY JONATHAN , CHABENNE JOSEPH , SMILEY DAVID L , WARD BRIAN C , PATTERSON JAMES , DIMARCHI RICHARD D , DIMARCHI MARIA
IPC分类号： C07K14/605 , A61K38/00
摘要： Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP- 1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C- terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).

4. 发明专利

EA019203B9 КОАГОНИСТЫ ГЛЮКАГОНОВОГО РЕЦЕПТОРА/GLP-1-РЕЦЕПТОРА 未知
公开(公告)号：EA019203B9
公开(公告)日：2014-03-31
申请号：EA201100038
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： DIMARCHI RICHARD D , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
IPC分类号： A61K38/00
摘要： Визобретениираскрытымодифицированныеглюкагоновыепептиды, имеющиеповышеннуюэффективностьнаглюкагоновомрецепторепосравнениюс нативнымглюкагоном. Благодарямодификацииглюкагоновыхпептидовпосредствомобразованиявнутримолекулярныхмостиковилипосредствомзаменыконцевойкарбоновойкислотыамиднойгруппойполучаютпептиды, демонстрирующиеактивностькоагонистовнаглюкагоновомрецепторе/GLP-1-рецепторе. Растворимостьи стабильностьэтихвысокоэффективныханалоговглюкагонаможеттакжебытьповышенамодификациейполипептидовпосредствомпэгилирования, ацилирования, алкилирования, заменыкарбоксиконцевыхаминокислот, С-концевогоусечениялибодобавлениякарбоксиконцевогопептида, выбранногоизгруппы, которуюсоставляютпоследовательность SEQ ID NO: 26 (GPSSGAPPPS), последовательность SEQ ID NO: 27 (KRNRNNIA) ипоследовательность SEQ ID NO: 28 (KRNR).

5. 发明专利

PE20100255A1 CO-AGONISTAS DEL RECEPTOR DE GLUCAGON/GLP-1 未知
公开(公告)号：PE20100255A1
公开(公告)日：2010-04-25
申请号：PE2009000875
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： DIMARCHI RICHARD , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
IPC分类号： A61K38/00 , C07K14/605
摘要： SE REFIERE A UN PEPTIDO DE TIPO GLUCAGON MODIFICADO, CARACTERIZADO POR LA FORMACION DE PUENTES INTRAMOLECULARES O LA SUSTITUCION DE LOS ACIDOS CARBOXILICOS TERMINALES CON UN GRUPO AMIDA; LA SOLUBILIDAD Y ESTABILIDAD SON MEJORADAS MEDIANTE LA MODIFICACION DE LOS POLIPEPTIDOS POR ACILACION, ALQUILACION O LA ADICION DE UN PEPTIDO CARBOXILO TERMINAL SELECCIONADO DEL GRUPO QUE CONSISTE EN SEC ID NO: 26, SEC ID NO: 27 Y SEC ID NO: 28. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHO PEPTIDO PRESENTA CO-ACTIVIDAD AGONISTA DE LOS RECEPTORES DE GLUCAGON/GLP-1 Y ES UTIL EN EL TRATAMIENTO DE HIPOGLUCEMIA Y DIABETES-2

6. 发明专利

CA2728284C GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 未知
公开(公告)号：CA2728284C
公开(公告)日：2019-09-10
申请号：CA2728284
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： DIMARCHI RICHARD D , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
IPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61P3/04 , A61P3/10 , C07K14/72
摘要： Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).

7. 发明专利

AU2009260302A1 Glucagon/GLP-1 receptor co-agonists 未知
公开(公告)号：AU2009260302A1
公开(公告)日：2009-12-23
申请号：AU2009260302
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： SMILEY DAVID L , DAY JONATHAN , PATTERSON JAMES , DIMARCHI RICHARD D , WARD BRIAN C , CHABENNE JOSEPH , DIMARCHI MARIA
IPC分类号： C07K14/605 , A61K38/00

8. 发明专利

AR072160A1 CO-AGONISTAS DEL RECEPTOR DE GLUCAGON/GLP-1 未知
公开(公告)号：AR072160A1
公开(公告)日：2010-08-11
申请号：ARP090102181
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： SMILEY DAVID L , DAY JONATHAN , PATTERSON JAMES , CHABENNE JOSEPH , DIMARCHI MARIA , WARD BRIAN C , DIMARCHI RICHARD D
IPC分类号： C07K14/605 , A61K38/00 , C07K14/435
摘要： Peptidos tipo glucagon modificados que tienen potencia aumentada en el receptor de glucagon en relacion con el glucagon nativo. La modificacion adicional del peptido tipo glucagon con formacion de puentes intramoleculares o la sustitucion del cido terminal carbox¡lico con un grupo amida produce peptidos que exhiben actividad co- agonista de glucagon/Receptor de GLP-1. La solubilidad y estabilidad de estos an logos de glucagon de alta potencia pueden variar por modificacion de polipeptidos mediante pegilacion, acilacion, alquilacion, sustitucion de amino cidos de carboxi terminal, truncacion C-terminal, o adicion de un peptido C-terminal seleccionado del grupo formado por ID SEC NO: 26 (GPSSGAPPPS), ID SEC NO: 27 (KRNRNNIA) y ID SEC NO: 28 (KRNR). Reivindicacion 1: Un peptido tipo glucagon que comprende una secuencia de amino cido de ID SEC NO: 1 con hasta diez modificaciones de amino cidos y que comprende un amino cido en la posicion 10 que se acila o alquila con un C4 a C30 cido graso.

9. 发明专利

PE02552010A1 CO-AGONISTAS DEL RECEPTOR DE GLUCAGON/GLP-1 未知
公开(公告)号：PE02552010A1
公开(公告)日：2010-04-25
申请号：PE0008752009
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： DIMARCHI RICHARD , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
IPC分类号： A61K38/00 , C07K14/605
CPC分类号： C07K14/605
摘要： SE REFIERE A UN PEPTIDO DE TIPO GLUCAGON MODIFICADO, CARACTERIZADO POR LA FORMACION DE PUENTES INTRAMOLECULARES O LA SUSTITUCION DE LOS ACIDOS CARBOXILICOS TERMINALES CON UN GRUPO AMIDA; LA SOLUBILIDAD Y ESTABILIDAD SON MEJORADAS MEDIANTE LA MODIFICACION DE LOS POLIPEPTIDOS POR ACILACION, ALQUILACION O LA ADICION DE UN PEPTIDO CARBOXILO TERMINAL SELECCIONADO DEL GRUPO QUE CONSISTE EN SEC ID NO: 26, SEC ID NO: 27 Y SEC ID NO: 28. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHO PEPTIDO PRESENTA CO-ACTIVIDAD AGONISTA DE LOS RECEPTORES DE GLUCAGON/GLP-1 Y ES UTIL EN EL TRATAMIENTO DE HIPOGLUCEMIA Y DIABETES-2

10. 发明专利

CA2728284A1 GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 未知
公开(公告)号：CA2728284A1
公开(公告)日：2009-12-23
申请号：CA2728284
申请日：2009-06-16
申请人： UNIV INDIANA RES & TECH CORP
发明人： DIMARCHI RICHARD D , SMILEY DAVID L , DIMARCHI MARIA , CHABENNE JOSEPH , DAY JONATHAN , PATTERSON JAMES , WARD BRIAN C
IPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61P3/04 , A61P3/10 , C07K14/72
摘要： Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP- 1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C- terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).

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