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1. 发明申请

US20110150884A1 CRYSTALLINE COMPOSITION OF GM-CSF/GM-CSFR 失效
标题翻译： GM-CSF / GM-CSFR的晶体组成
公开(公告)号：US20110150884A1
公开(公告)日：2011-06-23
申请号：US12513497
申请日：2007-11-01
申请人： Guido Hansen , Timothy Robert Hercus , Angel Francisco Lopez , William John Mckinstry , Michael William Parker
发明人： Guido Hansen , Timothy Robert Hercus , Angel Francisco Lopez , William John Mckinstry , Michael William Parker
IPC分类号： A61K39/395 , C07K14/715 , G01N33/53 , C07K16/28 , C07K16/24 , A61P29/00 , A61P35/02 , A61P11/06 , G06G7/60
CPC分类号： C07K14/535 , C07K14/7153 , C07K2299/00
摘要： The present invention relates generally to the field of crystallography. More particularly, the present invention provides crystalline forms of a complex between granulocyte macrophage-colony stimulating factor (GM-CSF) and its receptor (GM-CSFR). The present invention further provides methods for the design and selection of modulators of GM-CSF/GM-CSFR interaction and signaling as well as signaling of other cytokines.
摘要翻译：本发明一般涉及晶体学领域。更具体地，本发明提供粒细胞巨噬细胞集落刺激因子（GM-CSF）与其受体（GM-CSFR）之间的复合物的结晶形式。本发明还提供了用于设计和选择GM-CSF / GM-CSFR相互作用和信号传导调节剂以及其他细胞因子信号传导的方法。

2. 发明申请

US20080194636A1 Enzyme Inhibitors and Uses Thereof 审中-公开
标题翻译：酶抑制剂及其用途
公开(公告)号：US20080194636A1
公开(公告)日：2008-08-14
申请号：US11662392
申请日：2005-09-09
申请人： Siew Yeen Chai , Michael William Parker , Anthony Lloyd Albiston , Craig J. Morton , Hooi Ling Ng , Siying Ye , Frederick A.O. Mendelsohn
发明人： Siew Yeen Chai , Michael William Parker , Anthony Lloyd Albiston , Craig J. Morton , Hooi Ling Ng , Siying Ye , Frederick A.O. Mendelsohn
IPC分类号： A61K31/4433 , C12N9/99 , A61K31/352 , C12Q1/37 , A61P25/00
CPC分类号： C12N9/48 , A61K31/352 , A61K31/4433 , G01N2500/02
摘要： The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions, regulating cellular glucose uptake and homeostasis, inducing labour and lactation, and other disorders or conditions wherein excessive or undesirable IRAP activity is implicated.
摘要翻译：本发明涉及胰岛素调节氨基肽酶抑制剂（IRAP）及其抑制方法，以及包含所述抑制剂的组合物。特别地，本发明的抑制剂可用于治疗应用，包括增强记忆和学习功能，调节细胞葡萄糖摄取和体内平衡，诱导劳动和哺乳期以及涉及过度或不期望的IRAP活性的其它病症或病症。

3. 发明授权

US08377963B2 Insulin-regulated aminopeptidase (IRAP) inhibitors and uses thereof 失效
标题翻译：胰岛素调节氨肽酶（IRAP）抑制剂及其用途
公开(公告)号：US08377963B2
公开(公告)日：2013-02-19
申请号：US13570938
申请日：2012-08-09
申请人： Siew Yeen Chai , Michael William Parker , Anthony Lloyd Albiston , Frederick A. O. Mendelsohn , Keith Geoffrey Watson
发明人： Siew Yeen Chai , Michael William Parker , Anthony Lloyd Albiston , Frederick A. O. Mendelsohn , Keith Geoffrey Watson
IPC分类号： C07D407/04 , A61K31/4433 , A61K31/4725
CPC分类号： C07D405/04
摘要： The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.
摘要翻译：本发明涉及胰岛素调节氨基肽酶抑制剂（IRAP）及其抑制方法，以及包含所述抑制剂的组合物。特别地，本发明的抑制剂可用于治疗应用，包括增强记忆和学习功能。

4. 发明授权

US08263775B2 Insulin-regulated aminopeptidase (IRAP) inhibitors and uses thereof 失效
标题翻译：胰岛素调节氨肽酶（IRAP）抑制剂及其用途
公开(公告)号：US08263775B2
公开(公告)日：2012-09-11
申请号：US12743225
申请日：2008-11-18
申请人： Siew Yeen Chai , Michael William Parker , Anthony Lloyd Albiston , Frederick A. O. Mendelsohn , Keith Geoffrey Watson
发明人： Siew Yeen Chai , Michael William Parker , Anthony Lloyd Albiston , Frederick A. O. Mendelsohn , Keith Geoffrey Watson
IPC分类号： C07D407/04
CPC分类号： C07D405/04
摘要： The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.
摘要翻译：本发明涉及胰岛素调节氨基肽酶抑制剂（IRAP）及其抑制方法，以及包含所述抑制剂的组合物。特别地，本发明的抑制剂可用于治疗应用，包括增强记忆和学习功能。

5. 发明授权

US08489339B2 Crystalline composition of GM-CSF/GM-CSFR 失效
标题翻译： GM-CSF / GM-CSFR的结晶组成
公开(公告)号：US08489339B2
公开(公告)日：2013-07-16
申请号：US12513497
申请日：2007-11-01
申请人： Guido Hansen , Timothy Robert Hercus , Angel Francisco Lopez , William John McKinstry , Michael William Parker
发明人： Guido Hansen , Timothy Robert Hercus , Angel Francisco Lopez , William John McKinstry , Michael William Parker
IPC分类号： G01N23/02
CPC分类号： C07K14/535 , C07K14/7153 , C07K2299/00
摘要： The present invention relates generally to the field of crystallography. More particularly, the present invention provides crystalline forms of a complex between granulocyte macrophage-colony stimulating factor (GM-CSF) and its receptor (GM-CSFR). The present invention further provides methods for the design and selection of modulators of GM-CSF/GM-CSFR interaction and signaling as well as signaling of other cytokines.
摘要翻译：本发明一般涉及晶体学领域。更具体地，本发明提供粒细胞巨噬细胞集落刺激因子（GM-CSF）与其受体（GM-CSFR）之间的复合物的结晶形式。本发明还提供了用于设计和选择GM-CSF / GM-CSFR相互作用和信号传导调节剂以及其他细胞因子信号传导的方法。

6. 发明申请

US20110021563A1 INSULIN-REGULATED AMINOPEPTIDASE (IRAP) INHIBITORS AND USES THEREOF 失效
标题翻译：胰岛素调节氨基酸抑制剂（IRAP）抑制剂及其用途
公开(公告)号：US20110021563A1
公开(公告)日：2011-01-27
申请号：US12743225
申请日：2008-11-18
申请人： Siew Yeen Chai , Michael William Parker , Anthony Lloyd Albiston , Frederick A.O. Mendelsohn , Keith Geoffrey Watson
发明人： Siew Yeen Chai , Michael William Parker , Anthony Lloyd Albiston , Frederick A.O. Mendelsohn , Keith Geoffrey Watson
IPC分类号： C07D407/04 , A61K31/4725 , A61K31/4433 , C12Q1/37
CPC分类号： C07D405/04
摘要： The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.
摘要翻译：本发明涉及胰岛素调节氨基肽酶抑制剂（IRAP）及其抑制方法，以及包含所述抑制剂的组合物。特别地，本发明的抑制剂可用于治疗应用，包括增强记忆和学习功能。

7. 发明申请

US20120309787A1 INSULIN-REGULATED AMINOPEPTIDASE (IRAP) INHIBITORS AND USES THEREOF 失效
标题翻译：胰岛素调节氨基酸抑制剂（IRAP）抑制剂及其用途
公开(公告)号：US20120309787A1
公开(公告)日：2012-12-06
申请号：US13570938
申请日：2012-08-09
申请人： SIEW YEEN CHAI , Michael William Parker , Anthony Lloyd Albiston , Frederick A.O. Mendelsohn , Keith Geoffrey Watson
发明人： SIEW YEEN CHAI , Michael William Parker , Anthony Lloyd Albiston , Frederick A.O. Mendelsohn , Keith Geoffrey Watson
IPC分类号： A61K31/4709 , A61P25/00
CPC分类号： C07D405/04
摘要： The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.
摘要翻译：本发明涉及胰岛素调节氨基肽酶抑制剂（IRAP）及其抑制方法，以及包含所述抑制剂的组合物。特别地，本发明的抑制剂可用于治疗应用，包括增强记忆和学习功能。

8. 发明授权

US07220829B2 Cytokine binding domain of cytokine receptors 失效
标题翻译：细胞因子受体的细胞因子结合结构域
公开(公告)号：US07220829B2
公开(公告)日：2007-05-22
申请号：US09913419
申请日：2001-08-08
申请人： Jamie Rossjohn , William John McKinstry , Joanna May Woodcock , Michael William Parker , Angel Francisco Lopez , Christopher James Bagley
发明人： Jamie Rossjohn , William John McKinstry , Joanna May Woodcock , Michael William Parker , Angel Francisco Lopez , Christopher James Bagley
IPC分类号： C07K14/715
CPC分类号： C07K14/715 , A61K38/00 , C07K16/2866 , C07K2317/565
摘要： The present invention provides a cytokine-binding domain or portion thereof which binds to at least one cytokine and is capable of transducing a cytokine signal through a single cytokine receptor, said domain comprising a portion of the B′-C′ loop of domain 4 of a βc chain or analogous structure of a cytokine receptor. In another aspect of the invention there is provided a method of identifying a compound having cytokine agonist or antagonist activity, said method including subjecting a potential cytokine agonist and/or cytokine antagonist compound to a cytokine binding domain or portion thereof wherein said domain binds to at least one cytokine and is capable of transducing a cytokine signal through a single cytokine receptor, said domain comprising a portion of the B′-C′ loop of domain 4 of a βc chain or analogous structure of the cytokine receptor; and determining the presence of an agonist or antagonist response of the compound on the activity of a cytokine. In a preferred aspect there is provided a method fo identifying a GM-CSF, IL-3 and IL-5 agonist or antagonist, said method including: subjecting a potential agonist or antagonist to a GM-CSF, IL-3 and IL-5 binding domain or portion thereof wherein said domain binds to at least one of the cytokines and is capable of transducing a cytokine signal through a single cytokine receptor, said domain comprising a portion of the B′-C′ loop of domain 4 of a βc chain or analogous structure of the cytokine receptor; and determining the presence of a agonist or antagonist response from the compound on the activity of GM-CSF, IL-3 and IL-5.
摘要翻译：本发明提供了结合至少一种细胞因子并且能够通过单个细胞因子受体转导细胞因子信号的细胞因子结合结构域或其部分，所述结构域包含一部分结构域4的B'-C'环的部分细胞因子受体的β链或类似结构。在本发明的另一方面，提供了鉴定具有细胞因子激动剂或拮抗剂活性的化合物的方法，所述方法包括将潜在的细胞因子激动剂和/或细胞因子拮抗剂化合物经受细胞因子结合结构域或其部分，其中所述结构域结合于至少一种细胞因子，并且能够通过单个细胞因子受体转导细胞因子信号，所述结构域包含β3 C链的结构域4的部分B'-C'环或类似结构细胞因子受体; 并确定化合物的激动剂或拮抗剂应答对细胞因子活性的存在。在优选的方面，提供了鉴定GM-CSF，IL-3和IL-5激动剂或拮抗剂的方法，所述方法包括：使潜在的激动剂或拮抗剂对GM-CSF，IL-3和IL-5 结合结构域或其部分，其中所述结构域与至少一种细胞因子结合并且能够通过单个细胞因子受体转导细胞因子信号，所述结构域包含β4区域4的B'-C'环的一部分，细胞因子受体的链或类似结构; 并确定来自该化合物的激动剂或拮抗剂应答对GM-CSF，IL-3和IL-5的活性的存在。

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